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.
CAS Number: 1883548-89-7
Molecular Weight: 383.42
Chemical Name: 4-cyano-N-(1,3-dimethyl-2-oxo-1,2-dihydroquinolin-6-yl)-2-methoxybenzenesulfonamide
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO 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: ≥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
NI-57 was used at 10 µM final concentration in vitro and in cellular assays.
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