目录号 | 产品详情 | 靶点 | |
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T75715 | |||
Nonapeptide-1 (Melanostatine-5) acetate salt,一种多肽类激素,是 MC1R 选择性拮抗剂 (Ki: 40 nM)。 Nonapeptide-1 acetate salt 是一种竞争性的α-MSH 拮抗剂,可有效抑制黑素细胞中 α-MSH 诱导的细胞内 cAMP 和黑素体扩散 (IC50分别为 2.5 nM 和 11 nM)。 Nonapeptide-1 acetate salt 抑制黑色素合成,可用于研究皮肤色素沉着和肾上腺类固醇生成的调节、皮肤癌。 | |||
T63939 | |||
JBJ-09-063 是一种突变选择性变构 EGFR 抑制剂,对 EGFRL858R、EGFR L858R/T790M、EGFR L858R/T790M/C797S 和 EGFRLT/L747S 的 IC50分别为 0.147 nM、0.063 nM、0.083 nM 和 0.396 nM。JBJ-09-063 有效降低 EGFR、Akt 和 ERK1/2 磷酸化。JBJ-09-063 对EGFR 酪氨酸激酶抑制剂 (TKI) 敏感与耐药模型均有效。JBJ-09-063 可用于EGFR 突变型肺癌研究。 | |||
TMIH-0100 | |||
Atomoxetine-d7 HCl (Racemic) 是 Atomoxetine HCl (Racemic) 的氘代化合物。Atomoxetine HCl (Racemic) 的 CAS 号为 82248-59-7。Atomoxetine hydrochloride 是苯氧基-3-丙胺衍生物和选择性非兴奋剂,是去甲肾上腺素再摄取抑制剂,具有认知增强活性。 与人NET,SERT和DAT的放射性配体结合的Ki分别为5,77和1451 nM。 | |||
T35622 | |||
FKGK 18 is an inhibitor of group VIA (GVIA) calcium-independent phospholipase A2 (iPLA2). It inhibits GVIA iPLA2 by 99.9% at 0.091 mole fraction in a mixed micelle activity assay and is selective for GVIA iPLA2 over GIVA cPLA2 and GV sPLA2 where it shows 80.8 and 36.8% inhibition, respectively. FKGK 18 inhibits iPLA2β activity in cytosolic extracts from INS-1 cells overexpressing iPLA2β (IC50 = ~50 nM) as well as iPLA2γ activity in mouse heart membrane fractions (IC50s = ~1-3 μM). It inhibits glucose-induced increases in prostaglandin E2 production and insulin secretion in human pancreatic islets when used at a concentration of 10 μM and inhibits thapsigargin-induced apoptosis in INS-1 cells overexpressing iPLA2β in a concentration-dependent manner. FKGK 18 (20 mg/kg, 3 times per week) reduces blood glucose levels in an intraperitoneal glucose tolerance test, decreases the incidence of diabetes, and increases serum insulin levels in non-obese diabetic (NOD) mice. | |||
T80240 | |||
Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2是一类具有生物活性的肽,作为蛋白酶激活受体1 (PAR-1) 的选择性激动剂,其特异性优于PAR-2。该肽通过HEK293细胞进行的基于细胞的钙信号传导测定确认了其对PAR-1的高特异性,并可用于研究PAR-1在体内的激活。PAR-1除了介导凝血酶的多种细胞作用外,还与PAR-4协作,参与调控凝血酶诱导的被分类为“凝血型”的肝细胞癌。 | |||
T83926 | |||
S-Geranylgeranyl-L-glutathione是孤儿G蛋白偶联受体(GPCR)P2RY8的配体。该化合物在100 nM浓度下,选择性地诱导P2RY8而非鞘氨醇-1-磷酸受体2(S1P2)、GPR55、半胱氨酸白三烯受体1(CysLT1 receptor)以及CysLT2 receptor的内吞作用。在10 nM浓度下,S-Geranylgeranyl-L-glutathione抑制了表达P2RY8的WEHI-231 B细胞淋巴瘤细胞和分离的人扁桃体生发中心B细胞由趋化因子(C-X-C motif)配体12(CXCL12)诱导的迁移。 | |||
T83947 | |||
HDAC4 CHDI Degrader 11是一种高效且选择性的HDAC4降解剂(PROTAC),其在Jurkat E6-1细胞和Jurkat细胞中的DC50值分别为4 nM和6 nM。该化合物由类IIa HDAC抑制剂三氟甲基噁二唑通过连接体与Von Hippel-Lindau (VHL) 蛋白的配体连接而成。在亨廷顿病小鼠细胞模型中,HDAC4 CHDI Degrader 11能强效地降解HDAC4(DC50= 1nM)。在神经母细胞瘤细胞系中,可与P-糖蛋白抑制剂Elacridar联用以实现更有效的降解。 | |||
T61197 | |||
Irdabisant (CEP-26401) hydrochloride 是一种选择性、口服活性的组胺H3受体拮抗剂/逆激动剂,具备良好的血脑屏障渗透性。该化合物对大鼠和人类的H3受体具有高亲和力,其Ki值分别为7.2 nM和2.0 nM。此外,Irdabisant hydrochloride在抑制hERG电流方面表现出较低的活性,IC50为13.8 μM。在大鼠社会认知模型中,它展现了认知增强和唤醒的效果,可作为精神分裂症或认知障碍研究的潜在工具。 | |||
T82528 | |||
DQP-997-74(compound 2i)是一种针对NMDAR的选择性抑制剂,GluN2C/D的IC50分别为0.069 μM和0.035 μM,显示出良好的血脑屏障透过性。DQP为二氢喹啉-吡唑啉。该化合物能够在激动剂谷氨酸的作用下,表现出对高频兴奋性突触传递所驱动的超同步活动具有时间依赖性的增强抑制作用。在TSC诱导的癫痫小鼠模型中,DQP-997-74有效减少了发作次数,适用于NMDAR相关神经系统疾病的研究。 | |||
T38381 | |||
CAY17c is an inhibitor of bromodomain-containing protein 4 (BRD4; IC50= 0.71 μM), as well as class I histone deacetylases (HDACs; IC50s = 0.046, 0.058, 0.075, and 0.167 μM for HDAC1, -2, -3, and -8, respectively) and class IIb HDACs (IC50s = 0.073 and 0.923 μM for HDAC6 and HDAC10, respectively).1It is selective for these enzymes over BRD2, -3, and -T (IC50s = >20 μM for all), as well as over HDAC4, -5, -7, -9, and -11 (IC50s = >10 μM for all). CAY17c inhibits the proliferation of HCT116, SW620, and DLD-1 colorectal cancer cells (IC50s = 0.45, 1.78, and 2.11 μM, respectively), as well as induces apoptosis and autophagy in HCT116 cells. It reduces tumor growth in an HCT116 mouse xenograft model when administered at doses of 15 and 30 mg/kg. 1.Pan, Z., Li, X., Wang, Y., et al.Discovery of thieno[2,3-d]pyrimidine-based hydroxamic acid derivatives as bromodomain-containing protein 4/histone deacetylase dual inhibitors induce autophagic cell death in colorectal carcinoma cellsJ. Med. Chem.63(7)3678-3700(2020) |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPJ-01068 | FKBP25/FKBP3 Protein, Human, Recombinant (His) | Human | E. coli | ||
