L002 是一种细胞可渗透的，可逆特定性乙酰转移酶p300(KAT3B)抑制剂，IC50为 1.98 μM。 它结合乙酰辅酶 A 口袋并竞争性抑制 FATp300 催化结构域，阻断组蛋白乙酰化和 p53 乙酰化，且抑制 STAT3 激活，有用于高血压引起的心脏肥大和纤维化的研究潜力。

L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation. L002 has the potential for hypertension‐induced cardiac hypertrophy and fibrogenesis treatment. L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM.

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 deacetylases, additional acetyltransferases, and methyltransferases.

L002 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.

321695-57-2

C15H15NO5S

321.35

DMSO:60 mg/mL (186.71 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years