目录号 | 产品详情 | 靶点 | |
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T68249 | |||
IRC-083927 HCl is novel and potent microtubule inhibitor with potential anticancer activity. IRC-083927 inhibits the tubulin polymerization by a binding to the colchicine site. IRC-083927 inhibits in vitro cell growth of human cancer cell lines in the low nanomolar range. More interesting, it remains highly active against cell lines resistant to microtubule-interacting agents (taxanes, Vinca alkaloids, or epothilones). Chronic oral treatment with IRC-083927 (5 mg/kg) inhibits the growth of two human tumor xenografts in nude mice (C33-A, human cervical cancer and MDA-MB-231, human hormone-independent breast cancer). Together, the antitumor effects induced by IRC-083927 on tumor models resistant to tubulin agents support further investigations to fully evaluate its potential for the treatment of advanced cancers, particularly those resistant to current clinically available drugs. | |||
T35816 | |||
ZLY032 is a dual agonist of free fatty acid receptor 1 (FFAR1/GPR40; EC50= 68 nM in a FLIPR assay) and peroxisome proliferator-activated receptor δ (PPARδ; EC50= 102 nM in a reporter assay).1It is selective for FFAR1 and PPARδ over PPARα and PPARγ (EC50s = >10 μM for both). ZLY032 (40 mg/kg, twice per day) reduces blood glucose levels in an oral glucose tolerance test and decreases plasma total cholesterol and triglyceride levels in theob/obmouse model of metabolic disease.2It reduces hepatic steatosis and plasma alanine transaminase (ALT) and aspartate aminotransferase (AST) levels in a mouse model of non-alcoholic steatohepatitis (NASH) induced by a methionine and choline-deficient diet at the same dose. 1.Li, Z., Chen, Y., Zhou, Z., et al.Discovery of first-in-class thiazole-based dual FFA1/PPARδ agonists as potential anti-diabetic agentsEur. J. Med. Chem.164352-365(2019) 2.Li, Z., Zhou, Z., Hu, L., et al.ZLY032, the first-in-class dual FFA1/PPARδ agonist, improves glucolipid metabolism and alleviates hepatic fibrosisPharmacol Res.159105035(2020) | |||
T35426 | |||
β-Defensin-1 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts.1It inhibits the growth ofB. adolescentis,L. acidophilus,B. breve,B. vulgatus,L. fermentum,B. longum, andS. thermophilusin an antimicrobial radial diffusion assay.2β-Defensin-1 also inhibits the growth of periodontopathogenic and cariogenic bacteria, includingP. gingivalisandS. salivarius, and of susceptibleM. tuberculosisH37Rv but not of resistantM. tuberculosisRM22 when used at a concentration of 128 μg/ml.3,4It blocks human and mouse Kv1.3 voltage-gated potassium channels (IC50s = 11.8 and 13.2 μM, respectively).5Overexpression of β-defensin-1 in the human oral squamous cell carcinoma (OSCC) cell lines HSC-3, UM-1, and SCC-9 increases migration and invasion but not proliferation.6 1.Lehrer, R.I.Primate defensinsNat. Rev. Microbiol.2(9)727-738(2004) 2.Schroeder, B.O., Ehmann, D., Precht, J.C., et al.Paneth cell α-defensin 6 (HD-6) is an antimicrobial peptideMucosal Immunol.8(3)661-671(2015) 3.Ouhara, K., Komatsuzawa, H., Yamada, S., et al.Susceptibilities of periodontopathogenic and cariogenic bacteria to antibacterial peptides, β-defensins and LL37, produced by human epithelial cellsJ. Antimicrob. Chemother.55(6)888-896(2005) 4.Fattorini, L., Gennaro, R., Zanetti, M., et al.In vitro activity of protegrin-1 and beta-defensin-1, alone and in combination with isoniazid, against Mycobacterium tuberculosisPeptides25(7)1075-1077(2004) 5.Feng, J., Xie, Z., Yang, W., et al.Human beta-defensin 1, a new animal toxin-like blocker of potassium channelToxicon113(2016) 6.Han, Q., Wang, R., Sun, C., et al.Human beta-defensin-1 suppresses tumor migration and invasion and is an independent predictor for survival of oral squamous cell carcinoma patientsPLoS One9(3)e91867(2014) | |||
