Chemical Structure : ALKBH2 inhibitor AH2-15c
CAS No.:
ALKBH2 inhibitor AH2-15c
Catalog No.: PC-23546Not For Human Use, Lab Use Only.
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.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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).
Physicochemical Properties
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M.Wt
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378.43
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Formula
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C21H22N4O3
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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1-(5-((2,2-dimethyl-1-phenylpropyl)carbamoyl)pyridin-2-yl)-1H-pyrazole-4-carboxylic acid
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References
1. Xu K, et al. Eur J Med Chem. 2024 Nov 14;282:117054.
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