JNU-0921 is a potent and orally active CD137 agonist. JNU-0921 increases the mRNA expression of IFN-γ and GZMB. JNU-0921 induces luciferase activity with an EC50 value of 64.07 nM.JNU-0921 enhances effector and memory function of cytotoxic CD8+ T cells (CTLs) and alleviates their exhaustion. JNU-0921 also skews polarization of helper T cells toward T helper 1 type and enhances their activity to boost CTL function. JNU-0921 shows anticancer activity[1].