官网https://www.medchemexpress.cn/CCCP.html
CCCP 是氧化磷酸化 (OXPHOS) 解偶联剂。CCCP 诱导 PINK1 激活，促进 Parkin 在 Ser65 位点磷酸化。
生物活性
CCCP is an oxidative phosphorylation (OXPHOS) uncoupler. CCCP induces activation of PINK1 leading to Parkin Ser65 phosphorylation[1].

IC50 & Target
STING[1]
IFN-β[1]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HepG2 IC50
22 μM
Hepatotoxicity in human HepG2 cells assessed as decrease in cell viability after 24 hrs by PrestoBlue assay
[PMID: 27598234]
HepG2 IC50
36 μM
Hepatotoxicity in human HepG2 cells assessed as loss of mitochondrial membrane potential after 24 hrs by JC-1 staining based fluorescence assay
[PMID: 27598234]
HepG2 IC50
6 μM
Hepatotoxicity in human HepG2 cells assessed as decrease in cell viability after 48 hrs by PrestoBlue assay
[PMID: 27598234]
HepG2 IC50
7.2 μM
Hepatotoxicity in human HepG2 cells assessed as intracellular ATP level after 48 hrs by luminescence based ATP detection assay
[PMID: 27598234]
HepG2 IC50
9.8 μM
Hepatotoxicity in human HepG2 cells assessed as intracellular ATP level after 24 hrs by luminescence based ATP detection assay
[PMID: 27598234]
体外研究
(In Vitro)
CCCP 抑制由各种类型 STING 通路激活剂诱导的 IFN-β 产生。CCCP 通过破坏 STING 和 TBK1 的结合来抑制 STING、TBK1 和 IRF3 的磷酸化。CCCP 抑制 STING 及其下游信号分子 TBK1 和 IRF3 的激活，但不抑制 STING 易位到核周区域。CCCP 会损害 STING 和 TBK1 之间的相互作用，并同时触发线粒体裂变。重要的是，关键线粒体裂变调节因子 Drp1 的敲除恢复了 STING 活性，表明 CCCP 通过 DRP1 介导的线粒体断裂下调 STING 通路。破坏膜电位的质子载体 CCCP 会抑制 DMXAA 触发的 STING 信号通路。CCCP 显著抑制 DMXAA 处理的 RAW264.7 细胞和 MEF 中 IFN-β 的产生[1]。
低至 1 μM CCCP 就足以诱导有丝分裂。在用 10 μM CCCP (用于诱导线粒体自噬的剂量) 处理的细胞中，几乎不会诱导有丝分裂。从机制上讲，有丝分裂需要将受损的线粒体定位在细胞外围，这是因为受损的线粒体避免与内向运动蛋白结合[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

CCCP 相关抗体:
ERK1/2 Antibody
E-Cadherin Antibody (YA470)
Fatty Acid Synthase Antibody (YA766)
DYKDDDDK Tag (FLAG) Antibody
GAPDH Antibody
GFP Antibody
p53 Antibody (YA250)
RUNX2 Antibody
STING Antibody (YA048)
Ferritin Heavy Chain Antibody
COX2 Antibody
Ctip2 Antibody
Cyclin D1 Antibody (YA485)
Cytochrome C Antibody
c-Myc Antibody
Parkin Antibody
AIF Antibody (YA636)
ALIX Antibody
CNPase Antibody
Cortactin Antibody
COX IV Antibody
COX2/Cyclooxygenase 2 Antibody
Cyclin A2 Antibody
Cyclin B1 Antibody (YA486)
Drosha Antibody
E-Cadherin Antibody (YA778)
EEA1 Antibody
EpCAM Antibody (YA772)
Fatty Acid Synthase Antibody
FIP200 Antibody
体内研究
(In Vivo)
使用 CCCP 和 PPEF 各 3 mg/kg.bw 的相同剂量。在这两种情况下，细菌载量均观察到 1 个对数减少。然而，当 3 mg/kg.bw 的 PPEF 与 3 mg/kg.bw 的 CCCP 结合使用时，观察到细菌数量减少了 6 log10。开发的模型验证了联合疗法增强的抗菌活性[2]。99mSD 大鼠心脏中的 Tc-MIBI 信号给予 CCCP (4 mg/kg 腹膜内注射) 或对照组也被测量。99mTc-MIBI 信号在给予 CCCP 的大鼠心脏中降低，同时通过31P 磁共振波谱测量的 ATP 含量降低。为了研究 CCCP 是否降低了大鼠的 99mTc-MIBI 信号，我们分析了给予 CCCP 的大鼠离体心脏组织中的放射性同位素活性。99mTc-MIBI 注射后 180 分钟，CCCP 组心脏 99mTc-MIBI信号明显低于对照组[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量
204.62

Formula
C9H5ClN4

CAS 号
555-60-2

性状
固体

颜色
Yellow to brown

运输条件
Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year