目录号 | 产品详情 | 靶点 | |
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T73301 | |||
ATR-IN-20是一种高效的ATR(ATM/ATR)抑制剂, IC50值仅为3 nM。该化合物还能抑制mTOR(IC50值为18 nM),并展示出对PI3Kα(100 nM)、ATM(100 nM)和DNA-PK(662 nM)的良好选择性。ATR-IN-20具备优秀的药代动力学属性(F=30%),同时显示了其抗癌潜力。 | |||
TN4437 | MMP IL Receptor NF-κB DNA/RNA Synthesis | ||
Licorisoflavan A shows weak scavenging activity against superoxide anion radical, it and licoricidin have potential for the development of novel host-modulating strategies for the treatment of cytokine and/or MMP-mediated disorders such as periodontitis.L | |||
T72836 | |||
SHP2/CDK4-IN-1(化合物10)是一种针对SHP2和CDK4的口服双重抑制剂,具有IC50值分别为4.3和18.2 nM。该化合物能有效引起G0/G1期阻滞,抑制TNBC细胞的增殖,并在EMT6同源小鼠模型中展现出明显的抗肿瘤活性,适用于三阴性乳腺癌(TNBC)的研究。 | |||
T72465 | |||
Umbralisib (TGR-1202) tosylate是一种口服有效、具有选择性的PI3Kδ和酪蛋白激酶-1-ε (CK1ε) 双重抑制剂,EC50值分别为22.2 nM和6.0 μM。该化合物针对慢性淋巴细胞白血病 (CLL) 中的T细胞显示出独特的免疫调节作用,适用于血液系统恶性肿瘤的研究。 | |||
T61746 | |||
Anticancer agent 82 是 FiVe1 衍生物,是一种口服有效的选择性抗癌剂。FiVe1 能够结合 III 型中间丝蛋白vimentin(VIM),诱导 Ser56 过度磷酸化,导致有丝分裂的选择性中断和转化表达 VIM 的间充质癌细胞的多核化。Anticancer agent 82 比 FiVe1 表现出更好的口服利用度和药代动力学特征。 | |||
T22242 | |||
Amodiaquine dihydrochloride (Amodiaquin dihydrochloride) 是一种4-氨基喹啉类抗疟剂,是一种有效的口服活性的组胺 N-甲基转移酶 (histamine N-methyltransferase) 抑制剂,Ki 值为 18.6 nM。Amodiaquine dihydrochloride 也是一种Nurr1激动剂,可特异性结合Nurr1的配体结合域,EC50约为20 μM,具有抗炎作用。 | |||
T36759 | |||
Potent P2Y12 antagonist (IC50 = 17 nM). Displays antiplatelet and antithrombotic activity in vivo. Orally available. Boldron et al (2014) N-[6-(4-butanoyl-5-methyl-1H-pyrazol-1-yl)pyridazin-3-yl]-5-chloro-1-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]-1H-indole-3-carboxamide (SAR216471), a novel intravenous and oral, reversible, and directly acting P2Y12 antagonist. J.Med.Chem. 57 7293 PMID:25075638 | |||
T81661 | |||
NNMT-IN-4(compound 38),一种选择性、非竞争性且具有膜通透性的烟酰胺N-甲基转移酶(NNMT)抑制剂,在体外生化及细胞实验中的IC50值为42 nM和38 nM。该抑制剂展现出良好的PK/PD关系和安全性,同时具备优秀的口服生物利用度和药物制剂性质,适合作为NNMT活性研究的体内化学探针。 | |||
T35634 | |||
Platensimycin (PTM) is an antibiotic produced by S. platensis that inhibits Gram-positve bacteria by selectively inhibiting cellular lipid biosynthesis (IC50 = 0.1 μM). It targets the β-ketoacyl-acyl-carrier-protein synthase I/II, FabF/B, an enzyme that participates in the biosynthesis of fatty acids (IC50s = 48 and 160 nM for S. aureus and E. coli enzymes, respectively). By specifically targeting fatty acid synthesis in bacteria, PTM is thought to be a promising agent for overcoming antibiotic resistance. PTM is also a selective inhibitor of the mammalian fatty acid synthase and has been shown to reduce liver triglyceride levels and to improve insulin sensitivity in a diabetic mouse model after an oral dose of 30 mg/kg. | |||
T33450 | |||
ML 23 is a melatonin analogue in the treatment and management of Parkinson's disease. ML-23 is a potential clinical candidate for the treatment of PD, and the present study has been undertaken to determine the efficacy of ML-23 in the 1-methyl-4-phenyl, 1 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPY-01061 | FGF-10 Protein, Human, Recombinant | Human | E. coli | ||
Fibroblast growth factor 10 (FGF10) is a member of the fibroblast growth factor (FGF) family. FGF family members possess broad mitogenic and cell survival activities, and are involved in a variety of biological processes, including embryonic development, cell growth, morphogenesis, tissue repair, tumor growth and invasion. FGF10 exhibits mitogenic activity for keratinizing epidermal cells, but essentially no activity for fibroblasts, which is similar to the biological activity of FGF7. FGF10 plays an important role in the regulation of embryonic development, cell proliferation and cell differentiation. FGF10 is required for normal branching morphogenesis. It may play a role in wound healing. Defects in FGF10 are the cause of autosomal dominant aplasia of lacrimal and salivary glands (ALSG). ALSG has variable expressivity, and affected individuals may have aplasia or hypoplasia of the lacrimal, parotid, submandibular and sublingual glands and absence of the lacrimal puncta. The disorder is characterized by irritable eyes, recurrent eye infections, epiphora (constant tearing) and xerostomia (dryness of the mouth), which increases the risk of dental erosion, dental caries, periodontal disease and oral infections.
