NI-57 ( BRPF inhibitor NI57 )

Catalog No. M12933 CAS No. 1883548-89-7

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

NI-57
Note

Research use only, not for human use.
Brief Description

NI-57 is a potent inhibitor of the bromodomain of the BRPFs and binds to BRPF1B, BRPF2 and BRPF3 and with KD of 31 nM,108 nM and 408 nM (ITC), respectively.
Description

NI-57 is a potent inhibitor of the bromodomain of the BRPFs and binds to BRPF1B, BRPF2 and BRPF3 and with KD of 31 nM,108 nM and 408 nM (ITC), respectively; shows highly selectivity against other non-Class IV bromodomains, including the BETs, as measured by both biophysical and biochemical methods; displays 32-fold selectivity over the closest off-target BRD9; shows accelerated FRAP recovery at 1 uM in the BRPF2 FRAP assay preventing binding of full-length BRPF2 to chromatin.
Synonyms

BRPF inhibitor NI57
Pathway

Chromatin/Epigenetic
Target

Bromodomain
Recptor

Bromodomain
Research Area

Cancer
Indication

——

CAS Number

1883548-89-7
Formula Weight

383.42
Molecular Formula

C19H17N3O4S
Purity

>98% (HPLC)
Solubility

DMSO : ≥ 83.3 mg/mL 217.26 mM
SMILES

O=S(C1=CC=C(C#N)C=C1OC)(NC2=CC3=C(N(C)C(C(C)=C3)=O)C=C2)=O
Chemical Name

4-cyano-N-(1,2-dihydro-1,3-dimethyl-2-oxo-6-quinolinyl)-2-methoxy-benzenesulfonamide

1. Pérez-Salvia M, et al. Epigenetics. 2017 May 4;12(5):323-339.
2. Igoe N, et al. J Med Chem. 2017 Aug 10. doi: 10.1021/acs.jmedchem.7b00611.

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