目录号 | 产品详情 | 靶点 | |
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T72244 | |||
CBB1007三盐酸盐是 LSD1选择性抑制剂,IC50值为5.27uM。 | |||
T21668 | |||
Finasteride (MK-906) acetate 是一种高效的5α-还原酶 (5α-reductase) 竞争性抑制剂,其对 II 型 5α-还原酶的IC50值仅为 4.2 nM,其对该型酶的亲和力是对 I 型酶亲和力的约100倍。因此,Finasteride acetate 主要在良性前列腺增生症 (BPH) 和雄激素性脱发研究领域中应用。 | |||
T21848 | |||
A-841720 是一种有效的、非竞争性的、选择性的 mGlu1受体拮抗剂,对人 mGlu1 受体的 IC50为 10 nM。A-841720 的选择性是 mGlu5 的 34 倍 (IC50为 342 nM),并且对一系列其他神经递质受体、离子通道和转运蛋白没有显着活性。A-841720 具有镇痛的治疗潜力。 | |||
T35817 | |||
Photoswitchable PAD inhibitor is a photoactivated protein arginine deiminase (PAD) inhibitor and a derivative of BB-Cl-amidine that contains an azobenzene photoswitch allowing optical control of PAD activity.1 Without photoactivation, it is a weak inhibitor of PAD2 (IC50 = >100 μM) and is less potent than BB-Cl-amidine in inhibiting citrulline production in vitro (kinact/KIs = 2,300, 600, 1,000, and 10,510 M-1min-1 for PAD1-4, respectively) and does not inhibit histone H3 citrullination in HEK293T cells overexpressing PAD2 when used at concentrations up to 100 μM. However, it can rapidly be photoactivated with UV-A radiation to the more active cis-isomer, which is an irreversible, competitive inhibitor of histone H3 citrullination with an IC50 value of 9.1 μM.References1. Mondal, S., Parelkar, S.S., Nagar, M., et al. Photochemical control of protein arginine deiminase (PAD) activity. ACS Chem. Biol. 13(4), 1057-1065 (2018). Photoswitchable PAD inhibitor is a photoactivated protein arginine deiminase (PAD) inhibitor and a derivative of BB-Cl-amidine that contains an azobenzene photoswitch allowing optical control of PAD activity.1 Without photoactivation, it is a weak inhibitor of PAD2 (IC50 = >100 μM) and is less potent than BB-Cl-amidine in inhibiting citrulline production in vitro (kinact/KIs = 2,300, 600, 1,000, and 10,510 M-1min-1 for PAD1-4, respectively) and does not inhibit histone H3 citrullination in HEK293T cells overexpressing PAD2 when used at concentrations up to 100 μM. However, it can rapidly be photoactivated with UV-A radiation to the more active cis-isomer, which is an irreversible, competitive inhibitor of histone H3 citrullination with an IC50 value of 9.1 μM. References1. Mondal, S., Parelkar, S.S., Nagar, M., et al. Photochemical control of protein arginine deiminase (PAD) activity. ACS Chem. Biol. 13(4), 1057-1065 (2018). | |||
T35928 | |||
NVS-PAK1-C 是一种有效的、ATP 竞争的特异性变构 PAK1抑制剂探针。NVS-PAK1-C 可抑制去磷酸化的 PAK1(IC50= 5 nM) 和磷酸化的 PAK1(IC50= 6 nM)。NVS-PAK1-C 也可以抑制去磷酸化的 PAK2 (IC50=270 nM) 和磷酸化的 PAK2 (IC50=720 nM)。 | |||
T73230 | |||
UT-B-IN-1 (UTBINH-14),一种对UT-B(尿素转运蛋白B)显示出可逆、竞争性及选择性抑制作用的化合物,其对人和小鼠的UT-B的IC50值分别为10和25 nM。相较于UT-A亚型,此化合物具有低毒性和更高的选择性。在小鼠模型中,UT-B-IN-1能增加排尿量并降低尿液渗透性,适用于探究利尿机制的研究。 | |||
T22631 | Others | ||
Dolastatin 10 trifluoroacetate is a potent antimitotic polypeptide isolated from a marine animal and is developed as a potential antitumor agent. Dolastatin 10 is found to have an activity to inhibit tubulin polymerization (IC50: 1.2 μM). Besides that, it | |||
T72696 | |||
UCK2 Inhibitor-3是一款UCK2 (尿苷胞苷激酶2)的非竞争性抑制剂,其IC50值为16.6 μM。该化合物能在一定程度上补偿因感染或快速分裂的细胞中DHODH (二氢旋酸脱氢酶)功能的缺失,有效地挽救尿苷。此外,UCK2 Inhibitor-3还能抑制DNA聚合酶η和κ,其IC50值分别为56 μM和16 μM。 | |||
T4752 | Endogenous Metabolite NMDAR | ||
1-Aminocyclopropane-1-carboxylic acid (ACC) 是内源性代谢产物的一种。 | |||
T70538 | |||
