RECQL5-IN-1 (Compound 4a) acts as an orally effective RECQL5 inhibitor (targeting both enzymatic and nonenzymatic domain). RECQL5-IN-1 is a potent inhibitor of RECQL5 helicase activity (IC50=46.3 nM). RECQL5-IN-1 inhibits RECQL5-WT cells and RECQL5-KO2 cells with IC50s of 4.8 μM and 19.6 μM, respectively. RECQL5-IN-1 can be used for the research of breast cancer[1].
[1]. Saikat Chakraborty, et al. Targeting RECQL5 Functions, by a Small Molecule, Selectively Kills Breast Cancer in Vitr o and in Vivo. J Med Chem. 2021 Feb 11;64(3):1524-1544.
