SB431542 (301836-41-9) Description:
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 is a member of the class of benzamides that is 4-(imidazol-2-yl)benzamide carrying additional 1,3-benzodioxol-5-yl and pyridin-2-yl substituents at positions 4 and 5 respectively on the imidazole ring. It has a role as an EC 22.214.171.124 (receptor protein-tyrosine kinase) inhibitor. It is a member of benzamides, a member of imidazoles, a member of pyridines and a member of benzodioxoles.
Renal carcinoma studies have demonstrated that SB 431542 is a selective inhibitor of Smad3 phosphorylation (IC50= 94nM) and TGF-β-1 collagen induced lα1 (col Iα1). It has been reported that SB 431542 does not affect the JNK, ERK, or p38 MAP kinase pathways. SB 431542 has been shown to suppress TGF-β induced growth stimulation in MG63 cells, inhibit the motility and proliferation of glioma cells, and block the phosphorylation and translocation of SMADs.
SB-431542 is a potent and selective inhibitor of the TGF-β1 receptor ALK5 (IC50 = 94 nM)1. It is a less potent antagonist of ALK4 (IC50 = 140 nM)2 and ALK7.3 It does not affect the BMP receptors ALK2, ALK3, ALK6, or a panel of other kinases tested.3 SB-431542 specifically blocks Smad signaling, reducing gene expression relevant to fibrosis and cancer.3 Through its effects on ALK/Smad signaling, SB-431542 suppresses renewal in embryonic and induced pluripotent stem cells and promotes their differentiation.
SB431542 (301836-41-9) Specifications:
|Synonyms||SB-431542; SB 431542|
|Molecular Weight||384.395 g/mol|
|Monoisotopic Mass||384.122 g/mol|
|Solubility||Soluble in DMSO (20 mg/ml), and ethanol (20 mg/ml).|
|Storage Temp.||0 – 4 C for short term (days to weeks), or -20 C for long term (months).|
|Shelf life||>2 years if stored properly|
|Handling||Protect from air and light|
|Application||A specific and selective inhibitor of TGF-β type I ALK receptors and Smad3; TGF-beta/Smad inhibitor|