产品介绍
Product Description
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.
技术参数
Specifications
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | 2-8°C |
| SMILES string | CC(C)N(CC1)CCN1C2=CC=C(C3=C(C)C(Cl)=CN=C3)C=C2 |
| InChI | 1S/C19H24ClN3/c1-14(2)22-8-10-23(11-9-22)17-6-4-16(5-7-17)18-12-21-13-19(20)15(18)3/h4-7,12-14H,8-11H2,1-3H3 |
| InChI key | UFAWMCANSWTKEG-UHFFFAOYSA-N |
