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CPTH2(hydrochloride)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CPTH2(hydrochloride)图片
CAS NO:2108899-91-6
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍
CPTH2 (hydrochloride) 是一种有效的组蛋白乙酰转移酶 (HAT) 抑制剂。 CPTH2(盐酸盐)选择性地抑制 Gcn5 对组蛋白 H3 的乙酰化。 CPTH2(盐酸盐)通过抑制乙酰转移酶 p300 (KAT3B) 诱导细胞凋亡并降低透明细胞肾癌 (ccRCC) 细胞系的侵袭性。
Cas No.2108899-91-6
化学名2-[4-(4-chlorophenyl)-2-thiazolyl]hydrazone-cyclopentanone, monohydrochloride
Canonical SMILESClC(C=C1)=CC=C1C2=CSC(N/N=C3CCCC\3)=N2.Cl
分子式C14H14ClN3S o HCl
分子量328.3
溶解度≤5mg/ml in ethanol;16mg/ml in DMSO;5mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

CPTH2 is an inhibitor of HAT activity of Gcn5.

Histone acetyltransferases (HATs) has been identified to add the acetyl group on the specific lysine of histone H3 and H4 N-termini, and such signatures are able to increase the accessibility of the underlying chromatin at specific genes or over vast regions of the genome. Gcn5p is a chimeric protein made up of a number of functional domains.

In vitro: Previous study identified a novel molecule named CPTH2, which was selected based on its inhibitory effect on the growth of a gcn5Delta strain. This study indicated a specific chemical-genetic interaction between CPTH2 and HAT Gcn5p, suggesting that CPTH2 could inhibit the dependent functional network of Gcn5p. In addition, CPTH2 was found to be able to inhibit an in-vitro HAT reaction, which could be reverted by increasing concentration of histone H3 [1].

In vivo: In vivo, CPTH2 could decrease the acetylation of bulk histone H3 at the specific H3-AcK14 site [1].

Clinical trial: Up to now, CPTH2 is still in the preclinical development stage.

Reference:
[1] F.  Chimenti, B. Bizzarri, E. Maccioni, et al. A novel histone acetyltransferase inhibitor modulating Gcn5 network: Cyclopentylidene-[4-(4'-chlorophenyl)thiazol-2-yl)hydrazone. Journal of Medicinal Chemistry 52, 530-536 (2009).