BMS 502

BMS 502 is an inhibitor of diacylglycerol kinase α (DGK-α), DGK-ζ, and DGK-ι (IC₅₀s = 0.0046, 0.0021, and 0.0026 µM, respectively).¹ It is selective for these DGKs over DGK-β, DGK-γ, and DGK-κ (IC₅₀s = 1, 0.68, and 4.6 µM, respectively). BMS 502 increases levels of IFN-γ and phosphorylation of ERK in isolated human whole blood (EC₅₀s = 0.28 and 0.52 µM, respectively). It also increases the proliferation of CD8⁺ T cells (EC₅₀ = 0.065 µM), which express DGK-α and DGK-ζ but not DGK-ι. BMS 502 (0.3-10 mg/kg) increases the frequency of CD69⁺CD8⁺ T cells when administered in combination with the peptide antigen SIINFEKL in OT I mice, which express modified murine T cell receptors that recognize SIINFEKL.

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1. Chupak, L., Wichroski, M., Zheng, X., et al. Discovery of potent, dual-inhibitors of diacylglycerol kinases alpha and zeta guided by phenotypic optimization. ACS Med. Chem. Lett. 14(7), 929-935 (2023).