ChemicalBook > CAS DataBase List > Histone Acetyltransferase Inhibitor IV, CPTH2

Histone Acetyltransferase Inhibitor IV, CPTH2

Product Name
Histone Acetyltransferase Inhibitor IV, CPTH2
CAS No.
357649-93-5
Chemical Name
Histone Acetyltransferase Inhibitor IV, CPTH2
Synonyms
CPTH2;Histone Acetyltransferase Inhibitor IV, CPTH2;Cyclopentylidene-[4-(4-chlorophenyl)thiazol-2-yl)hydrazone;Cyclopentanone, 2-[4-(4-chlorophenyl)-2-thiazolyl]hydrazone;4-(4-Chlorophenyl)-2-(2-cyclopentylidenehydrazinyl)thiazole;4-(4-Chlorophenyl)-2-(2-cyclopentylidenehydrazineyl)thiazole;4-(4-Chlorophenyl)-2-(2-cyclopentylidenehydrazineyl)thiazole , CPTH2
CBNumber
CB22602855
Molecular Formula
C14H14ClN3S
Formula Weight
291.8
MOL File
357649-93-5.mol
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Histone Acetyltransferase Inhibitor IV, CPTH2 Property

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
Water Solubility 
Water: < 0.1 mg/mL (insoluble)
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.
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Safety

WGK Germany 
nwg
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
C9873
Product name
CPTH2
Purity
≥98% (HPLC), powder
Packaging
5mg
Price
$174
Updated
2024/03/01
Sigma-Aldrich
Product number
382111
Product name
Histone Acetyltransferase Inhibitor IV, CPTH2
Packaging
10mg
Price
$187
Updated
2024/03/01
Alfa Aesar
Product number
J65939
Product name
Histone Acetyltransferase Inhibitor IV, CPTH2
Packaging
5mg
Price
$88.5
Updated
2023/06/20
Alfa Aesar
Product number
J65939
Product name
Histone Acetyltransferase Inhibitor IV, CPTH2
Packaging
10mg
Price
$140
Updated
2023/06/20
Sigma-Aldrich
Product number
C9873
Product name
CPTH2
Purity
≥98% (HPLC), powder
Packaging
25mg
Price
$699
Updated
2024/03/01
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Histone Acetyltransferase Inhibitor IV, CPTH2 Chemical Properties,Usage,Production

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).

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

Histone Acetyltransferase Inhibitor IV, CPTH2 Preparation Products And Raw materials

Raw materials

Preparation Products

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357649-93-5, Histone Acetyltransferase Inhibitor IV, CPTH2Related Search:


  • Histone Acetyltransferase Inhibitor IV, CPTH2
  • CPTH2
  • Cyclopentylidene-[4-(4-chlorophenyl)thiazol-2-yl)hydrazone
  • Cyclopentanone, 2-[4-(4-chlorophenyl)-2-thiazolyl]hydrazone
  • 4-(4-Chlorophenyl)-2-(2-cyclopentylidenehydrazineyl)thiazole
  • 4-(4-Chlorophenyl)-2-(2-cyclopentylidenehydrazinyl)thiazole
  • 4-(4-Chlorophenyl)-2-(2-cyclopentylidenehydrazineyl)thiazole , CPTH2
  • 357649-93-5
  • HAT Inhibitor IV, Gcn5p Inhibitor, CPTH2
  • Aromatics, Heterocycles, Inhibitors, Pharmaceuticals, Intermediates & Fine Chemicals