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ALKBH2 inhibitor AH2-15c

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

M.Wt 378.43
Formula C21H22N4O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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

References

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

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