(5Z,2E) -CU-3

(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[1].

Product Specifications

CAS Number

[1815598-71-0]

UNSPSC

12352005

Target

Apoptosis; DGK

Type

Reference compound

Related Pathways

Apoptosis; Metabolic Enzyme/Protease

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/5z-2e-cu-3.html

Concentration

10mM

Purity

98.04

Solubility

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

Smiles

O=S(C1=CC=CC=C1)(NN(C/2=O)C(SC2=C/C=C/C3=CC=CO3)=S)=O

Molecular Formula

C16H12N2O4S3

Molecular Weight

392.47

References & Citations

[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.