OF-1, BRPF Bromodomain Inhibitor


Catalog No. size PriceQuantity
M60222-2S 2 mg solid $129
M60222-10S 10mg solid $522

Description

Product Information

Molecular Weight: 440.31
Formula: C17H18BrN3O4S
Purity: ≥98%
CAS#: 919973-83-4
Solubility: DMSO up to 20 mM
Chemical Name: 4-bromo-N-(6-methoxy-1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)-2-methylbenzenesulfonamide
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

 

Biological Activity:

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.


How to Use:

  • In vitro:  OF-1 was used at 5-10 µM final concentration in various in vitro assays.
  • In vivo: n/a 

Reference

  1.  http://www.thesgc.org/chemical-probes/OF-1 



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

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