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A TNKS2 inhibitor
CAY10753 is an inhibitor of tankyrase 2 (TNKS2; IC50 = 0.3 nM).1 It is selective for TNKS2 over TNKS1 (IC50 = 6.1 nM), as well as poly(ADP-ribose) polymerase 1 (PARP1) and PARP2 (IC50s = 89.6 and 37.8 nM, respectively). CAY10753 inhibits proliferation of DLD-1 colorectal cancer cells when used at a concentration of 1 µM.
1.Tomassi, S., Pfahler, J., Mautone, N., et al.From PARP1 to TNKS2 inhibition: A structure-based approachMed. Chem. Lett.(2020)
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