An inhibitor of the GBP1-Pim-1 protein-protein interaction
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NSC 756093

Item No. 35023

Technical Information
Formal Name
4,9-dihydro-4-(2-hydroxyethyl)-6-methoxy-9-phenyl-furo[3,4-b]quinolin-1(3H)-one
CAS Number
1629908-92-4
Molecular Formula
C20H19NO4
Formula Weight
Purity
≥98%
A solid
SMILES
O=C1OCC2=C1C(C3=CC=C(C=C3N2CCO)OC)C4=CC=CC=C4
InChi Code
InChI=1S/C20H19NO4/c1-24-14-7-8-15-16(11-14)21(9-10-22)17-12-25-20(23)19(17)18(15)13-5-3-2-4-6-13/h2-8,11,18,22H,9-10,12H2,1H3
InChi Key
SMEJQLRLHKWIFV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    NSC 756093 is an inhibitor of the protein-protein interaction between guanylate binding protein 1 (GBP1) and the serine/threonine kinase Pim-1.1 It binds to GBP1-Pim-1 (Kd = 38 nM) and inhibits the interaction by 65% when used at a concentration of 100 nM. NSC 756093 enhances radiation-induced cytotoxicity in FaDu hypopharyngeal carcinoma cells (IC50 = 496 nM), as well as induces apoptosis and cell cycle arrest at the G2/M phase in the same cells.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Andreoli, M., Persico, M., Kumar, A., et alIdentification of the first inhibitor of the GBP1:PIM1 interaction. Implications for the development of a new class of anticancer agents against paclitaxel resistant cancer cells. J. Med. Chem. 57(19), 7916-7932 (2014).

    2. Resendez, A., Tailor, D., Graves, E., et alRadiosensitization of head and neck squamous cell carcinoma (HNSCC) by a podophyllotoxin. ACS Med. Chem. Lett. 10(9), 1314-1321 (2019).