357649-93-5 Usage
Description
CPTH2 (357649-93-5) is a selective inhibitor of the histone acetyltransferase Gcn5P both?in vitro?and?in vivo?(IC50?= 0.8 mM).?In vitro, the HAT inhibitory activity of CPTH2 was caused via bridge-interaction with histone H3. It’s?in vivo?activity may involve more histonic and/or non-histonic Gcn5p substrates.
Uses
Different sources of media describe the Uses of 357649-93-5 differently. You can refer to the following data:
1. CPTH2 is a histone acetyltransferase inhibitor that modulates Gcn5p dependent functional network in vitro and in vivo.
2. Histone acetylation plays an important role in regulating the chromatin structure and is tightly regulated by two classes of enzyme, histone acetyltransferases (HAT) and histone deacetylases (HDAC). Deregulated HAT and HDAC activity plays a role in the development of a range of cancers. Consequently, inhibitors of these enzymes have potential as anticancer agents.
3. CPTH2 has been used for the inhibition of histone acetyltransferase in cortical cultures, bud cells and natural killer T cells (iNKT).
General Description
CPTH2 ((3-methylcyclopentylidene-[4-(4′-chlorophenyl)thiazol-2-yl]hydrazone)) inhibits histone acetyltransferase functionality and reduces acetylation of histone H3 and H4. CPTH2 promotes apoptosis in lymphoma cell lines. It may serve as an anticancer agent. CPTH2 inhibits α-tubulin acetylation and modulates autophagic pathway in human acute myeloid leukemia cell lines.
Biochem/physiol Actions
CPTH2 is a histone acetyltransferase (HAT) inhibitor modulating the Gcn5 network. Histone Acetyltransferase (HAT) inhibitor modulating Gcn5 network. Histone acetyltransferases (HATs) act as transcriptional coactivators. Histone acetylation plays an important role in regulating the chromatin structure and is tightly regulated by two classes of enzyme, histone acetyltransferases (HAT) and histone deacetylases (HDAC). Deregulated HAT and HDAC activity plays a role in the development of a range of cancers. Consequently, inhibitors of these enzymes have potential as anticancer agents.
References
1) Chimenti?et al. (2009),?A novel histone acetyltransferase inhibitor modulating Gcn5 network: cyclopentylidene-[4-(4′-chlorophenyl)thiazol-2-yl]hydrazone); J. Med .Chem.,?52?530
Check Digit Verification of cas no
The CAS Registry Mumber 357649-93-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 3,5,7,6,4 and 9 respectively; the second part has 2 digits, 9 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 357649-93:
(8*3)+(7*5)+(6*7)+(5*6)+(4*4)+(3*9)+(2*9)+(1*3)=195
195 % 10 = 5
So 357649-93-5 is a valid CAS Registry Number.
357649-93-5Relevant articles and documents
Application of alicyclic ketone hydrazone thiazole derivative serving as tyrosinase inhibitor
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Paragraph 0010; 0011, (2018/09/11)
The invention discloses an alicyclic ketone hydrazone thiazole derivative having tyrosinase inhibiting activity. Screening results of in-vitro inhibition tyrosinase show that the synthesized derivative has the tyrosinase inhibiting activity. The compound
Synthesis and in vitro activity of 2-thiazolylhydrazone derivatives compared with the activity of clotrimazole against clinical isolates of Candida spp.
Chimenti, Franco,Bizzarri, Bruna,Maccioni, Elias,Secci, Daniela,Bolasco, Adriana,Fioravanti, Rossella,Chimenti, Paola,Granese, Arianna,Carradori, Simone,Rivanera, Daniela,Lilli, Daniela,Zicari, Alessandra,Distinto, Simona
, p. 4635 - 4640 (2008/12/20)
In this paper, we report on the synthesis of a novel series of 2-thiazolylhydrazone derivatives and the influence of the substituents on the thiazole ring on antifungal activity. All synthesized compounds were screened for their in vitro activities agains
