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|Synonyms||SB 431542; SB431542; 4-(4-(benzo[d][1,3]dioxol-5-yl)-5-(pyridin-2-yl)-1H-imidazol-2-yl)benzamide|
SB-431542 is potent and selective inhibitor of the transforming growth factor-β (TGF-β) type I receptor activin receptor-like kinase ALK5 (IC50 = 94 nM) and its relatives ALK4 and ALK7.
|Inhibitor of the TGF-beta type I receptor kinase activity ......by AOBIOUS INC|
SB431542 is a selective ATP-competitive inhibitor of ALK5 (activin receptor-like kinase 5) with an IC50 value of 94 nM .
SB431542 showed most potent efficacy among the series of hits screened out. It inhibited TGF-β1-induced mRNA formation in A498 cells with IC50 value of 50 nM. It also markedly reduced TGF-β-induced nuclear accumulation of Smad proteins with IC50 value of 40 nM. SB431542 was found to be a selective inhibitor for ALK4, ALK5 and ALK7, suppresses the phosphorylation of Smad2. It showed no significant inhibition of ALK1, ALK2, ALK6 and showed weak effect on ALK3 at concentration of 10 μM [1, 2].
|SB-431542 is a potent and selective inhibitor of ALK5 with an IC50 value of 94 nM, and is also an inhibitor of TGF-β Receptor. ......by MedChemexpress Co., Ltd.|
|SB-431542 is a novel small molecule inhibitor of the type I TGF-beta receptor, on a panel of human malignant glioma cell lines. SB-431542 blocked the phosphorylation and nuclear translocation of the SMADs, intracellular mediators of TGF-beta signaling, with decreased TGF-beta-mediated transcription. Furthermore, SB-431542 inhibited the expression of two critical effectors of TGF-beta-vascular endothelial growth factor and plasminogen activator inhibitor-1. SB-431542 treatment of glioma cultures inhibited proliferation, TGF-beta-mediated morphologic changes, and cellular motility. Together, our results suggest that small molecule inhibitors of TGF-beta receptors may offer a novel therapy for malignant gliomas by reducing cell proliferation, angiogenesis, and motility. (source: Mol Cancer Ther. 2004 Jun;3(6):737-45.) Shelf life: >2 years if stored properly Drug formulation: This drug may be formulated in DMSO ......by MedKoo Biosciences, Inc.|
|SB431542 is a potent and selective inhibitor of ALK5 with IC50 of 94 nM, 100-fold more selective for ALK5 than p38 MAPK and other kinases. ......by Selleck Chemicals LLC|
|SB431542 is a potent and selective inhibitor of ALK5 with IC50 of 94 nM in a cell-free assay, 100-fold more selective for ALK5 than p38 MAPK and other kinases. ......by Target Molecule Corp.|
|Cell lines||D54MG, U87MG and U373MG cells|
|Conditions||10 μM, 24 hours|
|Method||SB-431542 at both 0.1 and 1μmol/L had a modest effect on DNA synthesis, but at 10 μmol/L, there was a consistent 60% to 70% reduction of thymidine incorporation for D54MG, U87MG, and U373MG cells. No evidence of apoptotic cell death on SB-431542 treatment was detected either by direct observation or on propidium iodide flow cytometric analysis. Thus, SB-431542 acts to inhibit the proliferation of the tested malignant glioma lines.|
|Source||Apexbio Technology LLC|
|Animal Models||BALB/c mice injected with colon-26 cells|
|Dosage Form||Intraperitoneal injection, 1 μM|
|Applications||Intraperitoneal injection of SB-431542 resulted in triggering CTL activities against colon-26 targets compared with vehicle alone. Moreover, the CTL activity against colon-26 cells was more potent when treated with SB combined a ligand for toll-like receptor 4, OK-432, compared with OK-432 alone. Thus, SB-431542 is likely to produce antitumor immunological outcomes through alteration of DC function suppressed by TGFß.|
|Source||Apexbio Technology LLC|
|Appearance:White to off-white solid||EBNumber:EB000029031|
|Store at RT||by Apexbio Technology LLC|
|Storage condition:Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). Stock solution storage:0 - 4 C for short term (days to weeks), or -20 C for long term (months). Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.||by MedKoo Biosciences, Inc.|
|Soluble in DMSO > 10 mM||by Apexbio Technology LLC|
|DMSO ≥75mg/mL Water <1.2mg/mL Ethanol ≥42mg/mL||by MedChemexpress Co., Ltd.|
|Soluble in DMSO, not in water||by MedKoo Biosciences, Inc.|
|DMSO 77 mg/mL (200 mM) ; Water <1 mg/mL (<1 mM) ; Ethanol 3 mg/mL (7 mM)||by Selleck Chemicals LLC|
|Company||Price and Availability||Country/Region|
|Apexbio Technology LLC||USA|
|BOC Sciences||50mg/USD198(In stock)|
|Biochempartner Co., Ltd||China|
|Chemfuture Pharma Tech (Jiangsu) Ltd.||China|
|MedChemexpress Co., Ltd.||10mg/USD96();50mg/USD360()||USA|
|MedKoo Biosciences, Inc.||USA|
|Pure Chemistry Scientific Inc.||10mg/USD65(In stock)||USA|
|Selleck Chemicals LLC||10mg/USD110(In stock);10mM/1mLIn DMSO/USD143(In stock);50mg/USD470(In stock);200mg/USD1270(In stock)||USA|
|Shanghai Haoyuan Chemexpress Co., Ltd.||10mg/USD96();50mg/USD360()||China|
|Target Molecule Corp.||10mg/USD80();50mg/USD266();100mg/USD475()||USA|
. Inman GJ, et al. SB-431542 is a potent and specific inhibitor of transforming growth factor-beta superfamily type I activin receptor-like kinase (ALK) receptors ALK4, ALK5, and ALK7. Mol Pharmacol, 2002, 62(1), 65-74.
. Laping NJ, et al. Inhibition of transforming growth factor (TGF)-beta1-induced extracellular matrix with a novel inhibitor of the TGF-beta type I receptor kinase activity: SB-431542. Mol Pharmacol, 2002, 62(1), 58-64.
 Hjelmeland M D, Hjelmeland A B, Sathornsumetee S, et al. SB-431542, a small molecule transforming growth factor-β-receptor antagonist, inhibits human glioma cell line proliferation and motility. Molecular Cancer Therapeutics, 2004, 3(6): 737-745.
 Tanaka H, Shinto O, Yashiro M, et al. Transforming growth factor b signaling inhibitor, SB-431542, induces maturation of dendritic cells and enhances anti-tumor activity. Oncology reports, 2010, 24: 1637-1643.......by Apexbio Technology LLC