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。
| Cas No. | 357649-93-5 |
| Canonical SMILES | ClC1=CC=C(C2=CSC(N/N=C3CCCC/3)=N2)C=C1 |
| 分子式 | C14H14ClN3S |
| 分子量 | 291.8 |
| 溶解度 | DMSO: 25 mg/mL (85.68 mM); Water:< 0.1 mg/mL (insoluble) |
| 储存条件 | 4°C, protect from light |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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. |
