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| Histone Acetyltransferase Inhibitor IV, CPTH2 Basic information |
| Histone Acetyltransferase Inhibitor IV, CPTH2 Chemical Properties |
| Melting point | 190-191 °C | | Boiling point | 460.3±37.0 °C(Predicted) | | density | 1.38±0.1 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | Soluble in DMSO | | form | powder | | pka | 14.57±0.20(Predicted) | | color | white to beige | | Sensitive | Light Sensitive | | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month. |
| Histone Acetyltransferase Inhibitor IV, CPTH2 Usage And Synthesis |
| 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 | CPTH2 is a histone acetyltransferase inhibitor that modulates Gcn5p dependent functional network in vitro and in vivo. | | Uses | 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. | | Uses | 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 |
| Histone Acetyltransferase Inhibitor IV, CPTH2 Preparation Products And Raw materials |
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