| Bioactivity | 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]. | ||||||||||||
| Target | IC50: 0.03 μM (RORγt) | ||||||||||||
| Invitro | 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: | ||||||||||||
| Name | TMP920 | ||||||||||||
| CAS | 1421837-45-7 | ||||||||||||
| Formula | C29H30N2O3 | ||||||||||||
| Molar Mass | 454.56 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |