Description: L002, a potent, cell-permeable, reversible, and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 µM, directly binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain. By blocking histone acetylation, p53 acetylation, and STAT3 activation, L002 shows...

L002 is an inhibitor of p300 histone acetyltransferase (KAT3B, IC50 = 1.98 µM in vitro). 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...