PD-85639 is a voltage-gated sodium (Na+) channel blocker (75% in 10 min & >95% in 25 min blockage of Na+ current by 25 μM PD85,639; whole-cell patch clamp using primary rat brain neurons) that is shown to target rat brain Nav1.2 with simultaneous high- and low-affinity modes of binding (EC50 = 56 nM/40% & 20 μM/60% at pH 9.0, 5 nM/28% & 3 μM/72% at pH 7.4, against 2 nM [3H]-PD85,639 for binding rat brain synaptosomes; EC50 = 17 nM/39% & 10 μM/61% using at pH 9.0 using rat brain synaptosome membranes) and a fast kinetic (t1/2 = 1.2 at 4°C, <0.5 min at 25°C), competitive against the local anesthetic Na+ channel blockers tetracaine, bupivacaine, and mepivacaine, as well as Na+ channel activators veratridine and batrachotoxin (K1 = 0.26 μM against 5 nM [3H]-BTX for binding rat neocrotical membranes). |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPJ-00473 | QPRTase Protein, Human, Recombinant (His) | Human | E. coli | ||
Nicotinate-Nucleotide Pyrophosphorylase (QPRT) belongs to the nadC/modD family. QPRT plays an improtant role in catabolism of quinolinate which acts as a potent endogenous exitotoxin to neurons. In addition, QPRT serves as an an intermediate in the Tryptophan-Nicotinamide Adenine Dinucleotide pathway. QPRT participates in some pathways including Cofactor biosynthesis, NAD(+) biosynthesis and the Nicotinate D-Ribonucleotide from Quinolinate. In addition, QPRT is involved in the catabolism of Quinolinic Acid (QA). The activity toward QA is slightly repressed by phosphoribosylpyrophosphate (PRPP) in both a competitive and a non-competitive manner.
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TMPH-00893 | AHCY Protein, Human, Recombinant (His & SUMO) | Human | E. coli | ||
Adenosylhomocysteine is a competitive inhibitor of S-adenosyl-L-methionine-dependent methyl transferase reactions; therefore adenosylhomocysteinase may play a key role in the control of methylations via regulation of the intracellular concentration of adenosylhomocysteine. AHCY Protein, Human, Recombinant (His & SUMO) is expressed in E. coli expression system with N-6xHis-SUMO tag. The predicted molecular weight is 63.6 kDa and the accession number is P23526.
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TMPK-00839 | ITGB6 Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
ITGB6 is known to be one of the major receptor components involved in host tropism of foot-and-mouth disease (FMD) virus in cattle. A competitive PCR technique called ARMS PCR was adapted to identify a single-nucleotide polymorphism (SNP), G29A, db SNP Id: rs109075046, in the 5' untranslated region (5'UTR) of the bovine ITGB6 gene. ITGB6 Protein, Human, Recombinant (His) is expressed in HEK293 mammalian cells with C-His tag. The predicted molecular weight is 75.4 kDa and the accession number is P18564-1.
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TMPK-01247 | ITGB6 Protein, Mouse, Recombinant (His) | Mouse | HEK293 Cells | ||
ITGB6 is known to be one of the major receptor components involved in host tropism of foot-and-mouth disease (FMD) virus in cattle. A competitive PCR technique called ARMS PCR was adapted to identify a single-nucleotide polymorphism (SNP), G29A, db SNP Id: rs109075046, in the 5' untranslated region (5'UTR) of the bovine ITGB6 gene. ITGB6 Protein, Mouse, Recombinant (His) is expressed in HEK293 mammalian cells with C-His tag. The predicted molecular weight is 75.7 kDa and the accession number is Q9Z0T9.
