Histone Acetyltransferase Inhibitor IV, CPTH2

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.

The Uses of Histone Acetyltransferase Inhibitor IV, CPTH2

CPTH2 is a histone acetyltransferase inhibitor that modulates Gcn5p dependent functional network in vitro and in vivo.

The Uses of Histone Acetyltransferase Inhibitor IV, CPTH2

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.

The Uses of Histone Acetyltransferase Inhibitor IV, CPTH2

CPTH2 has been used for the inhibition of histone acetyltransferase in cortical cultures, bud cells and natural killer T cells (iNKT).

Definition

ChEBI: Cyclopentylidene-[4-(4-chlorophenyl)thiazol-2-yl]hydrazone is a member of the class of 1,3-thiazole bearing 2-cyclopentylidenehydrazino and 4-chlorophenyl substituents at positions 2 and 4 respectively. It has a role as an EC 2.3.1.48 (histone acetyltransferase) inhibitor. It is a member of 1,3-thiazoles, a hydrazone and a member of monochlorobenzenes.

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