CPTH2 (hydrochloride)
目录号 : GC14428
A HAT inhibitor
Cas No.:2108899-91-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
CPTH2 is an inhibitor of HAT activity of Gcn5.
Histone acetyltransferases (HATs) has been identified to add the acetyl group on the specific lysine of histone H3 and H4 N-termini, and such signatures are able to increase the accessibility of the underlying chromatin at specific genes or over vast regions of the genome. Gcn5p is a chimeric protein made up of a number of functional domains.
In vitro: Previous study identified a novel molecule named CPTH2, which was selected based on its inhibitory effect on the growth of a gcn5Delta strain. This study indicated a specific chemical-genetic interaction between CPTH2 and HAT Gcn5p, suggesting that CPTH2 could inhibit the dependent functional network of Gcn5p. In addition, CPTH2 was found to be able to inhibit an in-vitro HAT reaction, which could be reverted by increasing concentration of histone H3 [1].
In vivo: In vivo, CPTH2 could decrease the acetylation of bulk histone H3 at the specific H3-AcK14 site [1].
Clinical trial: Up to now, CPTH2 is still in the preclinical development stage.
Reference:
[1] F. Chimenti, B. Bizzarri, E. Maccioni, et al. A novel histone acetyltransferase inhibitor modulating Gcn5 network: Cyclopentylidene-[4-(4'-chlorophenyl)thiazol-2-yl)hydrazone. Journal of Medicinal Chemistry 52, 530-536 (2009).
| Cas No. | 2108899-91-6 | SDF | |
| 化学名 | 2-[4-(4-chlorophenyl)-2-thiazolyl]hydrazone-cyclopentanone, monohydrochloride | ||
| Canonical SMILES | ClC(C=C1)=CC=C1C2=CSC(N/N=C3CCCC\3)=N2.Cl | ||
| 分子式 | C14H14ClN3S • HCl | 分子量 | 328.3 |
| 溶解度 | ≤5mg/ml in ethanol;16mg/ml in DMSO;5mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.046 mL | 15.23 mL | 30.4599 mL |
| 5 mM | 0.6092 mL | 3.046 mL | 6.092 mL |
| 10 mM | 0.3046 mL | 1.523 mL | 3.046 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。