Succinate Receptor 1 Inhibitor

SUCNR1-IN-1 is an orally active SUCNR1 inhibitor. SUCNR1-IN-1 exhibits inhibitory rates of 23% and 56% against rat and mouse SUCNR1 at 100 μM, respectively. SUCNR1-IN-1 can be used in the research of rheumatoid arthritis.

SUCNR1 antagonist-1 is an orally active SUCNR1 antagonist. SUCNR1 antagonist-1 forms stable, water-bridged hydrogen bonds with key residue Glu22^1.31 to stabilize binding conformation and modulates protein conformational flexibility. SUCNR1 antagonist-1 blocks succinate-mediated SUCNR1 signaling and induces cell apoptosis. SUCNR1 antagonist-1 can be used for the research of colorectal carcinoma.

SUCNR1-IN-2 (Statement 35) is a SUCNR1 inhibitor. SUCNR1-IN-2 can be used for the study of neurodegenerative diseases such as neuroinflammation.

4'-O-Methylbavachalcone is an orally active prenylated flavonoid that inhibits the activity of SARS-CoV papain-like protease (PLpro), with an IC₅₀ of 10.1 μM and a K_i of 4.6 μM. 4'-O-Methylbavachalcone inhibits poly (ADP-ribose) polymerase-mediated cell death (parthanatos), reduces cerebral infarct volume, binds to the orthosteric site of SUCNR1, blocks the interaction between succinate and SUCNR1, inhibits SUCNR1 activity, blocks the nuclear translocation of NFATc4, suppresses the activation of the ERK1/2 signaling pathway, inhibits cardiomyocyte hypertrophy and restores the expression of α-actinin. 4'-O-Methylbavachalcone can be used in studies related to ischemic stroke, SARS-CoV and cardiomyocyte hypertrophy.