SB-431542|SB431542,TGF-B-R inhibitor|supplier DC Chemicals

Cas No.:	301836-41-9
Chemical Name:	SB-431542
Synonyms:	4-(4-(Benzo[d][1,3]dioxol-5-yl)-5-(pyridin-2-yl)-1H-imidazol-2-yl)benzamide;SB431542;4-[4-(1,3-benzodioxol-5-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]Benzamide;SB-431542;SB431542 （SB-431542, SB 431542 ）;4-[4-(3,4-Methylenedioxyphenyl)-5-(2-pyridyl)-1H-imidazol-2-yl]benzamide;SB 431542;C22H16N4O3;E1557V1V0N;4-[4-(1,3-benzodioxol-5-yl)-5-pyridin-2-yl-1H-imidazol-2-yl]benzamide;4-(4-(1,3-Benzodioxole-5-yl)-5-(2-pyridyl)-1H-imidazole-2-yl)benzamide;4-[5-(1,3-Benzodioxol-5-Yl)-4-(Pyridin-2-Yl)-1h
SMILES:	O1C([H])([H])OC2C([H])=C([H])C(=C([H])C1=2)C1=C(C2=C([H])C([H])=C([H])C([H])=N2)N([H])C(C2C([H])=C([H])C(C(N([H])[H])=O)=C([H])C=2[H])=N1
Formula:	C₂₂H₁₆N₄O₃
M.Wt:	384.3874
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	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.
In Vivo:	SB-431542 (10 mg/kg, i.p.) decreases lung metastasis but does not significantly alter growth of the primary tumor 4T1 xenograft[5].
In Vitro:	SB-431542 (1 μM) significantly reduces the TGF-β-induced nuclear accumulation of Smad proteins in A498 cells. SB-431542 inhibits TGF-β1-induced collagen Iα1 and PAI-1 mRNA with IC50 values of 60 and 50 nM, respectively. In addition, SB-431542 inhibits TGF-β1-induced fibronectin mRNA and protein with IC50 values of 62 and 22 nM, respectively[1]. SB-431542 (10 μM) is a selective inhibitor of endogenous activin and TGF-β signaling but has no effect on BMP signaling in NIH 3T3 cells[2]. TRKI, SB-431542, inhibits TGF-beta-induced transcription, gene expression, apoptosis, and growth suppression. SB-431542 attenuates the tumor-promoting effects of TGF-beta, including TGF-beta-induced EMT, cell motility, migration and invasion, and vascular endothelial growth factor secretion in human cancer cell lines. SB-431542 induces anchorage independent growth of cells that are growth-inhibited by TGF-beta, whereas it reduces colony formation by cells that are growth-promoted by TGF-beta[3]. SB-431542 (0.3 μM) inhibits cell proliferation induced by TGF-β in MG63 cells[4].

Cat. No.	Product name	Field of application
DC7739	SD-208	SD-208 is a potent, orally active ATP-competitive transforming growth factor-β receptor 1 (TGF-βRI) inhibitor (IC50= 49 nM)
DC6312	SB525334	SB525334 is a potent and selective inhibitor of TGFβ receptor I (ALK5) with IC50 of 14.3 nM, is 4-fold less potent to ALK4 than ALK5 and inactive to ALK2, 3, and 6.
DC5189	SB-431542	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.
DC7259	Repsox（ALK5 Inhibitor II）	RepSox(E-616452; SJN 2511) is a potent and selective inhibitor of the TGFβR-1/ALK5 with IC50 of 23 nM and 4 nM for ATP binding to ALK5 and ALK5 autophosphorylation, respectively.
DC7587	ML347	ML347 is a selective BMP receptor inhibitor with IC50 of 32 nM for ALK2, >300-fold selectivity over ALK3. Also inhibits ALK1 activity with IC50 of 46 nM
DC10675	LY3200882	LY3200882 is a novel, highly selective TGFβRI small molecule inhibitor.
DC6306	LY2157299(Galunisertib)	LY2157299 is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM. Phase 2.
DC7914	LDN-214117	LDN-214117 is a potent and selective ALK2 inhibitor with IC50 of 22 nM; > 100 fold selectivity for ALK5; also inhibits BMP6(IC50=100 nM).
DC7742	K02288	K02288 is a potent, and selective type I BMP receptor inhibitor with IC50 of 1.1, 1.8, 6.4 nM for ALK2, ALK1 and ALK6, showing weaker inhibition on other ALKs (3, 4, 5) and ActRIIA.
DC8028	ITD-1	ITD-1 is a novel and highly selective TGFβ pathway inhibitor. ITD-1 molecule turns stem cells into heart cells.