Catalog No.: PC-72165Not For Human Use, Lab Use Only.
CPI-1612 (CPI 1612) is a highly potent, selective, orally bioavailable EP300/CBP histone acetyltransferase inhibitor with IC50 of 8.1 nM (EP300 HAT SPA).
CPI-1612 (CPI 1612) is a highly potent, selective, orally bioavailable EP300/CBP histone acetyltransferase inhibitor with IC50 of 8.1 nM (EP300 HAT SPA).
CPI-1612 displays no inhibitory activity in a panel of seven HAT targets (Tip60, HAT1, PCAF, MYST2, MYST3, MYST4, and GCN5L2) and had minimal activity against the antitargets in the Eurofins Safety44 off-target screening panel.
CPI-1612 inhibits JEKO-1 cell growth with GI50 of <7.9 nM, and H3K18Ac MSD EC50 of 14 nM.
CPI-1612 reduced the histone acetylation H3K18Ac in vivo at the primary chromatin acetylation targets of EP300/CBP in a dose- and time-dependent manner.
CPI-1612 showed 67% tumor growth inhibition (TGI) at a dose of 0.5 mg/kg PO BID with concomitant reduction of H3K27Ac in plasma and reduction of H3K18Ac in the tumor.
