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L002

CAS No. : 321695-57-2

MCE 国际站：L002

产品活性：L002 是一种有效的，细胞可渗透的，可逆的和特定的乙酰转移酶 p300(KAT3B) 抑制剂，IC₅₀ 为 1.98 μM。 L002 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。L002 有潜力用于高血压引起的心脏肥大和纤维化的研究。

研究领域：Epigenetics  |  Stem Cell/Wnt  |  JAK/STAT Signaling

作用靶点：Histone Acetyltransferase  |  STAT

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.

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.

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