| Description |
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].
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| Related Catalog |
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| Target |
IC50: 88 nM (RIP Kinase)[1]
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| In Vitro |
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: L929 cells Concentration: 10, 50, 250 nM Incubation Time: 1 h Result: Inhibited L929 cell necroptosis in a Dosedependent manner and increased the number of cells in the viable cell zone.
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| 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: Inflammatory mouse model[1] Dosage: 10, 25, 40 mg/kg Administration: i.p.; dissolved in saline containing 10% DMSO and 20% Tween80; 72 h Result: At 25, 40 mg/kg completely inhibited TNF-α induced death in mice, achieving 100% survival compared to 75% survival at 10 mg/kg.
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| References |
[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.
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