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NI-57

Chemical Structure : NI-57

CAS No.: 1883548-89-7

NI-57 (BRPF inhibitor NI57)

Catalog No.: PC-62286Not For Human Use, Lab Use Only.

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.

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Biological Activity

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.
NI-57 shows highly selectivity against other non-Class IV bromodomains, including the BETs, as measured by both biophysical and biochemical methods.
NI-57 displays 32-fold selectivity over the closest off-target BRD9.
NI-57 shows accelerated FRAP recovery at 1 uM in the BRPF2 FRAP assay preventing binding of full-length BRPF2 to chromatin.

Physicochemical Properties

M.Wt 383.422
Formula C19H17N3O4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

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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