CTPB
目录号 : GC14524A selective activator of p300 HAT
Cas No.:586976-24-1
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
CTPB is a selective activator of p300 HAT activity [1].
CREB binding protein (CBP) and E1A binding protein p300, also known as p300 are functionally related transcriptional co-activators (CoAs) and histone acetyltransferases (HATs). The p300/CBP is a global transcriptional coactivator, which plays a critical role in cell cycle control, differentiation, and apoptosis. Mutations in p300/CBP are associated with different human cancers and other human diseases [1][2].
CTPB, also known as N-(4-chloro-3-trifluoromethyl-phenyl)-2-ethoxy-6-pentadecyl-benza-mide, is an amide derivative that selectively activates p300 HAT activity. CTPB directly binds p300 [2]. CTPB exhibited an enhancement in the p300 HAT activity concentration-dependently with maximal activation at 275 μM. In the presence of p300, CTPB resulted in the gradual increase in the acetylation of both histones H3 and H4, peaking at 200 μM. Further increase in the concentration of CTPB reduced the HAT activity, could be due to an alteration in the reaction condition affecting the efficiency of the HAT. CTPB didn’t alter PCAF HAT or histone deacetylase activity [1].
References:
[1]. Balasubramanyam K, Swaminathan V, Ranganathan A, et al. Small molecule modulators of histone acetyltransferase p300. J Biol Chem. 2003 May 23;278(21):19134-40.
[2]. Devipriya B, Parameswari AR, Rajalakshmi G, et al. Exploring the binding affinities of p300 enzyme activators CTPB and CTB using docking method. Indian J Biochem Biophys. 2010 Dec;47(6):364-9.
| Cas No. | 586976-24-1 | SDF | |
| 化学名 | N-[4-chloro-3-(trifluoromethyl)phenyl]-2-ethoxy-6-pentadecyl-benzamide | ||
| Canonical SMILES | ClC1=CC=C(NC(C2=C(CCCCCCCCCCCCCCC)C=CC=C2OCC)=O)C=C1C(F)(F)F | ||
| 分子式 | C31H43ClF3NO2 | 分子量 | 554.1 |
| 溶解度 | ≤15mg/ml in ethanol;20mg/ml in DMSO;30mg/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 | 1.8047 mL | 9.0236 mL | 18.0473 mL |
| 5 mM | 0.3609 mL | 1.8047 mL | 3.6095 mL |
| 10 mM | 0.1805 mL | 0.9024 mL | 1.8047 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。