SR 0987

SR 0987 is an agonist of RORγt with EC50 value of ~800 nM for inducing reporter gene expression [1].

RORγt (retinoic acid receptor-related orphan receptor-γt), the T cell-specific isoform of RORγ, is the key lineage-defining transcription factor to initiate the differentiation program of TH17 and Tc17 cells, cells that have demonstrated anti-tumor efficacy [1].

SR 0987 is a RORγt agonist. In murine EL4 T lymphocytes, SR 0987 increased expression of IL17 while repressing the expression of the checkpoint receptor PD-1, suggesting that SR 0987 enhanced protective immunity by regulating expression of IL17 and PD-1 while maintaining the cytotoxic ability of these cells. In both the 5xRORE and IL17 promoter transfected cells, SR0987 concentration dependently induced reporter gene expression with an EC50 of ~800 nM. SR0987 also concentration dependently increased interaction of RORγt with the SRC1-3 NR box peptide [1].

Reference:
[1].  Chang MR, Dharmarajan V, Doebelin C, et al. Synthetic RORγt Agonists Enhance Protective Immunity. ACS Chem Biol. 2016 Apr 15;11(4):1012-8.