L002

L002 is an inhibitor of p300 histone acetyltransferase (KAT3B; IC₅₀ = 1.98 µM in vitro).¹ It has weaker inhibitory effects against PCAF and GCN5 (IC₅₀s = 35 and 34 µM, respectively) and is specific for p300 over a panel of additional acetyltransferases, deacetylases, and methyltransferases. L002 blocks acetylation of histones and p53 in cells treated with trichostatin A or etoposide, respectively, and reduces STAT3 phosphorylation, which requires p300-mediated acetylation of STAT3.¹ It induces growth arrest and apoptosis in certain cancer cell lines and, when administered intraperitoneally in mice, suppresses the growth of triple-negative breast cancer xenografts.¹

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1. Yang, H., Pinello, C.E., Luo, J., et al. Small-molecule inhibitors of acetyltransferase p300 identified by high-throughput screening are potent anticancer agents. Mol. Cancer Ther. 12(5), 610-620 (2013).

Kanada, F., Takamura, Y., Miyake, S., et al. Histone acetyltransferase and Polo-like kinase 3 inhibitors prevent rat galactose-induced cataract. Sci. Rep. 9(1), 20085 (2019).