M4K2234，5MG，SML3569-5MG，Sigma

Biochem/physiol Actions

M4K2234 is a potent and selective TGF-β type I receptors ALK1/ACVRL1 & ALK2/ACVR1 inhibitor (IC50 = 7/14 nM, [ATP] = 10 mM) that inhibits TNIK and ALK6/BMPR1B only at higher concentrations (IC50 = 41 & 88 nM, respectively) with good kinome selectivity over >370 other kinases, including ALK3/BMPR1A, ALK4/ACVR1B, ALK5/TGFBR1 (IC50 = 0.165, 1.66, 1.95 μM, respectively). M4K2234 inhibits cellular phospho-SMAD1/5/8 induction by 10 ng/mL BMP-7 and phospho-SMAD2 induction by either 10 ng/mL activin A or 100 ng/mL TGF-β1 with good target selectivity by cellular NanoBRET assays (ALK1/2 IC50 = 83/13 nM).
Potent and selective TGF-β type I receptors ALK1/ACVRL1 & ALK2/ACVR1 inhibitor.