TMP920

TMP920 is a highly potent and selective RORγt antagonist. TMP920 inhibits RORγt binding to the SRC1 peptide with an IC50 of 0.03 μM[1].

Signaling Pathways >> Metabolic Enzyme/Protease >> ROR

Research Areas >> Inflammation/Immunology

IC50: 0.03 μM (RORγt)[1]

TMP920 (0.09-30 μM) starts to show toxic effects on cell growth at >10 μM in Naïve CD4+ T cells[1]. TMP920 suppresses Th17 cell differentiation and lost its IL-17 inhibitory effect at <2.5 μM in vitro[1]. TMP920 suppresses IL-17 production from differentiated Th17 cells in vitro[1]. TMP920 suppresses the Th17 cell transcriptome and promotes alternate T-cell subsets[1]. TMP920 significantly reduces RORγt-DNA interactions[1]. Cell Cytotoxicity Assay[1] Cell Line: Naïve CD4 + T cells Concentration: 0.09-30 μM Incubation Time: 48 hours Result: Has toxic effects on cell growth at >10 μM.

[1]. Xiao S, et al. Small-molecule RORγt antagonists inhibit T helper 17 cell transcriptional network by divergent mechanisms. Immunity. 2014 Apr 17;40(4):477-89.