| 产品介绍 |
L002 (NSC764414) is a novel selective, cell permeable and reversible inhibitor of p300 histone acetyl transferase (IC50 ~1.98 μM). It has no activity in histone methyltransferases tested, including DOT1, EZH1, G9a, PRMT1, SETD2, SET7-9, SMYD2, and SUV39H2 etc. L002 was shown to occupy Ac-CoA binding pocket of p300, and is less potent to CBP, PCAF, GCN5 and GNAT. It suppresses Histone H3 and H4 acetylation in triple negative breast cancer cell line MDAMB-468 as well as in HCT116 cell line and blocks p300-mediated STAT3 phosphorylation in pancreatic cancer cell line MIA Paca-2. L002 can suppress tumor growth and histone acetylation in a mouse MDA-MB-468 xenograft model.
基本信息：
CAS：321695-57-2
分子式：C15H15NO5S
分子量：321.35
纯度：≥98%
溶解性：溶于DMSO : 62.5 mg/mL (194.49 mM; Need ultrasonic)
性状：白色固体
产品简介：
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
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