SB-431542

Research use only, not for human use.

SB-431542 is a potent, specific TGF-β type I receptor (ALK5) inhibitor with IC50 of 94 nM.

SB-431542 is a potent, specific TGF-β type I receptor (ALK5) inhibitor with IC50 of 94 nM; also substantially inhibits ALK4 and 7, but not other ALKs; efficiently inhibits the ability of activated ALK4, ALK5, and ALK7 to phosphorylate Smad2; a selective inhibitor of endogenous activin and TGF-beta signaling but has no effect on BMP signaling, and has no effect on components of the ERK, JNK, or p38 MAP kinase pathways.(In Vitro):SB-431542 can inhibit the activity for ALK4, ALK5 and ALK7 with IC50 values of 1 μM, 0.75 μM and 2 μM, respectively.SB-431542 (0- 10 μM; 24 h) inhibits ALK5 and also the activin type I receptor ALK4 and the nodal type I receptor ALK7, which are very highly related to ALK5 in their kinase domains.SB-431542 (0.1, 0.5, 1, 5, or 10 μM; 30 min) efficiently inhibits Smad phosphorylation induced by TGF-β and activin but not BMP4.SB-431542 (0-10 μM) inhibits TGF-beta-induced transcription, gene expression, apoptosis, and growth suppression.(In Vivo):SB-431542 (subconjunctival; 0.5 and 2 mM; on days 1, 2, 3, and 7) inhibits scar formation after glaucoma filtration surgery in New Zealand rabbits.

SB-431542 (GMP) (10 μM; 10 days) induces human pluripotent stem cells (hPSCs) to post-mitotic cortical neurons differentiation.SB-431542 (GMP) (10 μM) facilitates directed differentiation into midbrain dopamine neurons (mDA).SB-431542 (GMP) (3.8 μM) promotes differentiation of hPSCs to multipotent hematopoietic progenitors that arise from SOX17+ hemogenic endothelium in vitro. RT-PCRCell Line:Human pluripotent stem cells (hPSCs)Concentration:10 μM Incubation Time:10 days Result:Showed downregulation of the pluripotency marker OCT4 and induction of neural and neuronal markers PAX6, FOXG1 and DCX, as well as markers of early born cortical neurons, including TBR1 (preplate, subplate and layer VI) and REELIN, in LSB+X/P/S/D conditions.

——

SB 431542 | SB431542

TGF-beta/Smad

TGFBR

ALK5|ALK4

Cancer

——

301836-41-9

384.3875

C22H16N4O3

>98% (HPLC)

DMSO: ≥ 40 mg/mL; Ethanol: 11.17 mg/mL (Need ultrasonic and warming)

O=C(N)C1=CC=C(C2=NC(C3=CC=C(OCO4)C4=C3)=C(C5=NC=CC=C5)N2)C=C1

Benzamide, 4-[4-(1,3-benzodioxol-5-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]-

(-20℃)

With Ice Pack

≥ 2 years