OF-1 --- BRPF Bromodomain Inhibitor

OF-1 is the potent and selective BRPF (BRomodomain and PHD Finger containing) inhibitor. It binds to BRPF1B with a KD of 100 nM (ITC), to BRPF2 with a KD of 500 nM (ITC) and to BRPF3 with a KD of 2.4 mM (ITC). It has general >100-fold selectivity against other bromodomains (39-fold selectivity over BRD4). OF-1 increases thermal stability in the cellular thermal shift assay (CETSA) of full length BRPF1B at 1 µM and also demonstrates accelerated FRAP recovery at 5 µM in the BRPF2 FRAP assay. It shows modest general cytotoxicity.

Product information

CAS Number: 919973-83-4

Molecular Weight: 440.31

Formula: C17H18BrN3O4S

Synonym:

SGC OF-1

Chemical Name: 4-bromo-N-(6-methoxy-1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)-2-methylbenzenesulfonamide

Smiles: CC1=CC(Br)=CC=C1S(=O)(=O)NC1=CC2=C(C=C1OC)N(C)C(=O)N2C

InChiKey: YUNQZQREIHWDQT-UHFFFAOYSA-N

InChi: InChI=1S/C17H18BrN3O4S/c1-10-7-11(18)5-6-16(10)26(23,24)19-12-8-13-14(9-15(12)25-4)21(3)17(22)20(13)2/h5-9,19H,1-4H3

Technical Data

Appearance: Solid Power.

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

Solubility: DMSO up to 20 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:

OF-1 was used at 5-10 µM final concentration in various in vitro assays.

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