L002

L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an IC₅₀ of 1.98 μM^[1]. L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation^[2]. L002 has the potential for hypertension-induced cardiac hypertrophy and fibrogenesis treatment^[3]. IC50 & Target: IC50: 1.98 uM (KAT3B); 35 μM (PCAF); 34 μM (GCN5)^[1] ;STAT3; p53^[2] In Vitro: L002 also has weak 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^[1]. In Vivo: L002 (intraperitoneal injection; 20 μg/gm body weight; every 3rd day; 2 weeks) reverses hypertension-induced cardiac hypertrophy and fibrosis by treatment of mice after inducing hypertension for two weeks significantly.It also reduces the levels of perivascular and interstitial collagen in the myocardium compared to non-treated hypertensive mice^[3].