A1874

2064292-12-0

C58H62Cl3F2N9O7S

H2O : < 0.1 mg/mL (insoluble); DMSO : 150 mg/mL (127.81 mM; Need ultrasonic)

Epigenetics; PROTAC

A1874 is a nutlin-based and BRD4-degrading PROTAC with a DC₅₀ of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation^[1]. IC50 & Target: DC50: 32 nM (induce BRD4 degradation in cells)^[1]. In Vitro: Treatment of HCT116 cells of A1874 (0-10 uM, 24 hours) induces a dose-dependent knockdown of BRD4 levels, with near-maximum knockdown by 100 nmol/L and a maximum degradation (Dmax) of BRD4 of 98% of the levels in control (0.1% DMSO-treated) cells^[1].
Treatment of HCT116 cells of A1874 (0-10 uM, 24 hours) increases p53 levels in the HCT116 cells and showed dose-dependent p53 stabilization^[1].