SB-431542

301836-41-9

C22H16N4O3

DMSO : >= 40 mg/mL (104.06 mM); Ethanol : 11.17 mg/mL (29.06 mM; Need ultrasonic and warming)

TGF-beta/Smad

SB-431542 is a potent and selective inhibitor of ALK5/TGF-beta type I Receptor with an IC₅₀ value of 94 nM. IC50 & Target: IC50: 94 nM (ALK5)^[2] In Vitro: SB-431542 (1 uM) significantly reduces the TGF-beta-induced nuclear accumulation of Smad proteins in A498 cells. SB-431542 inhibits TGF-beta1-induced collagen Ialpha1 and PAI-1 mRNA with IC₅₀ values of 60 and 50 nM, respectively. In addition, SB-431542 inhibits TGF-beta1-induced fibronectin mRNA and protein with IC₅₀ values of 62 and 22 nM, respectively^[1]. SB-431542 (10 uM) is a selective inhibitor of TGF-beta 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 uM) inhibits cell proliferation induced by TGF-beta in MG63 cells^[4]. 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].