H3B-968 is a potent inhibitor of Werner syndrome protein (WRN) (IC50=~10 nM), which acts function as helicase, ATPase, and exonuclease. WRN exhibits synthetic lethal activity in cancer research. However, H3B-968 inhibits WRN helicase activity, competitively with ATP[1].
References:
[1]. Parker MJ, et al. Identification of 2-Sulfonyl/Sulfonamide Pyrimidines as Covalent Inhibitors of WRN Using a Multiplexed High-Throughput Screening Assay. Biochemistry. 2023 Jul 18;62(14):2147-2160.
















