PF-CBP1
目录号 : GC15152
An inhibitor of the CBP and p300 bromodomains
Cas No.:1962928-21-7
Sample solution is provided at 25 µL, 10mM.
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IC50: 125 and 363 nM for CREBBP and p300 bromodomain, respectively
PF-CBP1 is a CBP/p300 bromodomain inhibitor.
Bromodomains are reported to be involved in transcriptional regulation via the recognition of acetyl lysine modifications. However, selective bromodomain modulators are still lacking, though the hydrophobic pocket makes bromodomains attractive targets.
In vitro: PF-CBP1 showed a significant reduction in BRD4 potency, while retained CBP affinity. In order to evaluate compound-related cytotoxicity during gene transcription, primary macrophages were stimulated with LPS and were further analyzed to determine the cell viability. Results showed that PF-CBP1 and the negative control ISOX-INACT did not cause cytotoxicity even at high concentrations up to 30 mM. In addition, PF-CBP1 at 10 mM was able to moderately reduce LPS-induced IL-6 and IFN-b expression, and a decrease in IL-1b expression was observed at 3 mM. Moreover, the rat primary cortical neurons were treated with PF-CBP1, vehicle, or the negative control ISOX-INACT, and the results showed that at 1 hr, there were no changes in RGS4 expression compared with vehicle. However, the treatment of PF-CBP1 at 10-fold IC50 dose could significantly reduce RGS4 mRNA levels at 24 hr when compared with that of vehicle [1].
In vivo: So far, there is no animal in vivo data reported.
Clinical trial: Up to now, PF-CBP1 is still in the preclinical development stage.
Reference:
[1] Chekler EL, et al. Transcriptional Profiling of a Selective CREB Binding Protein Bromodomain Inhibitor Highlights Therapeutic Opportunities. Chem Biol. 2015 Dec 17;22(12):1588-96.
| Cas No. | 1962928-21-7 | SDF | |
| 化学名 | 4-(2-(5-(3,5-dimethylisoxazol-4-yl)-2-(4-propoxyphenethyl)-1H-benzo[d]imidazol-1-yl)ethyl)morpholine hydrochloride | ||
| Canonical SMILES | CCCOC1=CC=C(CCC2=NC3=CC(C4=C(C)ON=C4C)=CC=C3N2CCN5CCOCC5)C=C1.Cl | ||
| 分子式 | C29H37ClN4O3 | 分子量 | 525.08 |
| 溶解度 | ≥ 52.5mg/mL in DMSO | 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 | 1.9045 mL | 9.5224 mL | 19.0447 mL |
| 5 mM | 0.3809 mL | 1.9045 mL | 3.8089 mL |
| 10 mM | 0.1904 mL | 0.9522 mL | 1.9045 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet