PARP/EZH2-IN-2 

PARP/EZH2-IN-2 (compound 12e) is a dual target PARP1 and EZH2 inhibitor, with IC₅₀ values of 6.89 and 27.34 nM, respectively. PARP/EZH2-IN-2 shows anticancer activity, with no toxicity to normal cells. PARP/EZH2-IN-2 achieves synthetic lethality indirectly by inhibiting EZH2 to increase the sensitivity to PARP1, and induces cell death by regulating excessive autophagy^[1].

PARP/EZH2-IN-2 (compound 12e) shows an optimal cytotoxicity against MDA-MB-231 cells (IC₅₀=2.84 μM) and BT-549 cells (IC₅₀=0.91 μM), with no toxicity on normal breast cell lines^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PARP/EZH2-IN-2 (compound 12e) (20-50 mg/kg, IP) exhibits good antitumor activity, more effective than Niraparib (HY-10619) plus GSK126 (HY-13470)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

573.64

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• [1]. Li X, et al. Dual target PARP1/EZH2 inhibitors inducing excessive autophagy and producing synthetic lethality for triple-negative breast cancer therapy. Eur J Med Chem. 2023 Dec 17;265:116054.  [Content Brief]