AV123

AV123 (compound 12) is a non-cytotoxic RIPK1 inhibitor (IC50=12.12 µM). AV123 blocks the TNF-α-induced necroptotic (EC50=1.7 μM) but not the apoptotic cell death. AV123 can be used in the study of necrotic chronic conditions such as ischemia-reperfusion injury of the brain, heart and kidney, inflammatory diseases, neurodegenerative diseases and infectious diseases[1].

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Apoptosis >> RIP kinase

Research Areas >> Inflammation/Immunology

Research Areas >> Metabolic Disease

Research Areas >> Neurological Disease

IC50: 0.48 µM (CDK9/ CyclinT), 0.80 µM (CLK1 of Mus musculus), 1.80 µM (DYRK1A of Rattus norvegicus), >10 µM (CDK2/CyclinA, CDK5/p25, HASPIN, Pim1, CK1 ε, JAK3, ABL1, RIPK3, AURKB)[1].

AV123 (0.01-100 µM; 24 h) efficiently blocks necroptosis in a dose-dependent manner in FADD-deficient Jurkat cells[1]. AV123 (0.01-50 µM; 24 h) shows no toxicity to RPE-1 cells[1]. Cell Viability Assay[1] Cell Line: FADD-deficient Jurkat cells Concentration: 0.01-100 µM Incubation Time: 24 h Result: Significantly blocked the necroptotic cell-death induced by TNF-α with an EC50 value of 1.7 µM. Cell Cytotoxicity Assay[1] Cell Line: RPE-1 cells Concentration: 0.01-50 µM Incubation Time: 24 h Result: Exhibited no toxicity to RPE-1 cells.

[1]. Benchekroun M, et al. Discovery of simplified benzazole fragments derived from the marine benzosceptrin B as necroptosis inhibitors involving the receptor interacting protein Kinase-1. Eur J Med Chem. 2020 Sep 1;201:112337.