NI-57 | B2854

NI-57 is an inhibitor of the bromodomains of BRPF proteins. The bromodomain and plant homeodomain finger-containing (BRPF) family are scaffolding proteins important for the recruitment and activation of MOZ/MORF histone acetyltransferases to chromatin. NI-57 binds to BRPF1B, BRPF2 and BRPF3 with Kd values of 31 nM, 108 nM and 408 nM respectively. It inhibits BRPF1 with an IC₅₀ of 114 nM. It shows functional activity in cellular assays by modulating the phenotype at low micromolar concentrations in cancer and inflammatory models.

NI-57 is an inhibitor of the bromodomains of BRPF proteins. The bromodomain and plant homeodomain finger-containing (BRPF) family are scaffolding proteins important for the recruitment and activation of MOZ/MORF histone acetyltransferases to chromatin. NI-57 binds to BRPF1B, BRPF2 and BRPF3 with Kd values of 31 nM, 108 nM and 408 nM respectively. It inhibits BRPF1 with an IC₅₀ of 114 nM. It shows functional activity in cellular assays by modulating the phenotype at low micromolar concentrations in cancer and inflammatory models.

B2854 | NI-57 DataSheet

Alternate Name/Synonyms: 4-cyano-N-(1,3-dimethyl-2-oxoquinolin-6-yl)-2-methoxybenzenesulfonamide; 4-cyano-N-(1,2-dihydro-1,3-dimethyl-2-oxo-6-quinolinyl)-2-methoxy-benzenesulfonamide; 4-Cyano-~{n}-(1,3-Dimethyl-2-Oxidanylidene-Quinolin-6-Yl)-2-Methoxy-Benzenesulfonamide

Appearance: A crystalline solid

Formulation:

CAS Number: 1883548-89-7

Structure Available?: True

Peptide sequence:

Salt Form: False

Molecular Formula: C₁₉H₁₇N₃O₄S

Molecular Weight: 383.42

Cell-Permeable?: True

Purity: ≥98%

Solubilities: ~30 mg/ml in DMF in 0, ~25 mg/ml in in DMSO

Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.

Country of Origin: USA

Tag Line: An inhibitor of the bromodomains of BRPF proteins

MDL Number:

PubChem CID: 91827373

SMILES: CC1=CC2=C(C=CC(=C2)NS(=O)(=O)C3=C(C=C(C=C3)C#N)OC)N(C1=O)C

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

InChi Key: UEMQPCYDWCSVCU-UHFFFAOYSA-N