FKBP25 contains 1 PPIase FKBP-type domain, belongs to the FKBP-type PPIase family. FK506- and rapamycin-binding proteins (FKBPs) constitute a family of receptors for the two immunosuppressants which inhibit T-cell proliferation by arresting two distinct cytoplasmic signal transmission pathways. FKBP3 is a cis-trans prolyl isomerase enzyme that binds the immunosuppressants FK506 and rapamycin, as well as histone deacetylases, the transcription factor YY1, casein kinase II, and nucleolin. It has a higher affinity for rapamycin than for FK506 and thus may be an important target molecule for immunosuppression by rapamycin.
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TMPY-02292 | IGSF11 Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
Immunoglobulin superfamily member 11(IGSF11) is expressed on the plasma membrane in the testis and brain. These IGSF proteins undergo final modifications during capacitation and/or the acrosome reaction. IGSF proteins share significant homology with endothelial cell-selective adhesion molecule and coxsackievirus and adenovirus receptor, which mediates cell attachment and homotypic intercellular interactions. In clinical, the IGSF11 has been reported to overexpressed in colorectal cancers and hepatocellular carcinomas, as well as intestinal-type gastric cancers, compared to their corresponding non-cancerous tissues. The IGSF11 has also been found expressed abundantly in the testis and ovary and the IGSF11 can be used as a candidate of cancer-testis antigen.
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TMPY-01460 | ABHD4 Protein, Human, Recombinant (His) | Human | Baculovirus Insect Cells | ||
Abhydrolase domain containing 4 (ABHD4), also known as alpha/beta-hydrolase 4 (ABH4) , or lyso-N-acylphosphatidylethanolamine lipase, which belongs to the ABHD4/ABHD5 subfamily of peptidase S33 family. Abhydrolase domain containing (ABHD) gene was a small group belongs to alpha/beta hydrolase superfamily. Known members of this group are all found to be involved in important biochemical processes and related to various diseases. The alpha/beta-hydrolase 4 (ABH4) is a lysophospholipase/phospholipase B that selectively hydrolyzes N-acyl phosphatidylethanolamines (NAPEs) and lysoNAPEs. ABH4 accepts lysoNAPEs bearing both saturated and polyunsaturated N-acyl chains as substrates and displays a distribution that closely mirrors lysoNAPE-lipase activity in mouse tissues. The existence of an NAPE-PLD-independent route for NAE biosynthesis and suggest that ABH4 plays a role in this metabolic pathway by acting as a (lyso)NAPE-selective lipase.
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TMPH-03043 | PIA Protein, MenB, Recombinant (His) | MenB | E. coli | ||
Serves as a slightly cation selective porin. Major antigen on the gonococcal cell surface and it may have pathogenic properties in addition to its porin activity.
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TMPH-00108 | UBC11 Protein, Arabidopsis thaliana, Recombinant (His) | Arabidopsis thaliana | E. coli | ||
Accepts the ubiquitin from the E1 complex and catalyzes its covalent attachment to other proteins. Mediates the selective degradation of short-lived and abnormal proteins. UBC11 Protein, Arabidopsis thaliana, Recombinant (His) is expressed in E. coli expression system with N-6xHis tag. The predicted molecular weight is 20.6 kDa and the accession number is P35134.
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TMPH-00107 | UBC10 Protein, Arabidopsis thaliana, Recombinant (His) | Arabidopsis thaliana | E. coli | ||
Accepts the ubiquitin from the E1 complex and catalyzes its covalent attachment to other proteins. Mediates the selective degradation of short-lived and abnormal proteins. UBC10 Protein, Arabidopsis thaliana, Recombinant (His) is expressed in E. coli expression system with N-6xHis tag. The predicted molecular weight is 20.6 kDa and the accession number is P35133.