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TMPJ-00042 | TSLP Protein, Human, Recombinant | Human | E. coli | ||
Thymic stromal lymphopoietin (TSLP) is a novel member of the hemopoietic cytokine family that promotes the development of B cells and shares overlapping activity with IL-7. The human TSLP protein comprises a 28 amino acids (aa) signal sequence and 131 aa mature region. Human TSLP has two isoforms lfTSLP and sfTSLP produced by alternative splicing . lfTSLP is expressed in a number of tissues including heart, liver and prostate, and sfTSLP (63aa) is predominantly expressed in keratinocytes of oral mucosa, skin and in salivary glands. In aa sequence level, Human TSLP displays about 43% identity with mouse TSLP.TSLP is a cytokine that functions mainly on myeloid cells; it induces the release of T cell-attracting chemokines from monocytes and enhances the maturation of CD11c(+) dendritic cells.TSLP has proliferative effects on the myeloid cell line and may initiate asthma or atopic dermatitis responses by directly activating mast cells . TSLP signals cells via the interleukin-7 receptor-α chain (IL-7Rα),shared with IL-7, together with the TSLP receptor (TSLPR) subunit. Recent studies indicate that TSLP and its receptor are novel therapeutic targets for rheumatoid arthritis,for increased intraarticular TSLP concentrations in patients has caused chemotaxis and activation of arthritogenic T cells.
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TMPY-03225 | VSIG8 Protein, Human, Recombinant (hFc) | Human | HEK293 Cells | ||
V-set and immunoglobulin domain containing 8 (VSIG8) is essential in hair cycle, oral mucosa, and the nail matrix. Moreover, VSIG8 also has an important role in proper epithelial differentiation and function in the upper alimentary tract.
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TMPH-02336 | TAS2R10 Protein, Human, Recombinant (His & KSI) | Human | E. coli | ||
Gustducin-coupled strychnine receptor implicated in the perception of bitter compounds in the oral cavity and the gastrointestinal tract. Signals through PLCB2 and the calcium-regulated cation channel TRPM5. TAS2R10 Protein, Human, Recombinant (His & KSI) is expressed in E. coli expression system with N-6xHis-KSI tag. The predicted molecular weight is 19.6 kDa and the accession number is Q9NYW0.
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TMPY-03851 | BPIFB1 Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
BPIFB1, also known as LPLUNC1, belongs to the BPI/LBP/Plunc superfamily, plunc family. BPIFB1 may be involved in the innate immune response to bacterial exposure in the mouth, nasal cavities, and lungs. BPIFB1 is expressed in the upper respiratory tract and oral cavity, which may function in host defence. The expression of BPIF proteins is associated with CF lung disease in humans and mice. It is unclear if this elevation of protein production, which results from phenotypic alteration of the cells within the diseased epithelium, plays a role in the pathogenesis of the disease. BPIFB1 is an abundant, secreted product of goblet cells and minor mucosal glands of the respiratory tract and oral cavity and suggest that the protein functions in the complex milieu that protects the mucosal surfaces in these locations.
