NI-57, BRPF Bromodomain Inhibitor


Catalog No. size PriceQuantity
M60279-2S 2 mg solid $109
M60279-10S 10 mg solid $436

Description

Product Information
Molecular Weight: 383.42
Formula: C19H17N3O4S
Purity: ≥98%
CAS#: n/a
Solubility: DMSO up to 100 mM
Chemical Name: 4-cyano-N-(1,3-dimethyl-2-oxo-1,2-dihydroquinolin-6-yl)-2-methoxybenzenesulfonamide
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

 

Biological Activity:

NI-57 is a potent and selective inhibitor of the bromodomain of the BRPFs. It binds to BRPF1B with a KD of 31 nM (ITC), to BRPF2 with a KD of 108 nM (ITC) and to BRPF3 KD of 408 nM (ITC). NI-57 is very selective against other non-Class IV bromodomains, including the BETs, has minimum 32-fold selectivity against BRD9. It shows accelerated FRAP recovery at 1 µM in the BRPF2 FRAP assay preventing binding of full-length BRPF2 to chromatin.

How to Use:


In vitro:
 NI-57 was used at 10 µM final concentration in vitro and in cellular assays.
In vivo: n/a

Reference:

  • 1. http://www.thesgc.org/chemical-probes/NI-57/teaser.



     

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

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