A 83-01

Short Summary : ALK-5 inhibitor

Category : TGF-β / Smad Signaling|TGF-βR1(ALK5)

Purity : 0.98

CAS Number : 909910-43-6

Formula : C25H19N5S

Molecular Weight : 421.52

SMILE : CC1=CC=CC(=N1)C2=NN(C=C2C3=CC=NC4=CC=CC=C34)C(=S)NC5=CC=CC=C5

Solubility : >21.1mg/mL in DMSO

Storage : Store at -20°C

Description : A 83-01 is a small-molecule inhibitor of activin receptorlike kinase (ALK)-5 with IC50 value of 12 nM [1].
A 83-01 inhibited 68% of the transcriptional activation induced by ALK-5 at concentration of 1 M in Mv1LuR4-2 cells that transfected with luciferase reporter gene and constitutively active ALK-5. In cells transfected with luciferase reporter gene only, A 83-01 treatment inhibited the activity of ALK-5 induced by TGF- (IC50 value was 12 nM) but not BMP. A 83-01 also showed inhibition on the activity of ALK-4 and ALK-7 in R4-2 cells with IC50 values of 45 and 7.5 nM, respectively. For other ALK receptors such as ALK-1, 2, 3 and 6, A 83-01 showed weak inhibition. Besides that, A 83-01 was proved to reduce the cell growth inhibition [1].
References:1. Tojo M, Hamashima Y, Hanyu A, et al. The ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-. Cancer science, 2005, 96(11): 791-800.

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