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TMPH-01693 | MAP3K14 Protein, Human, Recombinant (His & Myc) | Human | E. coli | ||
Lymphotoxin beta-activated kinase which seems to be exclusively involved in the activation of NF-kappa-B and its transcriptional activity. Promotes proteolytic processing of NFKB2/P100, which leads to activation of NF-kappa-B via the non-canonical pathway. Could act in a receptor-selective manner.
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TMPH-00109 | UBC8 Protein, Arabidopsis thaliana, Recombinant (His & Myc) | Arabidopsis thaliana | E. coli | ||
Accepts the ubiquitin from the E1 complex and catalyzes its covalent attachment to other proteins. Mediates the selective degradation of short-lived and abnormal proteins. UBC8 Protein, Arabidopsis thaliana, Recombinant (His & Myc) is expressed in E. coli expression system with N-10xHis and C-Myc tag. The predicted molecular weight is 24.0 kDa and the accession number is P35131.
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TMPY-04904 | Zika virus (ZIKV) (strain Zika SPH2015) M/Membrane protein (Fc) | ZIKV | HEK293 Cells | ||
Zika virus (ZIKV) infection causes microcephaly and has been linked to other brain abnormalities. ZIKV has a more selective and larger impact on the expression of genes involved in DNA replication and repair. P53 inhibitors can block the apoptosis induced by ZIKV-M in hNPCs.
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TMPH-01816 | OX1R Protein, Human, Recombinant (His & SUMOstar) | Human | P. pastoris (Yeast) | ||
Moderately selective excitatory receptor for orexin-A and, with a lower affinity, for orexin-B neuropeptide. Triggers an increase in cytoplasmic Ca(2+) levels in response to orexin-A binding. OX1R Protein, Human, Recombinant (His & SUMOstar) is expressed in yeast with N-6xHis-sumostar tag. The predicted molecular weight is 21.4 kDa and the accession number is O43613.
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TMPH-03174 | LecA Protein, Pseudomonas aeruginosa, Recombinant (His) | Pseudomonas aeruginosa | E. coli | ||
D-galactose specific lectin. Binds in decreasing order of affinity: melibiose, methyl-alpha-D-galactoside, D-galactose, methyl-beta-D-galactoside, N-acetyl-D-galactosamine. Similar to plant lectins in its selective (carbohydrate-specific) hemagglutinating activity. LecA Protein, Pseudomonas aeruginosa, Recombinant (His) is expressed in E. coli expression system with N-6xHis tag. The predicted molecular weight is 16.8 kDa and the accession number is Q05097.
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TMPH-00379 | MLCK Protein, Chicken, Recombinant (His & Myc & SUMO) | Chicken | E. coli | ||
Phosphorylates a specific serine in the N-terminus of a myosin light chain, which leads to the formation of calmodulin/MLCK signal transduction complexes which allow selective transduction of calcium signals. MLCK Protein, Chicken, Recombinant (His & Myc & SUMO) is expressed in E. coli expression system with N-10xHis-SUMO and C-Myc tag. The predicted molecular weight is 52.9 kDa and the accession number is P11799.
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TMPH-02905 | TRPC1 Protein, Mouse, Recombinant (His) | Mouse | E. coli | ||
Thought to form a receptor-activated non-selective calcium permeant cation channel. Probably is operated by a phosphatidylinositol second messenger system activated by receptor tyrosine kinases or G-protein coupled receptors. Seems to be also activated by intracellular calcium store depletion. TRPC1 Protein, Mouse, Recombinant (His) is expressed in E. coli expression system with N-10xHis tag. The predicted molecular weight is 94.0 kDa and the accession number is Q61056.
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TMPJ-00273 | IGSF11 Protein, Human, Recombinant (hFc) | Human | HEK293 Cells | ||
Immunoglobulin superfamily member 11(IGSF11) is abundantly expressed in testis and ovary and to a lower extent in brain, kidney and skeletal muscle.IGSF11 functions as a cell adhesion molecule through homophilic interaction and can also stimulates cell growth.IGSF proteins share significant homology with endothelial cell-selective adhesion molecule and coxsackievirus and adenovirus receptor, which mediates cell attachment and homotypic intercellular interactions.
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TMPH-01684 | MAP1LC3C Protein, Human, Recombinant (His) | Human | E. coli | ||
Ubiquitin-like modifier that plays a crucial role in antibacterial autophagy (xenophagy) through the selective binding of CALCOCO2. Recruits all ATG8 family members to infecting bacteria such as S.Typhimurium. May also play a role in aggrephagy, the macroautophagic degradation of ubiquitinated and aggregated proteins. MAP1LC3C Protein, Human, Recombinant (His) is expressed in E. coli expression system with N-10xHis tag. The predicted molecular weight is 20.7 kDa and the accession number is Q9BXW4.
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TMPK-00564 | TNFR1/CD120a/TNFRSF1A Protein, Cynomolgus, Recombinant (His) | Cynomolgus | HEK293 Cells | ||
Tumour necrosis factor alpha (TNF-α) is a pleiotropic cytokine with both injurious and protective functions, which are thought to diverge at the level of its two cell surface receptors, TNFR1 and TNFR2. In the setting of acute injury, selective inhibition of TNFR1 is predicted to attenuate the cell death and inflammation associated with TNF-α, while sparing or potentiating the protective effects of TNFR2 signalling.
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TMPK-00392 | FGFR1 beta (IIIc) Protein, Human, Recombinant (His & Avi) | Human | HEK293 Cells | ||
Fibroblast growth factor receptor 1 (FGFR1) transmits signals through the plasma membrane regulating essential cellular processes like division, motility, metabolism, and death. Overexpression of FGFR1 is observed in numerous tumors and thus constitutes an attractive molecular target for selective cancer treatment. FGFR1 beta (IIIc) Protein, Human, Recombinant (His & Avi) is expressed in HEK293 mammalian cells with C-His-Avi tag. The predicted molecular weight is 25.23 kDa and the accession number is P11362-7.
