Lys-CoA TFA is a selective p300 histone acetyltransferase (HAT) inhibitor (IC50=50-500 nM). Lys-CoA TFA displays >100-fold selectivity for p300 over PCAF (IC50=200 μM). Lys-CoA TFA inhibits p300 HAT activity-dependent transcriptional activation[1][2].
Lys-CoA TFA (0.1 and 1 mM; 60 hours) induces a senescent phenotype in human normal melanocytes[3].
Cell Proliferation Assay[3]
| Cell Line: | Normal human melanocytes |
| Concentration: | 0.1 and 1 mM |
| Incubation Time: | 60 hours |
| Result: | Almost completely abolished proliferation, induced high levels of SA-β-Gal, and inhibited cyclin E expression in a dose-dependent manner. |
[1]. Cebrat M, et al. Synthesis and analysis of potential prodrugs of coenzyme A analogues for the inhibition of the histone acetyltransferase p300. Bioorg Med Chem. 2003;11(15):3307-3313.
[2]. Lau OD, et al. HATs off: selective synthetic inhibitors of the histone acetyltransferases p300 and PCAF. Mol Cell. 2000;5(3):589-595.