Bioactivity | KWCN-41 is a selective and efficient inhibitor of RIPK1 kinase with an IC50 value of 88 nM. KWCN-41 specifically inhibits cell necrosis but does not inhibit apoptosis. KWCN-41 also has anti-inflammatory effects[1]. |
Target | IC50: 88 nM (RIP Kinase) |
Invitro | KWCN-41(10, 50, 250 nM; 1 h)以剂量依赖性方式抑制 L929 细胞坏死,并增加活细胞区的细胞数量[1]。KWCN-41(10、50、250 nM;0.5、1.5、2.5 h)抑制 L929 细胞中 RIPK1/3 和 MLKL 的磷酸化[1]。KWCN-41 (0-10 μM) 以剂量依赖性方式抑制 TZ 诱导的 L929 细胞坏死,并类似地保护细胞免受 TSZ(TNF-α、Smac 模拟物和 z-VAD-FMK)诱导的 HT- 29 和 U937 细胞[1]。 Cell Viability Assay[1] Cell Line: |
In Vivo | KWCN-41(10、25、40 mg/kg;腹腔注射;72 小时)在 25、40 mg/kg 时完全抑制 TNF-α 诱导的小鼠死亡,实现 100% 的存活率,而在 10 mg/kg 时,小鼠存活率为 75%[1]。 Animal Model: |
Name | KWCN-41 |
CAS | 2913223-17-1 |
Formula | C18H17N3O2 |
Molar Mass | 307.35 |
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]. Cui N, et al. Discovery of Sibiriline derivatives as novel receptor-interacting protein kinase 1 inhibitors. Eur J Med Chem. 2023 Mar 15;250:115190. |