A BRPF bromodomain inhibitor
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NI-57

Item No. 17662

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)Epigenetic Chemical Probe Guide (PDF)
Technical Information
Formal Name
4-cyano-N-(1,2-dihydro-1,3-dimethyl-2-oxo-6-quinolinyl)-2-methoxy-benzenesulfonamide
CAS Number
1883548-89-7
Molecular Formula
C19H17N3O4S
Formula Weight
383.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 25 mg/ml
λmax
210, 236, 279, 310, 334 nm
SMILES
COC1=CC(C#N)=CC=C1S(NC2=CC=C(N(C)C(C(C)=C3)=O)C3=C2)(=O)=O
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $128

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    10 mg

    $219

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    50 mg

    $920

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    Product Description

    NI-57 is a potent inhibitor of the bromodomains of BRPF proteins that binds to BRPF1B, BRPF2, and BRPF3 with Kd values of 31, 108, and 408 nM, respectively, as determined by isothermal titration calorimetry. It is selective for BRPFs over other bromodomains. NI-57 shows accelerated FRAP recovery at 1 µM in the BRPF2 FRAP assay, preventing binding of full-length BRPF2 to chromatin. See the Structural Genomics Consortium (SGC) website for more information.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Citations

    Igoe, N., Bayle, E.D., Tallant, C., et al. Design of a chemical probe for the bromodomain and plant homeodomain finger-containing (BRPF) family of proteins. J. Med. Chem. 60(16), 6998-7011 (2017).