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TMPJ-01221 | UBE2J2 Protein, Human, Recombinant (GST) | Human | E. coli | ||
Ubiquitin-Conjugating Enzyme E2 J2 (UBE2J2) belongs to the ubiquitin-conjugating enzyme family. UBE2J2 is involved in the ubiquitiantion. UBE2J2 located in the membrane of the endoplasmic reticulum, catalyzes the covalent attachment of ubiquitin to other proteins. UBE2J2 may play a important role in the selective degradation of misfolded membrane protein from the endoplasmic reticulum.
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TMPK-00394 | FGFR1 beta (IIIc) Protein, Human, Recombinant (His & Avi), Biotinylated | Human | HEK293 Cells | ||
Fibroblast growth factor receptor 1 (FGFR1) transmits signals through the plasma membrane regulating essential cellular processes like division, motility, metabolism, and death. Overexpression of FGFR1 is observed in numerous tumors and thus constitutes an attractive molecular target for selective cancer treatment. FGFR1 beta (IIIc) Protein, Human, Recombinant (His & Avi), Biotinylated is expressed in HEK293 mammalian cells with C-His-Avi tag. The predicted molecular weight is 25.23 kDa and the accession number is P11362-7.
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TMPH-03606 | P3H 1 Protein, Streptomyces sp., Recombinant (His & Myc) | Streptomyces | E. coli | ||
Dioxygenase that catalyzes the 2-oxoglutarate-dependent selective hydroxylation of free L-proline to cis-3-hydroxy-L-proline (cis-3-Hyp). D-proline, trans-4-hydroxy-L-proline, cis-4-hydroxy-L-proline, cis-4-hydroxy-D-proline, and 3,4-dehydro-DL-proline are not substrates. P3H 1 Protein, Streptomyces sp., Recombinant (His & Myc) is expressed in E. coli expression system with N-10xHis and C-Myc tag. The predicted molecular weight is 44.0 kDa and the accession number is P96010.
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TMPH-03390 | TRPV2 Protein, Rat, Recombinant (His) | Rat | E. coli | ||
Calcium-permeable, non-selective cation channel with an outward rectification. Seems to be regulated, at least in part, by growth factors, like IGF1, PDGF and morphogenetic neuropeptide/head activator. May transduce physical stimuli in mast cells. Activated by temperatures higher than 52 degrees Celsius; is not activated by vanilloids and acidic pH. TRPV2 Protein, Rat, Recombinant (His) is expressed in E. coli expression system with N-10xHis tag. The predicted molecular weight is 88.2 kDa and the accession number is Q9WUD2.
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TMPK-00171 | TRAIL Trimer Protein, Human, Recombinant (His & Flag) | Human | HEK293 Cells | ||
Tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) is a member of the TNF superfamily that can initiate the apoptosis pathway by binding to its associated death receptors DR4 and DR5. The activation of the TRAIL pathway in inducing tumor-selective apoptosis leads to the development of TRAIL-based cancer therapies, which include recombinant forms of TRAIL, TRAIL receptor agonists, and other therapeutic agents.
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TMPH-02118 | SCN1A Protein, Human, Recombinant (His) | Human | E. coli | ||
Mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient. Plays a key role in brain, probably by regulating the moment when neurotransmitters are released in neurons. Involved in sensory perception of mechanical pain: activation in somatosensory neurons induces pain without neurogenic inflammation and produces hypersensitivity to mechanical, but not thermal stimuli.
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TMPY-05003 | GLTP Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
Glycolipid transfer proteins (GLTPs) originally were identified as small (~24 kDa), soluble, amphitropic proteins that specifically accelerate the intermembrane transfer of glycolipids. Human GLTP-motifs have evolved to function not only as glucosylceramide binding/transferring domains for phosphoinositol 4-phosphate adaptor protein-2 during glycosphingolipid biosynthesis but also as selective binding/transfer proteins for ceramide-1-phosphate. Glycolipid transfer protein (GLTP) accelerates glycolipid intermembrane transfer via a unique lipid transfer/binding fold (GLTP fold) that defines the GLTP superfamily and is the prototype for functional GLTP-like domains in larger proteins, i.e. FAPP2.
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TMPJ-01363 | CLIC5 Protein, Human, Recombinant (His) | Human | E. coli | ||
Chloride Intracellular Channel Protein 5 (CLIC5) is a single-pass membrane protein which belongs to the chloride channel CLIC family. It contains one GST C-terminal domain. Chloride intracellular channels are involved in chloride ion transport within various subcellular compartments. CLIC5 can insert into membranes and form selective ion channels regulated by actin that may transport chloride ions. It may play a role in the regulation of transepithelial ion absorption and secretion. CLIC5 specifically associates with the cytoskeleton of placenta microvilli. CLIC5 is required for the development and/or maintenance of the proper glomerular endothelial cell and podocyte architecture.
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TMPJ-00891 | Kallikrein 2/KLK2 Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
Kallikrein-2 (KLK2) is a secreted serine protease that belongs to the peptidase S1 family of Kallikrein subfamily. KLK2 contains 1 peptidase S1 domain. It is highly expressed in the human prostate gland. KLK2 can cleave Met-Lys and Arg-Ser bonds in kininogen to release Lys-bradykinin, but Preferential cleavages of Arg-|-Xaa bonds in small molecule substrates. It also highly selective action to release kallidin (lysyl-bradykinin) from kininogen involves hydrolysis of Met-|-Xaa or Leu-|-Xaa. KLK2 is inhibited by serpins such as protein C inhibitor, antichymotrypsin, and plasminogen. KLK2 is considered to be a biomarker for prostate cancer.
