| Bioactivity | 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]. |
| Target | 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). |
| Invitro | 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: |
| Name | AV123 |
| CAS | 233605-81-7 |
| Formula | C11H14N4O2 |
| Molar Mass | 234.25 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |