PF-CBP1 |
| Catalog No.GC15152 |
CBP/p300 bromodomain inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
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 | |
| Chemical Name | 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 | ||
| Formula | C29H37ClN4O3 | M.Wt | 525.08 |
| Solubility | ≥ 52.5mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)
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