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NecroIr1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
NecroIr1图片
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
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]

CDK4

 

RIPK3

 

RIPK1

 

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.
分子量

823.36

性状

Solid

Formula

C40H29ClIrN5O-

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
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.2145 mL6.0727 mL12.1454 mL
5 mM0.2429 mL1.2145 mL2.4291 mL
10 mM0.1215 mL0.6073 mL1.2145 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。