ALKBH1-IN-1 (Compound 13h) is a selective ALKBH1 inhibitor, with an IC50 of 0.026 μM and 1.39 μM in the fluorescence polarization and enzyme activity assay, respectively. ALKBH1-IN-1 can modulate the level of DNA 6mA modifications. ALKBH1-IN-1 can be used to study the functions of ALKBH1 and DNA 6mA.
ALKBH1-IN-1 (3 μM, 48 h) stabilizes the ALKBH1 protein in U251 cells overexpressed with ALKBH1[1].ALKBH1-IN-1 (10 μM, 48 h) increases the amount of 6mA in DNA in U251 cells[1].
References:
[1]. Xiong L, et al. Discovery of a Potent and Cell-Active Inhibitor of DNA 6mA Demetlase ALKBH1. J Am Chem Soc. 2024 Mar 13;146(10):6992-7006.