ALK5 Inhibitor I [3-(Pyridin-2-yl)-4-(4-quinonyl)]-1H-pyrazole TbR-I Inhibitor Transforming Growth Factor-b Type I Receptor Kinase Inhibitor Brown solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable diheteroaryl-substituted pyrazole compound that acts as a potent, selective, ATP-competitive inhibitor of TGF-b Receptor I kinase (IC50 = 51 nM). Displays ~15-fold greater selectivity over p38a MAP kinase (IC50 = 740 nM). Shown to inhibit TGF-b-dependent cellular growth (IC50 = 89 nM in NIH 3T3 mouse fibroblasts) and transcription activation (IC50 = 47 nM in mink lung cells). Purity: ≥97% by HPLC. CAS 396129-53-6. Ref.: Sawyer, J.S., et al. 2003. J. Med. Chem. 46, 3953. Singh, J., et al. 2003. Bioorg. Med. Chem. Lett. 13, 4355. |