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TMPJ-00157 | CD82 Protein, Human, Recombinant (hFc) | Human | HEK293 Cells | ||
CD82 antigen, also known as Kai-1, is a widely expressed palmitoylated molecule of the tetraspanin superfamily. KAI1/CD82 is localized on cell membrane and form interactions with other tetraspanins, integrins and chemokines which are respectively responsible for cell migration, adhesion and signaling. CD82/Kai-1 is a component of the promiscuous TIMP-1 interacting protein complex on the cell surface of human adenocarcinoma cells and gives insight into tumorigenic metastatic potential. CD82/Kai-1 suppresses EMT in prostate cancer cells adhered to fibronectin leading to reduced cell migration and invasiveness. CD82/Kai-1 function is important for muscle stem cell function in muscular disorders. Overexpression of CD82/Kai-1 suppresses growth, migration and invasion of oral cancer cells and may be considered as a potential therapeutic target in oral cancer.
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TMPH-03154 | Lys-gingipain 381 Protein, Porphyromonas gingivalis, Recombinant (His) | Porphyromonas gingivalis | E. coli | ||
Cysteine proteinase with a strong preference for substrates with Lys in the P1 position. Hydrolyzes bovine hemoglobin, bovine serum albumin, casein, human placental type I collagen and human IgA and IgG. Disrupts the functions of polymorphonuclear leukocytes. May act as a virulence factor in the development of peridontal disease. Involved in the coaggregation of P.gingivalis with other oral bacteria. Lys-gingipain 381 Protein, Porphyromonas gingivalis, Recombinant (His) is expressed in E. coli expression system with N-6xHis tag. The predicted molecular weight is 44.8 kDa and the accession number is P72194.
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TMPH-03155 | Lys-gingipain HG66 Protein, Porphyromonas gingivalis, Recombinant (His & Myc) | Porphyromonas gingivalis | E. coli | ||
Cysteine proteinase with a strong preference for substrates with Lys in the P1 position. Hydrolyzes bovine hemoglobin, bovine serum albumin, casein, human placental type I collagen and human IgA and IgG. Disrupts the functions of polymorphonuclear leukocytes. May act as a virulence factor in the development of peridontal disease. Involved in the coaggregation of P.gingivalis with other oral bacteria. Lys-gingipain HG66 Protein, Porphyromonas gingivalis, Recombinant (His & Myc) is expressed in E. coli expression system with N-10xHis and C-Myc tag. The predicted molecular weight is 46.4 kDa and the accession number is P72197.
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TMPJ-00860 | HTN3 Protein, Human, Recombinant | Human | E. coli | ||
HTN3 belongs to the histatin/statherin family. Histatins are salivary proteins that are considered to be major precursors of the protective proteinaceous structure on tooth surfaces (enamel pellicle). In addition, histatins exhibit antibacterial and antifungal activities. Post-translational proteolytic processing results in many histatins: e.g., histatins 4-6 are derived from histatin 3 by proteolysis. Histatins 1 and 3 are primary products of HIS1and HIS2 alleles, respectively. Histatins are believed to have important non-immunological, anti-microbial function in the oral cavity.
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TMPH-03156 | Lys-gingipain Protein, Porphyromonas gingivalis, Recombinant (His & SUMO) | Porphyromonas gingivalis | E. coli | ||
Cysteine proteinase with a strong preference for substrates with Lys in the P1 position. Hydrolyzes bovine hemoglobin, bovine serum albumin, casein, human placental type I collagen and human IgA and IgG. Disrupts the functions of polymorphonuclear leukocytes. May act as a virulence factor in the development of peridontal disease. Involved in the coaggregation of P.gingivalis with other oral bacteria. Lys-gingipain Protein, Porphyromonas gingivalis, Recombinant (His & SUMO) is expressed in E. coli expression system with N-6xHis-SUMO tag. The predicted molecular weight is 56.6 kDa and the accession number is B2RLK2.
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TMPY-03971 | Statherin Protein, Human, Recombinant (mFc) | Human | HEK293 Cells | ||
Statherin, also known as STATH, belongs to the histatin/statherin family. Statherin may play an important role in the maintenance of oral health. It prevents calcium phospate precipitation in saliva, so maintaining a high calcium level in saliva and preventing teeth from dissolving. Statherin also inhibits spontaneous precipitation of calcium phosphate salts. Thus, statherin and PRPs may prevent build-up of harmful deposits in the salivary glands and on the tooth surfaces. Statherin is a highly stable salivary protein of low molecular mass (5,380).
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TMPJ-00764 | Catalase/CAT Protein, Human, Recombinant | Human | E. coli | ||
Catalase (CAT) is a member of the catalase family. It exists as a homotetramer that occurs in almost all aerobically respiring organisms and serves to protect cells from the toxic effects of hydrogen peroxide. Catalase is localized in the peroxisome. Catalase promotes growth of cells including T-cells, B-cells, myeloid leukemia cells, melanoma cells, mastocytoma cells, and normal and transformed fibroblast cells. Defects in CAT are the cause of acatalasemia which is characterized by absence of catalase activity in red cells and is associated with ulcerating oral lesions.
