Bioactivity | Anti-inflammatory agent 79 (compound 17q) is an isoquinolinone derivative-based HIF-1 inhibitor (IC50: 0.55 μM), which can effectively block HIF-1 signals and increase HIF- Degradation of 1α. Anti-inflammatory agent 79 inhibits synovial invasion and migration and inhibits angiogenesis. Anti-inflammatory agent 79 also effectively reduced foot swelling and arthritis in a mouse inflammation model, and down-regulated the levels of inflammatory factors and blood vessel proliferation in the body.[13][1]. |
Invitro | Anti-inflammatory agent 79 (2.5-10 μM; 24 h) 可浓度依赖性地阻断缺氧诱导的 HIF-1α 蛋白积累,减少炎症反应,抑制细胞侵袭性并促进人 RA 滑膜细胞系中 VHL 依赖性 HIF-1α 降解[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Anti-inflammatory agent 79 相关抗体: Western Blot Analysis[1] Cell Line: |
In Vivo | Anti-inflammatory agent 79 (30 mg/kg, 60 mg/kg; ip; 2 天 1 次, 共 16 天) 改善了佐剂诱导关节炎 (AIA) 大鼠模型中踝关节的病理损伤,减少了血管生成并减弱了炎症反应[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
Formula | C21H17NO2 |
Molar Mass | 315.37 |
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]. Cai L, et al. Discovery of novel diaryl substituted isoquinolin-1(2H)-one derivatives as hypoxia-inducible factor-1 signaling inhibitors for the treatment of rheumatoid arthritis. Eur J Med Chem. 2024 Apr 16;271:116417. |