NI-57, BRPF Bromodomain Inhibitor


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

Description

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.

Product information

CAS Number: 1883548-89-7

Molecular Weight: 383.42

Formula: C19H17N3O4S

Chemical Name: 4-cyano-N-(1,3-dimethyl-2-oxo-1,2-dihydroquinolin-6-yl)-2-methoxybenzenesulfonamide

Smiles: CC1=CC2=CC(=CC=C2N(C)C1=O)NS(=O)(=O)C1=CC=C(C=C1OC)C#N

InChiKey: UEMQPCYDWCSVCU-UHFFFAOYSA-N

InChi: InChI=1S/C19H17N3O4S/c1-12-8-14-10-15(5-6-16(14)22(2)19(12)23)21-27(24,25)18-7-4-13(11-20)9-17(18)26-3/h4-10,21H,1-3H3

Technical Data

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

In Vitro:

NI-57 was used at 10 µM final concentration in vitro and in cellular assays.

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

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