CB2R agonist 4 is a cannabinoid receptor 2 (CB2R) agonist with an EC50 value of 6.9 μM. It can induce apoptosis, promote reactive oxygen species (ROS) production, and cause protein misfolding. Additionally, CB2R agonist 4 exhibits cytotoxicity against various tumor cells and is applicable for cancer research.

CB2 receptor:6.9 μM (EC50)

CB2R agonist 4 (Compound 63) exhibits cytotoxicity in HaCaT, HEPG2, A375, SHSY5Y, MCF7, and A549 cells, with EC₅₀ values of 21.41, 2.17, 2.29, 23.21, 27.93, and 36.4 μM, respectively. It significantly inhibits TRPM8 and BRD4 with IC₅₀ values of 0.36 μM and 0.11 μM, while showing weaker inhibition of BRK with an IC₅₀ of 29.17 μM, and it activates TRPA1 with an EC₅₀ of 2.54 μM. In A357 cells, it induces lipid remodeling, characterized by reduced diacylglycerol and cholesterol ester, and increased lysophosphatidylcholine and lysophosphatidylethanolamine. Additionally, CB2R agonist 4 (2.5-10 μM, 2-8 h) triggers reactive oxygen species (ROS) generation in A357 cells and (5-20 μM, 24 h) increases misfolded protein levels. Furthermore, it induces apoptosis in A357 cells at concentrations of 1.25-5 μM over 72 hours.