T82251 | NO Synthase | ||
GW274150 (dihydrochloride) 是高效、选择性的 NADPH 依赖型人诱导型一氧化氮合成酶 (iNOS) (Kd=40 nM) 抑制剂,具有口服活性,同时对大鼠 (iNOS) 也有效。相较于人和大鼠的内皮一氧化氮合酶 (eNOS) 及神经元一氧化氮合酶 (nNOS),其效力显著较低。GW274150 (dihydrochloride) 在急性肺损伤炎症模型中具有保护作用。 | |||
T14493 | Others | ||
Balapiravir (R1626, Ro 4588161) is the prodrug of a nucleoside analogue inhibitor of the hepatitis C virus (HCV) RNA-dependent RNA polymerase (R1479, RG1479). IC50 Value: Target: HCV Balapiravir was discontinued for safety reasons in 28-36% of patients (m | |||
T35813 | |||
Peroxisome proliferator-activated receptors (PPARs) α, δ, γ are ligand-activated nuclear transcription factors involved in the regulation of energy homeostasis as well as insulin sensitivity and glucose metabolism. Pharmacologies of PPARδ receptor agonists, though relatively obscure, have recently been reported to elevate high-density lipoprotein (HDL) cholesterol and lower plasma triglyceride (TG) levels in obese insulin resistant rhesus monkeys. CAY10592 is a full PPARδ agonist (EC50 = 30 nM) in a fatty acid oxidation assay of rat L6 muscle cells with desirable oral pharmacokinetic properties. In a transactivation assay using human PPAR receptors, CAY10592 acts as a selective partial PPARδ agonist (EC50 = 53 nM) with no effect on PPARα or PPARγ activity up to 30 μM. Chronic treatment of high fat fed ApoB100/CETP-transgenic mice with CAY10592 at a dose of 20 mg/kg increases HDL levels, decreases LDL and TG levels, and improves insulin sensitivity. | |||
T71252 | |||
PC-046 is a potent tubulin-binding agent, which was originally identified for development based on selective activity in deleted in pancreas cancer locus 4 (DPC4/SMAD4) deficient tumors. PC-046 has growth inhibitory activity in a variety of tumor types in vitro, and efficacy in SCID mice was shown in human tumor xenografts of MV-4-11 acute myeloid leukemia, MM.1S multiple myeloma, and DU-145 prostate cancer. Pharmacokinetic studies demonstrated relatively high oral bioavailability (71 %) with distribution to both plasma and bone marrow. No myelosuppression was seen in non-tumor bearing SCID mice given a single dose just under the acute lethal dose. The COMPARE algorithm in the NCI-60 cell line panel demonstrated that PC-046 closely correlated to other known tubulin destabilizing agents (correlation coefficients ≈0.7 for vincristine and vinblastine). Mechanism of action studies showed cell cycle arrest in metaphase and inhibition of tubulin polymerization. Overall, these studi...... | |||
T3512 | FGFR c-Met/HGFR TAM Receptor | ||
S49076 HCl (S-49076 Hydrochloride) 是 MET、AXL/MER 和 FGFR1/2/3 的有效抑制剂。S49076 HCl 在体外和体内有效阻断 MET、AXL 和 FGFR 的细胞磷酸化并抑制下游信号传导。在细胞模型中,S49076 HCl (S-49076 Hydrochloride) 抑制 MET 和 FGFR2 依赖性胃癌细胞的增殖,阻断 MET 驱动的肺癌细胞迁移,并抑制表达 FGFR1/2 和 AXL 的肝癌细胞的集落形成。在肿瘤异种移植模型中,建立了口服 S49076 HCl (S-49076 Hydrochloride) 后 MET 和 FGFR2 抑制的良好药代动力学/药效学关系,并与对肿瘤生长的影响密切相关。 | |||
T63074 | |||
Ivaltinostat (CG-200745) formic 是一种口服具有活力的泛 HDAC 抑制剂,具有异羟肟酸部分,能够在催化袋底部结合锌。Ivaltinostat formic 对组蛋白 H3 和微管蛋白的脱乙酰作用具有抑制效果。Ivaltinostat formic 能够促使 p53 的积累,诱导 p53 依赖性反式激活,并提高 MDM2 和 p21 (Waf1/Cip1) 蛋白的表达。Ivaltinostat formic 增加 Gemcitabine 耐药细胞对 Gemcitabine 和 5-Fluorouracil (5-FU) 的敏感性。Ivaltinostat formic 诱导凋亡,并具有抗肿瘤效果。 | |||
T11449 | STAT | ||
Golotimod (SCV 07) hydrochloride 是一种免疫调节肽,具抗菌活性,能显著提升抗结核疾病研究效果。该化合物通过刺激胸腺和脾细胞增殖、改善巨噬细胞功能,展现其生物调节能力。此外,Golotimod hydrochloride 通过抑制STAT3信号传导,有效调节接受放疗或与顺铂联用治疗动物模型中的口腔粘膜炎持续时间和严重程度。还显示出对研究复发性生殖器单纯疱疹病毒 2 型 (HSV-2) 具有潜在应用价值。 |
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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