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TMPH-02365 | JC polyomavirus (JCV) Minor capsid protein VP2 (His) | JCPyV | E. coli | ||
Isoform VP2 is a structural protein that resides within the core of the capsid surrounded by 72 VP1 pentamers. Participates in host cell receptor binding together with VP1. Following virus endocytosis and trafficking to the endoplasmic reticulum, VP2 and VP3 form oligomers and integrate into the endoplasmic reticulum membrane. Heterooligomer VP2-VP3 may create a viroporin for transporting the viral genome across the endoplasmic reticulum membrane to the cytoplasm. Nuclear entry of the viral DNA involves the selective exposure and importin recognition of VP2 or Vp3 nuclear localization signal (shared C-terminus). Plays a role in virion assembly within the nucleus in particular through a DNA-binding domain located in the C-terminal region. A N-terminal myristoylation suggests a scaffold function for virion assembly.; structural protein that resides within the core of the capsid surrounded by 72 VP1 pentamers. Following virus endocytosis and trafficking to the endoplasmic reticulum, VP2 and VP3 form oligomers and integrate into the endoplasmic reticulum membrane. Heterooligomer VP2-VP3 may create a viroporin for transporting the viral genome across the endoplasmic reticulum membrane to the cytoplasm. Nuclear entry of the viral DNA involves the selective exposure and importin recognition of VP2 or Vp3 nuclear localization signal (shared C-terminus). Isoform VP3 plays a role in virion assembly within the nucleus. May participate in host cell lysis when associated with VP4.; Isoform VP4 is a viroporin inducing perforation of cellular membranes to trigger virus progeny release. Forms pores of 3 nm inner diameter. VP4 is expressed about 24 hours after the late structural proteins and is not incorporated into the mature virion.
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TMPH-02301 | VPS35 Protein, Human, Recombinant (His & Myc) | Human | E. coli | ||
Acts as component of the retromer cargo-selective complex (CSC). The CSC is believed to be the core functional component of retromer or respective retromer complex variants acting to prevent missorting of selected transmembrane cargo proteins into the lysosomal degradation pathway. The recruitment of the CSC to the endosomal membrane involves RAB7A and SNX3. The CSC seems to associate with the cytoplasmic domain of cargo proteins predominantly via VPS35; however, these interactions seem to be of low affinity and retromer SNX proteins may also contribute to cargo selectivity thus questioning the classical function of the CSC. The SNX-BAR retromer mediates retrograde transport of cargo proteins from endosomes to the trans-Golgi network (TGN) and is involved in endosome-to-plasma membrane transport for cargo protein recycling. The SNX3-retromer mediates the retrograde endosome-to-TGN transport of WLS distinct from the SNX-BAR retromer pathway. The SNX27-retromer is believed to be involved in endosome-to-plasma membrane trafficking and recycling of a broad spectrum of cargo proteins. The CSC seems to act as recruitment hub for other proteins, such as the WASH complex and TBC1D5. Required for retrograde transport of lysosomal enzyme receptor IGF2R and SLC11A2. Required to regulate transcytosis of the polymeric immunoglobulin receptor (pIgR-pIgA). Required for endosomal localization of WASHC2C. Mediates the association of the CSC with the WASH complex via WASHC2. Required for the endosomal localization of TBC1D5.; (Microbial infection) The heterotrimeric retromer cargo-selective complex (CSC) mediates the exit of human papillomavirus from the early endosome and the delivery to the Golgi apparatus.
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TMPH-02347 | Influenza A H1N1 (strain A/USA:Phila/1935) Matrix protein 2 (His) | H1N1 | E. coli | ||
Forms a proton-selective ion channel that is necessary for the efficient release of the viral genome during virus entry. After attaching to the cell surface, the virion enters the cell by endocytosis. Acidification of the endosome triggers M2 ion channel activity. The influx of protons into virion interior is believed to disrupt interactions between the viral ribonucleoprotein (RNP), matrix protein 1 (M1), and lipid bilayers, thereby freeing the viral genome from interaction with viral proteins and enabling RNA segments to migrate to the host cell nucleus, where influenza virus RNA transcription and replication occur. Also plays a role in viral proteins secretory pathway. Elevates the intravesicular pH of normally acidic compartments, such as trans-Golgi network, preventing newly formed hemagglutinin from premature switching to the fusion-active conformation.
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TMPH-02348 | Influenza A H1N1 (strain A/Puerto Rico/8/1934) Matrix protein 2 (His & Myc) | H1N1 | E. coli | ||
Forms a proton-selective ion channel that is necessary for the efficient release of the viral genome during virus entry. After attaching to the cell surface, the virion enters the cell by endocytosis. Acidification of the endosome triggers M2 ion channel activity. The influx of protons into virion interior is believed to disrupt interactions between the viral ribonucleoprotein (RNP), matrix protein 1 (M1), and lipid bilayers, thereby freeing the viral genome from interaction with viral proteins and enabling RNA segments to migrate to the host cell nucleus, where influenza virus RNA transcription and replication occur. Also plays a role in viral proteins secretory pathway. Elevates the intravesicular pH of normally acidic compartments, such as trans-Golgi network, preventing newly formed hemagglutinin from premature switching to the fusion-active conformation.
