NEO2734 (EP31670) is an orally active dual p300/CBP and BET bromodomain selective inhibitor, with IC50 values of <30 nM for both p300/CBP and BET bromodomains[1]. NEO2734 is active in SPOP mutant and wild-type prostate cancer[2].
NEO2734 (1 μM) induces differentiation and G1-phase cell cycle arrest[1].
NEO2734 (1 μM) rapidly induces squamous differentiation in NMC cell lines, and expression of the terminal squamous differentiation marker, involucrin, or keratins[1].
NEO2734 is active in both hotspot mutant (F133V) and non-hotspot mutant (Q165P) PCa cells in vitro and in vivo[2].
Reference:
[1]. Chevaun D Morrison-Smit, et al. Combined Targeting of the BRD4-NUT-p300 Axis in NUT Midline Carcinoma by Dual Selective Bromodomain Inhibitor, NEO2734. Mol Cancer Ther. 2020 Jul;19(7):1406-1414.
[2]. Yuqian Yan, et al. The novel BET-CBP/p300 dual inhibitor NEO2734 is active in SPOP mutant and wild-type prostate cancer. EMBO Mol Med. 2019 Nov 7;11(11):e10659.