Description
PF-CBP1 is a potent and selective CBP/p300 bromodomain inhibitor (IC50 ~125 nM for CBP and 363 nM for p300). It has >100-fold selectivity for CBP over BRD4, and shows selectivity over a panel of other bromodomains. PF-CBP1 reduces LPS-induced IL-1β, IL-6 and IFN-β expression in macrophages in vitro. It can also downregulate RGS4 expression in primary cortical neurons in vitro.
Product information
CAS Number: 1962928-21-7
Molecular Weight: 488.62
Formula: C29H36N4O3
Synonym:
PF-06670910
Chemical Name: 4-(2-(5-(3,5-dimethylisoxazol-4-yl)-2-(4-propoxyphenethyl)-1H-benzo[d]imidazol-1-yl)ethyl)morpholine
Smiles: CCCOC1C=CC(CCC2=NC3=CC(=CC=C3N2CCN2CCOCC2)C2C(C)=NOC=2C)=CC=1
InChiKey: CGWBJJZOKGZCSJ-UHFFFAOYSA-N
InChi: InChI=1S/C29H36N4O3/c1-4-17-35-25-9-5-23(6-10-25)7-12-28-30-26-20-24(29-21(2)31-36-22(29)3)8-11-27(26)33(28)14-13-32-15-18-34-19-16-32/h5-6,8-11,20H,4,7,12-19H2,1-3H3
Technical Data
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 100 mM; EtOH up to 100 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
In Vitro:
PF-CBP1 was used at 10 µM final concentration in various assays.
References:
- Chekler EL, et al. Transcriptional Profiling of a Selective CREB Binding Protein Bromodomain Inhibitor Highlights Therapeutic Opportunities. (2015) Chem Biol. 22(12):1588-96.
Products are for research use only. Not for human use.
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