CB-6644 is an inhibitor of the RUVBL1/2 complex, a complex with ATPase activity that regulates several cellular processes, including chromatin remodeling and gene expression.1 It inhibits the ATPase activity of the RUVBL1/2 complex (IC50 = 15 nM) and is selective for the RUVBL1/2 complex over a panel of 224 ATPases at 10 ?M. CB-6644 reduces viability in a panel of cancer cell lines with EC50 values ranging from 41 to 785 nM. It induces apoptosis in HCT116 colon cancer cells when used at a concentration of 0.4 ?M. CB-6644 (150 mg/kg) reduces tumor growth in Ramos Burkitt’s lymphoma and RPMI-8226 multiple myeloma xenograft mouse models.
1.Assimon, V.A., Tang, Y., Vargas, J.D., et al.CB-6644 is a selective inhibitor of the RUVBL1/2 complex with anticancer activityACS Chem Biol.14(2)236-244(2019)