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TMPH-00227 | Beta-casein Protein, Bovine, Recombinant (His & Myc) | Bovine | E. coli | ||
Important role in determination of the surface properties of the casein micelles.; Casoparan acts as a macrophage activator, increasing the phagocytic activity of macrophages and peroxide release from macrophages. It also acts as a bradykinin-potentiating peptide.; Casohypotensin acts as a bradykinin-potentiating peptide. Induces hypotension in rats. Acts as a strong competitive inhibitor of endo-oligopeptidase A.; Antioxidant peptide has antioxidant activity. Beta-casein Protein, Bovine, Recombinant (His & Myc) is expressed in E. coli expression system with N-10xHis and C-Myc tag. The predicted molecular weight is 28.6 kDa and the accession number is P02666.
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TMPH-02941 | MAFK Protein, Mouse, Recombinant (His & Myc & SUMO) | Mouse | E. coli | ||
Since they lack a putative transactivation domain, the small Mafs behave as transcriptional repressors when they dimerize among themselves. However, they act as transcriptional activators by dimerizing with other (usually larger) basic-zipper proteins, such as NFE2, NFE2L1/NRF1, NFE2L2/NRF2 and NFE2L3/NRF3, and recruiting them to specific DNA-binding sites. Small Maf proteins heterodimerize with Fos and may act as competitive repressors of the NF-E2 transcription factor. MAFK Protein, Mouse, Recombinant (His & Myc & SUMO) is expressed in E. coli expression system with N-10xHis-SUMO and C-Myc tag. The predicted molecular weight is 37.5 kDa and the accession number is Q61827.
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TMPH-02940 | MAFK Protein, Mouse, Recombinant (His & Myc) | Mouse | HEK293 Cells | ||
Since they lack a putative transactivation domain, the small Mafs behave as transcriptional repressors when they dimerize among themselves. However, they act as transcriptional activators by dimerizing with other (usually larger) basic-zipper proteins, such as NFE2, NFE2L1/NRF1, NFE2L2/NRF2 and NFE2L3/NRF3, and recruiting them to specific DNA-binding sites. Small Maf proteins heterodimerize with Fos and may act as competitive repressors of the NF-E2 transcription factor. MAFK Protein, Mouse, Recombinant (His & Myc) is expressed in HEK293 mammalian cells with N-10xHis and C-Myc tag. The predicted molecular weight is 21.5 kDa and the accession number is Q61827.
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TMPJ-01309 | PKI-Beta Protein, Human, Recombinant (His) | Human | E. coli | ||
cAMP-Dependent Protein Kinase Inhibitor β (PKI-β) is a member of the PKI family. As a member of the cAMP-dependent protein kinase inhibitor family,It has been shown that PKI-β is an extremely potent competitive inhibitor of cAMP-dependent protein kinase activity; this protein interacts with the catalytic subunit of the enzyme after the cAMP-induced dissociation of its regulatory chains. It may play a role in the protein kinase A (PKA) pathway by interacting with the catalytic subunit of PKA, and overexpression of this gene may play a role in prostate cancer.
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TMPY-01769 | 4EBP1 Protein, Human, Recombinant (His) | Human | E. coli | ||
The translational suppressor eIF4E binding protein-1, 4E-BP1 functions as a key regulator in cellular growth, differentiation, apoptosis and survival. The Eif4ebp1 gene, encoding 4E-BP1, is a direct target of a transcription factor activating transcription factor-4 (ATF4), a master regulator of gene expression in stress responses. 4E-BP1 is characterized by its capacity to bind specifically to eIF4E and inhibit its interaction with eIF4G. Phosphorylation of 4E-BP1 regulates eIF4E availability, and therefore, cap-dependent translation, in cell stress. Binding of eIF4E to eIF4G is inhibited in a competitive manner by 4E-BP1. Phosphorylation of 4E-BP1 decreases the affinity of this protein for eIF4E, thus favouring the binding of eIF4G and enhancing translation. 4E-BP1 is important for beta-cell survival under endoplasmic reticulum (ER) stress. 4E-BP1 mediates the regulation of protein translation by hormones, growth factors and other stimuli that signal through the MAP kinase and mTORC1 pathways. Recently, 4E-BP1 was found to be a key factor, which converges several oncogenic signals, phosphorylates the molecules, and drives the downstream proliferative signals. Recent studies showed that high expression of phosphorylated 4E-BP-1 (p-4E-BP1) is associated with poor prognosis, tumor progression, or nodal metastasis in different human cancers.
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