| CPTH2 (hydrochloride)inhibitor of HAT activity of Gcn5 |
Sample solution is provided at 25 µL, 10mM.
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| Cas No. | N/A | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | 2-[4-(4-chlorophenyl)-2-thiazolyl]hydrazone-cyclopentanone, monohydrochloride | ||
| Canonical SMILES | ClC(C=C1)=CC=C1C2=CSC(N/N=C3CCCC3)=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 |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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).
