PFI-4, BRPF1 Bromodomain Inhibitor

PFI-4 is a potent, selective and cell permeable BRPF1 bromodomain inhibitor. It binds to BRPF1B with a Kd of 13 nM (ITC). It has general >100-fold selectivity against other bromodomains including BRPF2, BRPF3 and BRD4. It reduces recovery time in triple BRD cell construct in FRAP and is potent in cells with IC50 250 nM, while showing no effect on BRPF1A.

Product information

CAS Number: 900305-37-5

Molecular Weight: 380.44

Formula: C21H24N4O3

Chemical Name: N-(1,3-dimethyl-2-oxo-6-(pyrrolidin-1-yl)-2,3-dihydro-1H-benzo[d]imidazol-5-yl)-2-methoxybenzamide

Smiles: COC1=CC=CC=C1C(=O)NC1=CC2=C(C=C1N1CCCC1)N(C)C(=O)N2C

InChiKey: QCIJLRJBZDBVDB-UHFFFAOYSA-N

InChi: InChI=1S/C21H24N4O3/c1-23-17-12-15(22-20(26)14-8-4-5-9-19(14)28-3)16(25-10-6-7-11-25)13-18(17)24(2)21(23)27/h4-5,8-9,12-13H,6-7,10-11H2,1-3H3,(H,22,26)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 50 mM, EtOH up to 10 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:

PFI-4 was used at 5-10 µM final concentration in various in vitro assays.

References:

1. http://www.thesgc.org/chemical-probes/PFI-4

Products are for research use only. Not for human use.