| CAS: | 321695-57-2 | |||
| 分子式: | C15H15NO5S | |||
| 分子量: | 321.35 | |||
| 英文名称: |
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| 用途: | 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。 |
| 货号 | 品牌 | 产品名称 | 规格 | 包装、参考价格 | |||||||||||||||||||||||||||||
| L910608 | MACKLIN | L002(NSC764414) | 98% | 978元/5mg; 1672元/10mg; 3349元/25mg; 10852元/100mg; | 咨询 | ||||||||||||||||||||||||||||
储存：-20°C，密闭，干燥 | |||||||||||||||||||||||||||||||||
| SML0759 | Sigma-Aldrich | L002 | ≥98% (HPLC) | 1040.89元/5 MG; | 咨询 | ||||||||||||||||||||||||||||
产品说明 包装 5, 25 mg in glass bottle 生化/生理作用 L002 (NSC764414) is an inhibitor of acetyltransferase p300, a lysine acetyltransferase that catalyzes acetyl group attachment to lysine residues of a variety of proteins including histones and p53, and acts as a critical coactivator of several oncogenic transcription factors involved in cancer cell survival and proliferation including STAT3, NF-kB, and hypoxia-inducible factor-1α (HIF-1α). L002 (NSC764414) was discovered from compounds assayed for cytotoxicity to the triple-negative breast cancer (TNBC) cell line MDA-MB-231 but not to the human mammary epithelial cells, then further screened for inhibition of p300. L002 has an in vitro IC50 of 1.98 μM for p300 with lesser inhibition of the GNAT (GCN5-related N-acetyltransferase) family, and no inhibition against the MYST family of histone acetyltransferases (HATs), histone deacetylases (HDACs), or histone methyltransferases (HMTs). L002 potently suppressed tumor growth and histone acetylation of MDA-MB-468 xenografts and leukemia and lymphoma cell lines. 基本信息
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