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TMPH-00331 | ALS3 Protein, Candida albicans, Recombinant (B2M & His & Myc) | Candida albicans | E. coli | ||
Cell surface adhesion protein which mediates both yeast-to-host tissue adherence and yeast aggregation. Plays an important role in the biofilm formation and pathogenesis of C.albicans infections. Necessary for C.albicans to bind to N-cadherin on endothelial cells and E-cadherin on oral epithelial cells and subsequent endocytosis by these cells. During disseminated infection, mediates initial trafficking to the brain and renal cortex and contributes to fungal persistence in the kidneys. ALS3 Protein, Candida albicans, Recombinant (B2M & His & Myc) is expressed in E. coli expression system with N-10xHis-B2M and C-Myc tag. The predicted molecular weight is 37.9 kDa and the accession number is O74623.
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TMPJ-00160 | EMMPRIN/CD147 Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
Extracellular Matrix Metalloproteinase Inducer (EMMPRIN) belongs to the immunoglobulin superfamily, which has the homology to both the immunoglobulin V domain and MHC class II antigen β-chain. EMMPRIN is a transmembrane glycoprotein with different forms, resulting from different modes of glycosylation and N-terminal sequence variants. EMMPRIN can be expressed in breast cancer, oral squamous cell carcinoma, glioma, lymphoma, lung, bladder, and melanoma carcinomas cells. EMMPRIN promotes invasion, metastasis, growth, and survival of malignants cells, serves as a receptor for extracellular cyclophilinthe, may play a role in signal transduction.
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TMPJ-01207 | UPP1 Protein, Human, Recombinant (His) | Human | E. coli | ||
Uridinephosphorylase 1 (UPP1) is a member of the family of pentosyltransferase. UPP1 catalyses the reversible phosphorolysis of uridine to uracil. The expression levels and the enzymatic activity of UPP1 are higher in human solid tumors than in adjacent normal tissues. The high level of UPP1 expression in some tumors makes it a potential prognosticfactor for some cancers, such as oral squamous cell carcinoma. UPP1 is important for the homeostatic regulation of intracellular and plasma uridine concentratios. UPP1 plays an important role in the pyrimidine salvage pathway through its catalysis of the reversible phosphorolysis of uridine to uracil.
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TMPY-03332 | PRTFDC1 Protein, Human, Recombinant (His) | Human | E. coli | ||
PRTFDC1 is a member of the purine/pyrimidine phosphoribosyltransferase family. It can bind GMP, IMP and alpha-D-5-phosphoribosyl 1-pyrophosphate (PRPP). The epigenetic silencing of PRTFDC1 by hypermethylation of the CpG island leads to a loss of PRTFDC1 function, which might be involved in squamous cell oral carcinogenesis. PRTFDC1 is a genetic modifier of HPRT-deficiency in the mouse and has important implications for unraveling the molecular etiology of lesch-Nyhan disease(LND). LND is a severe X-linked neurological disorder caused by a deficiency of hypoxanthine phosphoribosyltransferase. PRTFDC1 has a low, barely measurable phosphoribosyltransferase activity (in vitro).
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TMPJ-01372 | Cornulin Protein, Human, Recombinant (His) | Human | E. coli | ||
Cornulin is a member of the fused gene family of molecular chaperones. Human Cornulin contains N-terminus EF-hand domains and Ca2+ binding domains, and two glutamine- and threonine-rich 60 amino acid repeats in its C-terminus. Cornulin involves in the mucosal/epithelial immune response and epidermal differentiation. Cornulin is a survival factor that participates in the clonogenicity of squamous esophageal epithelium cell lines, attenuates deoxycholic acid (DCA)-induced apoptotic cell death and release of calcium. When Cornulin is overexpressed in oral squamous carcinoma cell lines, it regulates negatively cell proliferation by the induction of G1 arrest.
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TMPY-04170 | DEFB1 Protein, Human, Recombinant (hFc) | Human | HEK293 Cells | ||
The DEFB1 gene, encoding for the constitutively expressed human beta-defensin 1 (hBD1) antimicrobial peptide is a potential candidate when studying genetic susceptibility to caries. DEFB1 genetic variations have been reported as contributing to hBD1 production impairment, leading to a greater susceptibility to be infected by oral pathogens, also leading to periodontitis. To counteract host immunity, Cryptosporidium parvum has evolved multiple strategies to suppress host antimicrobial defense. One such strategy is to reduce the production of the antimicrobial peptide beta-defensin 1 (DEFB1) by host epithelial cells. Beta-Defensin-1, an antimicrobial peptide encoded by the DEFB1 gene, is known to play an important role in lung mucosal immunity.
