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;CPTH2 ，S1242;CPTH2, 10 mM in DMSO;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
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.
- InChI
- InChI=1S/C14H14ClN3S/c15-11-7-5-10(6-8-11)13-9-19-14(16-13)18-17-12-3-1-2-4-12/h5-9H,1-4H2,(H,16,18)
- InChIKey
- YYTHPXHGWSAKIZ-UHFFFAOYSA-N
- SMILES
- C1(=N/NC2=NC(C3=CC=C(Cl)C=C3)=CS2)/CCCC/1
Safety
- WGK Germany
- nwg
- Storage Class
- 11 - Combustible Solids
N-Bromosuccinimide Price
- Product number
- C9873
- Product name
- CPTH2
- Purity
- ≥98% (HPLC), powder
- Packaging
- 5mg
- Price
- $192
- Updated
- 2026/04/30
- Product number
- 382111
- Product name
- Histone Acetyltransferase Inhibitor IV, CPTH2
- Packaging
- 10mg
- Price
- $175
- Updated
- 2026/04/30
- Product number
- C9873
- Product name
- CPTH2
- Purity
- ≥98% (HPLC), powder
- Packaging
- 25mg
- Price
- $771
- Updated
- 2026/04/30
- Product number
- 007099
- Product name
- CPTH2
- Packaging
- 25mg
- Price
- $460
- Updated
- 2021/12/16
- Product number
- C781460
- Product name
- CPTH2
- Packaging
- 25mg
- Price
- $160
- Updated
- 2021/12/16
Histone Acetyltransferase Inhibitor IV, CPTH2 Chemical Properties,Usage,Production
Description
CPTH2 (357649-93-5) is a selective inhibitor of the histone acetyltransferase Gcn5P bothin vitroandin vivo(IC50= 0.8 mM).In vitro, the HAT inhibitory activity of CPTH2 was caused via bridge-interaction with histone H3. It’sin vivoactivity 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.
Synthesis
7283-39-8
536-38-9
357649-93-5
General procedure for the synthesis of 4-(4-chlorophenyl)-2-(2-cyclopentylidenehydrazinyl)thiazole from 2-cyclopentylidenehydrazine-1-carbothioamide and α-bromo-4-chloroacetophenone: Accurately weighed 0.157 g of cyclopentanone condensed thiosemicarbazone Schiff base and 0.234 g of p-chloro-α-bromoacetophenone were placed in a reaction vial, and 15 mL of isopropanol was added as solvent. The reaction mixture was stirred at room temperature and the progress of the reaction was monitored by thin layer chromatography (TLC, unfolding agent ratio of ethyl acetate: petroleum ether = 1:2). After 4 hours of reaction, no significant change in the reaction system was observed and the reaction was terminated. The reaction mixture was filtered and the resulting filter cake was washed with ethanol to yield 0.271 g of white solid product.
References
[1] FRANCO CHIMENTI. A Novel Histone Acetyltransferase Inhibitor Modulating Gcn5 Network: Cyclopentylidene-[4-(4′-chlorophenyl)thiazol-2-yl)hydrazone[J]. Journal of Medicinal Chemistry, 2008, 52 2: 530-536. DOI:10.1021/jm800885d
Histone Acetyltransferase Inhibitor IV, CPTH2 Preparation Products And Raw materials
Raw materials
Preparation Products
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