PF-CBP1，CBP/p300 Bromodomain Inhibitor

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: ≥360 days 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:

1. 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.