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CPTH2 (hydrochloride)

Catalog No.
C3208
inhibitor of HAT activity of Gcn5
Grouped product items
SizePriceStock Qty
5mg
$110.00
Ship with 5-10 days
10mg
$143.00
Ship with 5-10 days

Tel: +1-832-696-8203

Email: [email protected]

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Background

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).

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt328.3
FormulaC14H14ClN3S·HCl
Solubility≤5mg/ml in ethanol;16mg/ml in DMSO;5mg/ml in dimethyl formamide
Chemical Name2-[4-(4-chlorophenyl)-2-thiazolyl]hydrazone-cyclopentanone, monohydrochloride
SDFDownload SDF
Canonical SMILESClC(C=C1)=CC=C1C2=CSC(N/N=C3CCCC\3)=N2.Cl
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

CPTH2 (hydrochloride)