ALKBH2 inhibitor AH2-15c

Chemical Structure : ALKBH2 inhibitor AH2-15c

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货号: PC-23546Not For Human Use, Lab Use Only.

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50 mg		Get quote
100 mg		Get quote
250 mg		Get quote

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生物&药学活性

ALKBH2 inhibitor AH2-15c is a potent and selective inhibitor of 2OG-dependent DNA demethylase AlkB homolog 2 (ALKBH2) with IC50 of 31 nM in fluorescence polarization (FP) assays, >200-fold selectivity over other AlkB subfamily members.
AH2-15c shows high affinity with ITC KD value of 226 nM.
AH2-15c could inhibit the demethylation of ALKBH2 with an IC50 value of 1.48 ± 0.045 μM in the presence of 300 μM α-KG in methylation-sensitive restriction enzyme digestion assay.
AH2-15c does not inhibit the demethylase activities of ALKBH1, ALKBH3, ALKBH5 and FTO, with IC50 values of >200 μM.
AH2-15c is a very weak inhibitory effect on U87 cells with an IC50 value of 103 uM, becuase of the poor cell membrane permeability.
AH2-15c directly binds to ALKBH2 and increases the levels of DNA 3meC in cells (5 uM).

物理化学性质&存储条件

分子量	378.43
分子式	C21H22N4O3
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	1-(5-((2,2-dimethyl-1-phenylpropyl)carbamoyl)pyridin-2-yl)-1H-pyrazole-4-carboxylic acid

参考文献

1. Xu K, et al. Eur J Med Chem. 2024 Nov 14;282:117054.