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TMPJ-01173 | TFF3 Protein, Mouse, Recombinant (His) | Mouse | HEK293 Cells | ||
Trefoil factors (TFF) are secretory products of mucin producing cells. They play a key role in the maintenance of the surface integrity of oral mucosa and enhance healing of the gastrointestinal mucosa by a process called restitution. TFF comprises the gastric peptides (TFF1), spasmolytic peptide (TFF2), and the intestinal trefoil factor (TFF3). They have an important and necessary role in epithelial restitution within the gastrointestinal tract. Members of the trefoil family are characterized by having at least one copy of the trefoil motif, a 40-amino acid domain that contains three conserved disulfide bonds. They are stable secretory proteins expressed in gastrointestinal mucosa. Trefoil Factor 3(TFF3) is involved in the maintenance and repair of the intestinal mucosa. TFF3 promotes the mobility of epithelial cells in healing processes (motogen).
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TMPH-00672 | Metalloprotease stcE Protein, E. coli O157:H7, Recombinant (His) | E. coli | E. coli | ||
Virulence factor that contributes to intimate adherence of enterohemorrhagic E.coli (EHEC) O157:H7 to host cells. Is able to cleave the secreted human mucin 7 (MUC7) and the glycoprotein 340 (DMBT1/GP340). Also cleaves human C1 inhibitor (SERPING1), a regulator of multiple inflammatory pathways, and binds and localizes it to bacterial and host cell surfaces, protecting them from complement-mediated lysis. Therefore, the current model proposes two roles for StcE during infection: it acts first as a mucinase, allowing passage of EHEC through the oral cavity by cleaving the salivary glycoproteins that are responsible for bacterial aggregation. Similarly, in the colon, StcE cleaves the glycoproteins that protect the intestinal epithelial surface, allowing EHEC to come into close contact with host cell membranes. Secondly, it acts as an anti-inflammatory agent by localizing SERPING1 to cell membranes.
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TMPY-02391 | SUMO1 Protein, Human, Recombinant (His) | Human | E. coli | ||
Small ubiquitin-like modifier protein (SUMO) modification is a highly dynamic process, catalyzed by SUMO-specific activating (E1), conjugating (E2) and ligating (E3) enzymes, and reversed by a family of SUMO-specific proteases (SENPs). Small ubiquitin-like modifier 1 (SUMO1) is a member of the superfamily of ubiquitin-like proteins. Despite its structural similarity with ubiquitin, SUMO1 does not seem to play any role in protein degradation. SUMO1 plays an important role in modulation of NOX activity required for ROS generation. SUMO1 haploinsufficiency results in cleft lip and palate in animal models. SUMO1 gene variation in human non-syndromic cleft lip with or without cleft palate (NSCLP) development. SUMO-1 may be useful as a novel target for therapy in oral squamous cell carcinoma (SCC) as well as a clinical indicator for tumor recurrence together with Mdm2.
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TMPY-02220 | HRAS Protein, Human, Recombinant (His) | Human | Baculovirus Insect Cells | ||
HRas, also known as HRAS, belongs to the small GTPase superfamily, Ras family, and is widely expressed. It functions in signal transduction pathways. HRas can bind GTP and GDP, and they have intrinsic GTPase activity. It undergoes a continuous cycle of de- and re-palmitoylation, which regulates its rapid exchange between the plasma membrane and the Golgi apparatus. Defects in HRAS are the cause of faciocutaneoskeletal syndrome (FCSS). FCSS is a rare condition characterized by prenatally increased growth, postnatal growth deficiency, mental retardation, distinctive facial appearance, cardiovascular abnormalities, tumor predisposition, skin, and musculoskeletal abnormalities. Defects in HRAS also can cause congenital myopathy with excess of muscle spindles. HRAS deficiency may be a cause of susceptibility to Hurthle cell thyroid carcinoma. It has been shown that defects in HRAS can cause susceptibility to bladder cancer which is a malignancy originating in tissues of the urinary bladder. It often presents with multiple tumors appearing at different times and different sites in the bladder. Most bladder cancers are transitional cell carcinomas. They begin in cells that normally make up the inner lining of the bladder. Other types of bladder cancer include squamous cell carcinoma (cancer that begins in thin, flat cells) and adenocarcinoma (cancer that begins in cells that make and release mucus and other fluids). Bladder cancer is a complex disorder with both genetic and environmental influences. Defects in HRAS are the cause of oral squamous cell carcinoma.Cancer ImmunotherapyImmune CheckpointImmunotherapyTargeted Therapy
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