DATASHEET
Formulation
Powder
Storage:
Store in dry, dark place at -20C for 1 year.
Product Information:
Molecular Weight: 343.42
Formula: C21 H21 N5
CAS Number: 356559-20-1
InChi Key: DKPQHFZUICCZHF-UHFFFAOYSA-N
InChi: InChI=1S/C21H21N5/c1-13-6-5-7-16(24-13)19-18(25-20(26-19)21(2,3)4)14-8-9-15-17(12-14)23-11-10-22-15/h5-12H,1-4H3,(H,25,26)
Smiles: CC1=CC=CC(=N1)C1NC(=NC=1C1C=C2N=CC=NC2=CC=1)C(C)(C)C
Purity: 98.0
Solubility: Soluble in DMSO, not in water
Appearance: Solid Power.
Shelf Life: 1.0 years
Description:
SB525334 is a potent and selective inhibitor of the transforming growth factor-beta1 (TGF-beta1) receptor, activin receptor-like kinase (ALK5). SB525334 inhibited ALK5 kinase activity with an IC(50) of 14.3 nM and was approximately 4-fold less potent as an inhibitor of ALK4 (IC(50) = 58.5 nM). SB-525334 was inactive as an inhibitor of ALK2, ALK3, and ALK6 (IC(50) > 10,000 nM). In cell-based assays, SB-525334 (1 microM) blocked TGF-beta1-induced phosphorylation and nuclear translocation of Smad2/3 in renal proximal tubule cells and inhibited TGF-beta1-induced increases in plasminogen activator inhibitor-1 (PAI-1) and procollagen alpha1(I) mRNA expression in A498 renal epithelial carcinoma cells.