CPTH2 (hydrochloride) |
| Catalog No.GC14428 |
CPTH2(염산염)는 강력한 히스톤 아세틸트랜스퍼라제(HAT) 억제제입니다. CPTH2(염산염)는 Gcn5에 의한 히스톤 H3의 아세틸화를 선택적으로 억제합니다. CPTH2(염산염)는 아세틸트랜스퍼라제 p300(KAT3B)의 억제를 통해 세포 사멸을 유도하고 투명 세포 신암(ccRCC) 세포주의 침습성을 감소시킵니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2108899-91-6
Sample solution is provided at 25 µL, 10mM.
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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).
Average Rating: 5 (Based on Reviews and 14 reference(s) in Google Scholar.)
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