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CPTH2 (hydrochloride)

Catalog No.GC14428

inhibitor of HAT activity of Gcn5

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CPTH2 (hydrochloride) Chemical Structure

Cas No.: 2108899-91-6

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5mg
$136.00
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10mg
$179.00
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Sample solution is provided at 25 µL, 10mM.

Description of CPTH2 (hydrochloride)

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 of CPTH2 (hydrochloride)

Cas No. 2108899-91-6 SDF
Chemical Name 2-[4-(4-chlorophenyl)-2-thiazolyl]hydrazone-cyclopentanone, monohydrochloride
Canonical SMILES ClC(C=C1)=CC=C1C2=CSC(N/N=C3CCCC\3)=N2.Cl
Formula C14H14ClN3S • HCl M.Wt 328.3
Solubility ≤5mg/ml in ethanol;16mg/ml in DMSO;5mg/ml in dimethyl formamide Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of CPTH2 (hydrochloride)

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1 mg 5 mg 10 mg
1 mM 3.046 mL 15.23 mL 30.4599 mL
5 mM 0.6092 mL 3.046 mL 6.092 mL
10 mM 0.3046 mL 1.523 mL 3.046 mL
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