NecroIr1 是一种铱 (III) 复合物，是顺铂 (Cisplatin, HY-17394) 耐药肺癌细胞 (A549R) 的坏死诱导剂。NecroIr1 选择性积累在线粒体中，导致氧化应激和线粒体膜电位 (MMP) 的损失。NecroIr1 能够激活受体相互作用的丝氨酸苏氨酸激酶 3 (RIPK3) 和混合谱系激酶结构域样假激酶 (MLKL)，调节CDK4表达。
| 生物活性 | NecroIr1 is an iridium(III) complex, serves asnecroptosisinducers inCisplatin(HY-17394)-resistant lungcancercells (A549R). NecroIr1 selectively accumulates in mitochondria, leading to oxidative stress and loss of mitochondrial membrane potential (MMP). NecroIr1 activates receptor-interactingserine-threonine kinase 3(RIPK3) andMixed Lineage Kinase(MLKL), and regulatesCDK4expression[1]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | NecroIr1 (2 μM; 1-2 d) exerts subcellular distribution over 90% accumulated in mitochondria in non-labelled A549R and CFSElabelled L02 cells[1].
NecroIr1 (1.5 μM and 3 μM; 24 h) results ROS generation increasing and loss of mitochondrial membrane potential[1].
NecroIr1 (1.5 μM and 3 μM; 24 h) activates necroptosis proteins, increases the phosphorylation of RIPK1 and RIPK3[1].
NecroIr1 (0.75 μM and 1.5 μM; 24 h) induces necroptosis by arresting cell cycle at G0/G1[1].
NecroIr1 (0.75-3.0 μM; 24 h) inhibits A549R cells proliferation[1].
Western Blot Analysis[1] | Cell Line: | A549R cells | | Concentration: | 1.5 μM and 3 μM | | Incubation Time: | 24 hours | | Result: | Increased phospho-RIPK1 (p-PIPK1), total RIPK3, and phospho-RIPK3 (p-PIPK3) level. |
Cell Cycle Analysis[1] | Cell Line: | A549R cells | | Concentration: | 0 μM, 0.75 μM and 1.5 μM | | Incubation Time: | 24 hours | | Result: | Arrested cell cycle at G0/G1 phase in a dose-dependent manner. |
Cell Proliferation Assay[1] | Cell Line: | A549R cells | | Concentration: | 0 μM, 0.75 μM, 1.5 μM and 3.0 μM | | Incubation Time: | 24 hours | | Result: | Inhibits cell proliferation in a dose-dependent manner. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(121.45 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.2145 mL | 6.0727 mL | 12.1454 mL | | 5 mM | 0.2429 mL | 1.2145 mL | 2.4291 mL | | 10 mM | 0.1215 mL | 0.6073 mL | 1.2145 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
