SUCNR1 antagonist-1

SUCNR1 antagonist-1 (Compound 26) potently and competitively inhibits SUCNR1 activity in transiently transfected HEK293 cells, with an IC₅₀ of 11.7 nM in the Glosensor cAMP assay^[1].
SUCNR1 antagonist-1 (18.0 nM; 6 h) inhibits succinate-mediated SUCNR1 signaling in transiently transfected HEK293 cells, with an IC₅₀ of 18.0 nM in the CRE reporter assay^[1].
SUCNR1 antagonist-1 (up to 30 μM; 72 h) exhibits no significant cytotoxicity toward HEK293 cells and THP-1 cells, with an IC₅₀ >30 μM^[1].
SUCNR1 antagonist-1 (0.1-10 μM; 12 h) dose-dependently inhibits succinate-induced expression of immunosuppression-related genes in THP-1 cells^[1].
SUCNR1 antagonist-1 (10 μM; 72 h) reverses succinate-induced immunosuppression by THP-1 macrophages, restoring Jurkat T cell proliferation to 60.6% after 72 h coculture^[1].
SUCNR1 antagonist-1 (10 μM; 5 days) remodels the immune landscape in patient-derived colorectal cancer ALI-PDTIOs, reducing immunosuppressive macrophages, expanding effector T cells, and inducing tumor cell apoptosis after 5 days of treatment^[1].
SUCNR1 antagonist-1 forms stable, high-affinity interactions with SUCNR1, including unique water-bridged hydrogen bonds with Glu22^1.31, which enhances its binding affinity and antagonistic potency^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.