An inhibitor of the BRPF1 bromodomain
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NI-42

Item No. 28293

Technical Information
Formal Name
4-cyano-N-(1,2-dihydro-1,3-dimethyl-2-oxo-6-quinolinyl)-benzenesulfonamide
CAS Number
1884640-99-6
Molecular Formula
C18H15N3O3S
Formula Weight
Purity
≥98%
A crystalline solid
λmax
239, 273, 335 nm
SMILES
O=S(C1=CC=C(C#N)C=C1)(NC2=CC(C=C(C)C(N3C)=O)=C3C=C2)=O
InChi Code
InChI=1S/C18H15N3O3S/c1-12-9-14-10-15(5-8-17(14)21(2)18(12)22)20-25(23,24)16-6-3-13(11-19)4-7-16/h3-10,20H,1-2H3
InChi Key
BMVCSXFOQPYKKC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    NI-42 is an inhibitor of the bromodomain and PHD finger-containing 1 (BRPF1) bromodomain (IC50 = 7.9 nM).1 It is selective for BRPF1 over BRPF2/BRD1, BRPF3, BRD9, and BRD4/BD1 (IC50s = 48, 260, 310, and 4,500 nM, respectively).2 NI-42 inhibits the growth of OCI-AML2, Nomo-1, THP-1, KG-1, and MV-4-11 acute myeloid leukemia (AML) cells (GI50s = 1.3, 4.6, 5.7, 7, and 9.9 µM, respectively) and a variety of non-AML cells (GI50s = 1-10 µM).1 It also inhibits the growth of DMS114 lung, HRA-19 colon, and RERF-LC-Sq1 lung cancer cells (GI50s = 16.6, 15.6, and 17.1 µM, respectively) but not NCI H1703 lung cancer cells (GI50 = >30 µM).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Igoe, N., Bayle, E.D., Fedorov, O., et al. Design of a biased potent small molecule inhibitor of the bromodomain and PHD finger-containing (BRPF) proteins suitable for cellular and in vivo studies. J. Med. Chem. 60(2), 668-680 (2017).

    2. 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).