CPTH2 是有效的组蛋白乙酰基转移酶 (HAT) 抑制剂，可通过底物竞争方式抑制重组人 Gcn5 对组蛋白 H3 的乙酰化。CPTH2 通过抑制乙酰转移酶 p300 (KAT3B) 诱导凋亡 (apoptosis) 并降低透明细胞肾癌 (ccRCC) 细胞系的侵袭性。
货号:ajcx16492
CAS:357649-93-5
分子式:C14H14ClN3S
分子量：291.8
溶解度:DMSO: 25 mg/mL (85.68 mM); H2O:< 0.1 mg/mL (insoluble)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

CPTH2 is a potent histone acetyltransferase (HAT) inhibitor and selectively inhibits the acetylation of histone H3 by recombinant human Gcn5 in a substrate-competive manner. CPTH2 induces apoptosis and decreases the invasiveness of a clear cell renal carcinoma (ccRCC) cell line through the inhibition of acetyltransferase p300 (KAT3B)[1][2].

[1]. Cocco E, et al. KAT3B-p300 and H3AcK18/H3AcK14 levels are prognostic markers for kidney ccRCC tumoraggressiveness and target of KAT inhibitor CPTH2. Clin Epigenetics. 2018 Apr 4;10:44. [2]. Chimenti F, et al. A novel histone acetyltransferase inhibitor modulating Gcn5 network: cyclopentylidene-[4-(4'-chlorophenyl)thiazol-2-yl)hydrazone. J Med Chem. 2009 Jan 22;52(2):530-6.