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TMPH-00789 | Hamster polyomavirus (HaPyV) VP1 Protein (His & Myc) | HaPyV | E. coli | ||
Forms an icosahedral capsid with a T=7 symmetry and a 40 nm diameter. The capsid is composed of 72 pentamers linked to each other by disulfide bonds and associated with VP2 or VP3 proteins. Interacts with sialic acids on the cell surface to provide virion attachment to target cell. Once attached, the virion is internalized by endocytosis and traffics to the endoplasmic reticulum. Inside the endoplasmic reticulum, the protein folding machinery isomerizes VP1 interpentamer disulfide bonds, thereby triggering initial uncoating. Next, the virion uses the endoplasmic reticulum-associated degradation machinery to probably translocate in the cytosol before reaching the nucleus. Nuclear entry of the viral DNA involves the selective exposure and importin recognition of VP2/Vp3 nuclear localization signal. In late phase of infection, neo-synthesized VP1 encapsulates replicated genomic DNA in the nucleus, and participates in rearranging nucleosomes around the viral DNA.
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TMPH-00201 | BK polyomavirus (BKPyV) VP2 Protein (His) | BKPyV | E. coli | ||
Isoform VP2 is a structural protein that resides within the core of the capsid surrounded by 72 VP1 pentamers. Participates in host cell receptor binding together with VP1. Following virus endocytosis and trafficking to the endoplasmic reticulum, VP2 and VP3 form oligomers and integrate into the endoplasmic reticulum membrane. Heterooligomer VP2-VP3 may create a viroporin for transporting the viral genome across the endoplasmic reticulum membrane to the cytoplasm. Nuclear entry of the viral DNA involves the selective exposure and importin recognition of VP2 or Vp3 nuclear localization signal (shared C-terminus). Plays a role in virion assembly within the nucleus in particular through a DNA-binding domain located in the C-terminal region. A N-terminal myristoylation suggests a scaffold function for virion assembly.; structural protein that resides within the core of the capsid surrounded by 72 VP1 pentamers. Following virus endocytosis and trafficking to the endoplasmic reticulum, VP2 and VP3 form oligomers and integrate into the endoplasmic reticulum membrane. Heterooligomer VP2-VP3 may create a viroporin for transporting the viral genome across the endoplasmic reticulum membrane to the cytoplasm. Nuclear entry of the viral DNA involves the selective exposure and importin recognition of VP2 or Vp3 nuclear localization signal (shared C-terminus). Isoform VP3 plays a role in virion assembly within the nucleus. May participate in host cell lysis when associated with VP4.; Isoform VP4 is a viroporin inducing perforation of cellular membranes to trigger virus progeny release. Forms pores of 3 nm inner diameter. VP4 is expressed about 24 hours after the late structural proteins and is not incorporated into the mature virion.
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TMPH-02803 | NRROS Protein, Mouse, Recombinant (His) | Mouse | E. coli | ||
Key regulator of transforming growth factor beta-1 (TGFB1) specifically required for microglia function in the nervous system. Required for activation of latent TGF-beta-1 in macrophages and microglia: associates specifically via disulfide bonds with the Latency-associated peptide (LAP), which is the regulatory chain of TGFB1, and regulates integrin-dependent activation of TGF-beta-1. TGF-beta-1 activation mediated by LRRC33/NRROS is highly localized: there is little spreading of TGF-beta-1 activated from one microglial cell to neighboring microglia, suggesting the existence of localized and selective activation of TGF-beta-1 by LRRC33/NRROS. Indirectly plays a role in Toll-like receptor (TLR) signaling: ability to inhibit TLR-mediated NF-kappa-B activation and cytokine production is probably a consequence of its role in TGF-beta-1 signaling (Probable).
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TMPY-01812 | Enoyl-ACP Reductase Protein, E. coli, Recombinant (His) | E. coli | E. coli | ||
Enoyl-ACP reductase, also known as NADH-dependent enoyl-ACP reductase and FABI, is a cell inner membrane and peripheral membrane protein which belongs to theshort-chain dehydrogenases/reductases (SDR) family and FabI subfamily. Microorganisms produce many kinds of antibiotics which function in an antagonistic capacity in nature where they have much competition. Bacterial FAS provides essential fatty acids for use in the assembly of key cellular components. Among them, FABI is an enoyl-ACP reductase which catalyzes the final and rate-limiting step of bacterial FAS. The antibiotic diazaborine interferes with the activity by binding to the protein. FABI is a potential target for selective antibacterial action, because it shows low overall sequence homology with mammalian enzymes. Various compounds have been reported as inhibitors of bacterial FabI-inhibitory compounds.
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TMPY-02842 | UBE2L6 Protein, Human, Recombinant (His) | Human | E. coli | ||
UBCH8, also known as UBE2L6, belongs to the ubiquitin-conjugating enzyme family. The family of ubiquitin-conjugating (E2) enzymes is characterized by the presence of a highly conserved ubiquitin-conjugating (UBC) domain. These domains accommodate the ATP-activated ubiquitin (Ub) or ubiquitin-like (UBL) protein via a covalently linked thioester onto its active-site residue. E2 enzymes act via selective protein-protein interactions with the E1 and E3 enzymes and connect activation to covalent modification. By doing so, E2s differentiate effects on downstream substrates, either with a single Ub/UBL molecule or as a chain. UBCH8 is highly similar in primary structure to the enzyme encoded by the UBE2L3 gene. It catalyzes the covalent attachment of ubiquitin or ISG15 to other proteins. UBCH8 functions in the E6/E6-AP-induced ubiquitination of p53/TP53 and promotes ubiquitination and subsequent proteasomal degradation of FLT3. At protein level, it is present in natural killer cells.
