CZL-105

CZL-105 potently inhibits purified human p300 bromodomain with an IC₅₀ of 11.8 nM^[1].
CZL-105 (up to 1 μM) potently inhibits purified human p300 and CBP bromodomains with IC₅₀ values of 0.09 μM and 0.08 μM, respectively, and shows no activity against BET bromodomains at concentrations up to 1 μM^[1].
CZL-105 (200 μM; 30 min) is a selective binder to purified human p300 and CBP bromodomains, with ΔT_m values of 15.25 °C and 14.5 °C respectively, and does not stabilize other tested non-BET bromodomains^[1].
CZL-105 (1 μM; 0, 7, 17, 30, 60 min) has favorable metabolic stability in mouse liver microsomes, with a half-life of 88.5 min^[1].
CZL-105 (gradient concentrations; 6 days) potently inhibits the proliferation of OPM-2 multiple myeloma cells with an IC₅₀ of 57 nM^[1].
CZL-105 (250-500 nM; 3 days) induces G₀/G₁ phase arrest in OPM-2 multiple myeloma cells in a dose-dependent manner after 3 days of treatment^[1].
CZL-105 (250-500 nM; 1-3 days) induces apoptosis in OPM-2 multiple myeloma cells in both time- and dose-dependent manners, as evidenced by flow cytometry and activation of apoptosis-related proteins^[1].
CZL-105 (3 days) increases lipid ROS levels in OPM-2 multiple myeloma cells in a dose-dependent manner, but cell death induced by CZL-105 is not primarily mediated by the canonical ferroptosis pathway^[1].

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