Chemical Structure : NI-57
CAS No.: 1883548-89-7
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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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.
| M.Wt | 383.422 | |
| Formula | C19H17N3O4S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
4-cyano-N-(1,2-dihydro-1,3-dimethyl-2-oxo-6-quinolinyl)-2-methoxy-benzenesulfonamide |
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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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