(5Z,2E)-CU-3

(5Z,2E)-CU-3 is an isomer of CU-3 (HY-121638). CU-3 is a DGKα inhibitor with an IC₅₀ of 0.6 μM. CU-3 competitively reduces DGKα’s affinity for ATP via binding to the enzyme’s catalytic region. CU-3 induces apoptosis in cancer cells. CU-3 promotes T-cell activation and enhances IL-2 production. CU-3 can be used for the research of hepatocellular carcinoma and cervical cancer^[1]. IC50 & Target:IC50: 0.6 μM (DGKα)^[1] In Vitro:CU-3 potently and selectively inhibits purified pig DGK α activity with an IC₅₀ of 0.6 μM by targeting the catalytic domain and competitively interfering with ATP binding^[1].
CU-3 (2 μM; 24 h) inhibits intracellular DGK α activity in COS-7 cells, reducing phosphatidic acid production induced by overexpressed constitutively active DGK α^[1].
CU-3 (5 μM; 24 h) induces apoptosis in HepG2 and HeLa cancer cells, as measured by increased caspase-3/7 activity, without causing nonspecific toxicity to noncancerous COS-7 cells^[1].
CU-3 (5 μM; 5 min) enhances Con A-induced IL-2 mRNA expression in Jurkat T cells by inhibiting DGK α, promoting T-cell activation^[1].