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Chemical Structure : CPI-1612
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).
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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.
| M.Wt | 450.546 | |
| Formula | C27H26N6O | |
| Appearance | Solid | |
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1. Jonathan E Wilson, et al. ACS Med Chem Lett. 2020 Apr 23;11(6):1324-1329.
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