cu3

CU-3 is a potent and selective inhibitor of diacylglycerol kinase alpha (DGKalpha). CU-3 attenuates cancer cell proliferation and simultaneously enhances immune responses including anti-cancer immunity.

(5Z,2E)-CU-3 是一种具有有效性和选择性的 DGKα 同工酶抑制剂，IC50 值为 0.6 μM，通过对竞争ATP来抑制 DGKα，Km 值为 0.48 mM。(5Z,2E)-CU-3 具有选择性，靶向 DGKα 催化区域，但不作用于调节区域。(5Z,2E)-CU-3 具有抗肿瘤和免疫原性作用，促进癌细胞的凋亡和 T 细胞的活化。

CU-32 is an inhibitor of cyclic GMP-AMP (cGAMP) synthase (cGAS; IC50= 0.45 μM).1It reduces DNA-, but not Sendai virus-, induced dimerization of IFN regulatory factor 3 in THP-1 cells, indicating selectivity for the cGAS DNA sensing pathway over the RIG-I-MAVS RNA sensing pathway. It is also selective for cGAS over toll-like receptors (TLRs) at 50 μM. CU-32 decreases IFN-stimulatory DNA-induced production of IFN-β in THP-1 cells when used at concentrations of 10, 30, and 100 μM. 1.Padilla-Salinas, R., Sun, L., Anderson, R., et al.Discovery of small-molecule cyclic GMP-AMP synthase inhibitorsJ. Org. Chem.85(3)1579-1600(2020)