M4K2234 | ALK1/2 inhibitor | Probechem Biochemicals

Chemical Structure : M4K2234

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M4K2234 (ALK1/2 inhibitor)

货号: PC-72014Not For Human Use, Lab Use Only.

M4K2234 is a potent, selective ALK1 (ACVRL1) and ALK2 (ACVR1) protein kinase inhibitor with IC50 of 7 and 14 nM, respectively.

规格	价格	库存	数量
10 mg		Get quote
25 mg		Get quote
100 mg		Get quote

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生物&药学活性

M4K2234 is a potent, selective ALK1 (ACVRL1) and ALK2 (ACVR1) protein kinase inhibitor with IC50 of 7 and 14 nM, respectively.
M4K2234 inhibits only ALK1/2 and one additional off target (TNIK) by kinome-wide screening against 375 protein kinases at 1 uM.
M4K2234 demonstrated in cell based target engagement assays with an IC50 of 83nM for ALK1 and 13 nM for ALK2.
M4K2234 exhibits only very weak potency against ALK4/5.
M4K2234 affects phosphorylation of SMAD1/5/8 that corresponds to BMP branch of signalling which is mediated, besides others, also by ALK1/2 kinases.
M4K2234 has only a very weak effect on SMAD2/3 phosphorylation that corresponds to TGF beta branch of signalling which is mediated mostly via ALK4/5/7.

物理化学性质&存储条件

分子量	462.57
分子式	C27H31FN4O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	Benzamide, 2-fluoro-6-methoxy-4-[4-methyl-5-[4-[4-(1-methylethyl)-1-piperazinyl]phenyl]-3-pyridinyl]-

参考文献

1. Ensan D, et al. J Med Chem. 2020 May 14;63(9):4978-4996.