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TMPH-01517 | FCGRT Protein, Human, Recombinant (GST) | Human | E. coli | ||
Cell surface receptor that transfers passive humoral immunity from the mother to the newborn. Binds to the Fc region of monomeric immunoglobulin gamma and mediates its selective uptake from milk. IgG in the milk is bound at the apical surface of the intestinal epithelium. The resultant FcRn-IgG complexes are transcytosed across the intestinal epithelium and IgG is released from FcRn into blood or tissue fluids. Throughout life, contributes to effective humoral immunity by recycling IgG and extending its half-life in the circulation. Mechanistically, monomeric IgG binding to FcRn in acidic endosomes of endothelial and hematopoietic cells recycles IgG to the cell surface where it is released into the circulation. In addition of IgG, regulates homeostasis of the other most abundant circulating protein albumin/ALB.; (Microbial infection) Acts as an uncoating receptor for a panel of echoviruses including Echovirus 5, 6, 7, 9, 11, 13, 25 and 29.
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TMPH-01516 | FCGRT Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
Cell surface receptor that transfers passive humoral immunity from the mother to the newborn. Binds to the Fc region of monomeric immunoglobulin gamma and mediates its selective uptake from milk. IgG in the milk is bound at the apical surface of the intestinal epithelium. The resultant FcRn-IgG complexes are transcytosed across the intestinal epithelium and IgG is released from FcRn into blood or tissue fluids. Throughout life, contributes to effective humoral immunity by recycling IgG and extending its half-life in the circulation. Mechanistically, monomeric IgG binding to FcRn in acidic endosomes of endothelial and hematopoietic cells recycles IgG to the cell surface where it is released into the circulation. In addition of IgG, regulates homeostasis of the other most abundant circulating protein albumin/ALB.; (Microbial infection) Acts as an uncoating receptor for a panel of echoviruses including Echovirus 5, 6, 7, 9, 11, 13, 25 and 29.
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TMPJ-00782 | Amyloid Precursor Protein, Human, Recombinant (hFc) | Human | HEK293 Cells | ||
Amyloid precursor protein (APP) is a type I membrane protein with several isoforms due to alternative splicing, performs physiological functions on the surface of neurons relevant to neurite growth, neuronal adhesion and axonogenesis. Of the three major splice isoforms of APP (APP695, APP751, and APP770) APP695 is the predominant neuronal form from which Amyloid beta peptide and transcriptionally-active cleaved intracellular domain of APP (AICD) are preferentially generated by selective processing through the amyloidogenic pathway. Human APP695 consists of a 17 amino acid (aa) signal sequence, a 607 aa extracellular domain (ECD), a 24 aa transmembrane domain, and a 47 aa cytoplasmic domain. Within the ECD, human APP695 shares 97% aa sequence identity with mouse and rat APP695. Amyloid beta is a major molecule implicated in pathogenesis of Alzheimer's disease (AD) and related dementias. AICD regulates expression by direct promoter binding of multiple genes, including APP itself, the beta-secretase, BACE-1 and the Amyloid beta-degrading enzyme, Neprilysin. As such, APP695 plays an important role in brain development, learning and memory, synaptic plasticity, and neurodegeneration including AD.
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TMPY-04554 | JNK1 Protein, Human, Recombinant (GST) | Human | Baculovirus Insect Cells | ||
Mitogen-activated protein kinase 8 (MAPK8), also known as JNK1, is a member of the MAP kinase family. MAP kinases act as an integration point for multiple biochemical signals and are involved in a wide variety of cellular processes such as proliferation, differentiation, transcription regulation, and development. The protein kinases JNK1 has been found to serve as critical molecular links between obesity, metabolic inflammation, and disorders of glucose homeostasis. It is critically involved in the promotion of diet-induced obesity, metabolic inflammation, and beta-cell dysfunction. The selective deficiency of JNK1 in the murine nervous system is sufficient to suppress diet-induced obesity. Genetic analysis indicates that the effects of JNK1 can be separated from the effects of JNK1 on obesity. JNK1 is a potential pharmacological target for the development of drugs that might be useful for the treatment of metabolic syndrome, and type 2 diabetes. Furthermore, JNK1 plays a major role in hypoxic cellular damage. JNK1 protein might be an attractive target for anti-hypoxic therapy in increasing resistance to many pathological conditions and diseases, leading to the oxygen deficit.
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TMPY-04402 | CSNK1G1 Protein, Human, Recombinant (His & GST) | Human | Baculovirus Insect Cells | ||
Casein kinase I isoform gamma-1, also known as CSNK1G1, is a member of the protein kinase superfamily, CK1 Ser/Thr protein kinase family and casein kinase I subfamily. Thecasein kinase I family of protein kinases are serine / threonine-selective enzymes that function as regulators ofsignal transductionpathways in most eukaryotic cell types. Casein has been used as a substrate since the earliest days of research on protein phosphorylation. Casein kinase activity associated with the endoplasmic reticulum of mammary glands was first characterized in 1974 and its activity was shown to not depend on cyclic AMP. The CKI family of monomeric serine–threonine protein kinases is found in eukaryotic organisms from yeast to human. Mammals have seven family members: alpha, beta 1, gamma 1, gamma 2, gamma 3, delta, and epsilon. The family members have the highest homology in their kinase domains (53%–98% identical) and differ from most other protein kinases by the presence of the sequence S-I-N instead of A-P-E in kinase domain VIII. The CKI family members appear to have similar substrate specificity and substrate selection is thought to be regulated via subcellular localization and docking sites in specific substrates.
