An antagonist of A-FABP/aP2 protein-protein interactions
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HTS 01037

Item No. 10699

Technical Information
Formal Name
4-[(3-carboxy-1-oxo-2-propen-1-yl)amino]-[2,2'-bithiophene]-5-carboxylic acid, 5-methyl ester
CAS Number
682741-29-3
Molecular Formula
C14H11NO5S2
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 3 mg/mlDMSO: 5 mg/mlDMSO:PBS (pH 7.2) (1:10): 0.1 mg/ml
λmax
331 nm
SMILES
O=C(/C=C/C(O)=O)NC1=C(C(OC)=O)SC(C2=CC=CS2)=C1
InChi Code
InChI=1S/C14H11NO5S2/c1-20-14(19)13-8(15-11(16)4-5-12(17)18)7-10(22-13)9-3-2-6-21-9/h2-7H,1H3,(H,15,16)(H,17,18)/b5-4+
InChi Key
GJODSFZNKNHKML-SNAWJCMRSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    HTS 01037 is a high-affinity ligand of adipocyte fatty acid binding protein (A-FABP/aP2) (Ki = 0.67 μM) that presumably competes with fatty acids for functional binding in the ligand-binding cavity of A-FABP/aP2.1 At a concentration of 10 μM, HTS 01037 antagonizes the protein-protein interaction of A-FABP/aP2 with hormone sensitive lipase in cultured C8PA lipocytes. 1 HTS 01037 inhibits lipolysis in 3T3L1 adipocytes and reduces lipopolysaccharide-stimulated inflammation in bone marrow-derived macrophages, both effects of which are similar to the phenotype of A-FABP/aP2 knockout mice.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hertzel, A.V., Hellberg, K., Reynolds, J.M., et alIdentification and characterization of a small molecule inhibitor of fatty acid binding proteins. J. Med. Chem. 52, 6024-6031 (2009).