(5Z, 2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z, 2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z, 2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells.

Product information

CAS Number: 1815598-71-0

Molecular Weight: 392.47

Formula: C16H12N2O4S3

Chemical Name: N-[(5Z)-5-[(2E)-3-(furan-2-yl)prop-2-en-1-ylidene]-4-oxo-2-sulfanylidene-1, 3-thiazolidin-3-yl]benzenesulfonamide

Smiles: O=C1/C(=C/C=C/C2=CC=CO2)/SC(=S)N1NS(=O)(=O)C1C=CC=CC=1

InChiKey: YIUMXULORVBWLL-SPGDJUBISA-N

InChi: InChI=1S/C16H12N2O4S3/c19-15-14(10-4-6-12-7-5-11-22-12)24-16(23)18(15)17-25(20,21)13-8-2-1-3-9-13/h1-11,17H/b6-4+,14-10-

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 20 mg/mL (50.96 mM; ultrasonic and warming and heat to 60°C)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

References:

1. Liu K, et al. A novel diacylglycerol kinase α-selective inhibitor, CU-3, induces cancer cell apoptosis and enhances immune response. J Lipid Res. 2016 Mar;57(3):368-79.

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