CPTH2 (357649-93-5) is a selective inhibitor of the histone acetyltransferase Gcn5P both in vitro and in vivo (IC50 = 0.8 mM). In vitro, the HAT inhibitory activity of CPTH2 was caused via bridge-interaction with histone H3. It’s in vivo activity may involve more histonic and/or non-histonic Gcn5p substrates.
References/Citations:
1) Chimenti et al. (2009), A novel histone acetyltransferase inhibitor modulating Gcn5 network: cyclopentylidene-[4-(4′-chlorophenyl)thiazol-2-yl]hydrazone); J. Med .Chem., 52 530
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