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TMPY-00564 | MCP-4 Protein, Human, Recombinant (His) | Human | P. pastoris (Yeast) | ||
Monocyte Chemoattractant Proteins 4 (MCP-4/CCL13) is a member of a distinct, structurally-related subclass of CC chemokines mainly involved in recruitment of eosinphils to inflammatory sites. CCL13/MCP-4, is a CC family chemokine that is chemoattractant for eosinophils, basophils, monocytes, macrophages, immature dendritic cells, and T cells, and its capable of inducing crucial immuno-modulatory responses through its effects on epithelial, muscular and endothelial cells. Similar to other CC chemokines, CCL13 binds to several chemokine receptors (CCR1, CCR2 and CCR3), allowing it to elicit different effects on its target cells. A number of studies have shown that CCL13 is involved in many chronic inflammatory diseases, in which it functions as a pivotal molecule involved in the selective recruitment of cell lineages to the inflamed tissues and their subsequent activation. MCP-4/CCL13 is secreted from chondrocytes and activates the proliferation of rheumatoid synovial cells, thereby leading to joint destruction in RA. The interferon-gamma in combination with interleukin-1beta/tumor necrosis factor-alpha activates the production of MCP-4/CCL13 from chondrocytes in RA joints, and that secreted MCP-4/CCL13 enhances fibroblast-like synoviocyte proliferation by activating the extracellular signal-regulated kinase mitogen-activated protein kinase cascade. CCL13 may have some role in the pathogenesis of systemic sclerosis (SSc).
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TMPY-01187 | Rac1 Protein, Human, Recombinant (GST) | Human | Baculovirus Insect Cells | ||
RAC1 is a GTPase that belongs to the RAS superfamily of small GTP-binding proteins. Members of this superfamily appear to regulate a diverse array of cellular events, including the control of cell growth, cytoskeletal reorganization, and the activation of protein kinases. Two transcript variants encoding different isoforms have been found for RAC1 gene. RAC1 is a plasma membrane-associated small GTPase which cycles between active GTP-bound and inactive GDP-bound states. In its active state, binds to a variety of effector proteins to regulate cellular responses such as secretory processes, phagocytosis of apoptotic cells, epithelial cell polarization and growth-factor induced formation of membrane ruffles. RAC1 p21/rho GDI heterodimer is the active component of the cytosolic factor sigma 1, which is involved in stimulation of the NADPH oxidase activity in macrophage. RAC1 is essential for the SPATA13-mediated regulation of cell migration and adhesion assembly and disassembly. RAC1's isoform B has an accelerated GEF-independent GDP/GTP exchange and an impaired GTP hydrolysis, which is restored partially by GTPase-activating proteins. It is able to bind to the GTPase-binding domain of PAK but not full-length PAK in a GTP-dependent manner, suggesting that the insertion does not completely abolish effector interaction. Stat3 is an important transcription factor that regulates both proinflammatory and anti-apoptotic pathways in the heart. It forms a multiprotein complex with RAC1 and PKC in an H/R-dependent manner by expression of constitutively active Rac1 mutant protein, and by RNA silencing of RAC1. Selective inhibition of PKC with calphostin C produces a marked suppression of Stat3 S727 phosphorylation. The association of Stat3 with Rax1 occurs predominantly at the cell membrane, but also inside the nucleus, and occurs through the binding of the coiled-coil domain of Stat3 to the 54 NH(2)-terminal residues of RAC1. Transfection with a peptide comprising the NH(2)-terminal 17 amino acid residues of RAC1-dependent signaling pathways resulting in a physical association between Rac1 and Stat3 and the formation of a novel multiprotein complex with PKC.
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TMPH-00616 | DNA-binding protein H-NS Protein, E. coli, Recombinant (His) | E. coli | E. coli | ||
A DNA-binding protein implicated in transcriptional repression (silencing). Also involved in bacterial chromosome organization and compaction. H-NS binds tightly to AT-rich dsDNA and inhibits transcription. Binds upstream and downstream of initiating RNA polymerase, trapping it in a loop and preventing transcription. Binds to hundreds of sites, approximately half its binding sites are in non-coding DNA, which only accounts for about 10% of the genome. Many of these loci were horizontally transferred (HTG); this offers the selective advantage of silencing foreign DNA while keeping it in the genome in case of need. Suppresses transcription at many intragenic sites as well as transcription of spurious, non-coding RNAs genome-wide. Repression of HTG by H-NS is thought to allow their DNA to evolve faster than non-H-NS-bound regions, and facilitates integration of HTG into transcriptional regulatory networks. A subset of H-NS/StpA-regulated genes also require Hha (and/or Cnu, ydgT) for repression; Hha and Cnu increase the number of genes DNA bound by H-NS/StpA and may also modulate the oligomerization of the H-NS/StpA-complex. The protein forms 2 clusters in the nucleoid which gather hns-bound loci together, bridging non-contiguous DNA, and causes DNA substantial condensation. Binds DNA better at low temperatures than at 37 degrees Celsius; AT-rich sites nucleate H-NS binding, further DNA-binding is cooperative and this cooperativity decreases with rising temperature. Transcriptional repression can be inhibited by dominant-negative mutants of StpA or itself. May effect transcriptional elongation. Can increase translational efficiency of mRNA with suboptimal Shine-Dalgarno sequences. Plays a role in the thermal control of pili and adhesive curli fimbriae production, by inducing transcription of csgD. Plays a role in flagellar function. Represses the CRISPR-cas promoters, permits only weak transcription of the crRNA precursor; its repression is antagonized by LeuO. Binds preferentially to the upstream region of its own gene recognizing two segments of DNA on both sides of a bend centered around -150. Overexpression suppresses secY24, a temperature-sensitive mutation. Has also been reported to activate transcription of some genes.
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