L-002 (NSC 764414, L002) is a novel potent, specific acetyltransferase p300 (KAT3B) inhibitor with IC50 of 1.98 uM.
L-002 also shows weak inhibitory activity against PCAF (KAT2B) and GCN5 (KAT2A) with IC50 of 34.7 and 33.9 uM, displays no inhibition against Tip60, MYST2 and MYST4 (IC50>100 uM), as well as a panel of HDACs and HMTs.
L-002 inhibits acetylation of histones and p53, and suppresses STAT3 activation in cell-based assays.
L-002 exhibits extreme sensitivity against leukemia, breas and lymphoma cell lines; potently suppresses tumor growth and histone acetylation of MDA-MB-468 xenografts.
