Histone Acetyltransferase Inhibitor IV, CPTH2 Struktur

Histone Acetyltransferase Inhibitor IV, CPTH2

Bezeichnung:Histone Acetyltransferase Inhibitor IV, CPTH2

CAS-Nr357649-93-5

Englisch Name:Histone Acetyltransferase Inhibitor IV, CPTH2

CBNumberCB22602855

SummenformelC14H14ClN3S

Molgewicht291.8

MOL-Datei357649-93-5.mol

Histone Acetyltransferase Inhibitor IV, CPTH2 physikalisch-chemischer Eigenschaften

Schmelzpunkt	190-191 °C
Siedepunkt	460.3±37.0 °C(Predicted)
Dichte	1.38±0.1 g/cm3(Predicted)
storage temp.	2-8°C
Löslichkeit	Soluble in DMSO
Aggregatzustand	powder
pka	14.57±0.20(Predicted)
Farbe	white to beige
Wasserlöslichkeit	Water: < 0.1 mg/mL (insoluble)
Sensitive	Light Sensitive
Stabilität	Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.

Sicherheit

WGK Germany

nwg

Histone Acetyltransferase Inhibitor IV, CPTH2 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
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.
Verwenden
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.
Verwenden
CPTH2 has been used for the inhibition of histone acetyltransferase in cortical cultures, bud cells and natural killer T cells (iNKT).
Verwenden
CPTH2 is a histone acetyltransferase inhibitor that modulates Gcn5p dependent functional network in vitro and in vivo.
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.
Allgemeine Beschreibung
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.
Einzelnachweise
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 Upstream-Materialien And Downstream Produkte

Histone Acetyltransferase Inhibitor IV, CPTH2 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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