AMPK
信号通路图
研究领域
抑制剂选择性比较
AMPK产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S7306 |
Dorsomorphin (Compound C) 2HClDorsomorphin (Compound C) 2HCl是一种有效的，可逆的，选择性AMPK抑制剂，在无细胞试验中Ki为109 nM，对一些结构相关的激酶，包括ZAPK， SYK， PKCθ，PKA和JAK3没有显著的抑制作用。也会抑制I型BMP受体。 |
AMPK inhibition by compound C(Dorsomorphin) inhibited autophagy activation and neuroprotection induced by IPC in PC12 cells. (A) Compound C (Comp C) abolished IPC induced neuroprotection in PC12 cells. Cells were incubated with compound C 5 μM 60 min before the onset of IPC. Twelve hours after IPC, the cells were subjected to OGD for 10 h and cell viability was examined with CCK-8 kit. (B) Compound C reduced LC3II/LC3I ratio. The cells were incubated with compound C 5 μM 60 min before the onset of IPC. Then the cells were harvested 12 h after IPC and subjected to Western blot analysis. Bar represents mean ± SD, n = 3. *P < 0.05, ***P < 0.001 compared with the control group; $$$ P < 0.001 compared with the OGD group; %%% P < 0.001 compared with the IPC + OGD group; # P < 0.05 compared with the IPC group. |
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| S7317 |
WZ4003WZ4003是高特异性的NUAK kinase抑制剂，细胞试验中作用于NUAK1和NUAK2的IC50分别为20 nM和100 nM，对其他139个激酶没有显著抑制作用。 |
Indicated cells were treated with LPS (200 ng/ml) in the absence or presence of indicated AMPK activators (AICAR [100 μM] and A-769662 [2 μM]) or inhibitors (compound C [200 nM] and WZ4003 [100 nM]) for 24 hours. OCR and ECAR were monitored (n=3, *p < 0.05 versus single LPS group).
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| S7318 |
HTH-01-015HTH-01-015 是一种有效的选择性 NUAK1 抑制剂，其IC50 为100 nM，比作用于NUAK2的选择性高100多倍。 |
Mouse BMDMs and human THP1 cells were treated with LPS (200 ng/ml) in the absence or presence of indicated AMPK activators (metformin, quercetin, resveratrol, AICAR, A-769662, and salicylate), AMPK inhibitors (compound C, WZ4003, and HTH-01-015), or HMGB1 inhibitor (glycyrrhizin) for 24 h. HMGB1 release in cell medium was assayed using ELISA kit, respectively (n = 3, *p < .05 versus LPS or Escherichia coli group).
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| S7840 |
Dorsomorphin (Compound C)Dorsomorphin (Compound C)是一种有效的，可逆选择性 AMPK 抑制剂，无细胞试验中 Ki 为 109 nM，对几个结构相关的激酶，包括ZAPK，SYK，PKCθ，PKA，和 JAK3没有显著的抑制作用。 也会抑制 I型 BMP receptor 活性。 |
(A) Cells were pre-treated with 10 ng/ml TGF-β for 24 h, then 5 mM metformin and/or 1 uM (μM) dorsomorphin were added to the medium for another 24 h. Immunofluorescence staining showed that AMPK inhibition abolished metformin's effect of decreasing TGF-β-induced α-actin expression in HFL-1 cells. The nucleus were stained with 4', 6-diamidino-2-phenylindole in the merged images. Scale bars: 150 μm.
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| S2697 |
A-769662A-769662是一种有效的，可逆的AMPK激活剂，在无细胞试验中EC50为0.8 μM，对GPPase/FBPase活性几乎没有作用。 |
Cells were treated with CP, DOXO, SRT1720 (100 nM), EX527 (100 nM), A769662 (10 μM) and Compound C (1 μM) under normoxic or hypoxic conditions for 48 hours, and then their viabilities were measured by MTT. |
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| S1802 |
AICAR (Acadesine)AICAR (Acadesine)是AMPK的激活剂，引起ZMP积累，模拟AMP对AMPK和AMPKK的刺激作用。Phase 3。 |
(E) LDLR blocks the translocation of ALDH2 even AMPK activation. Scale bars: 5 μm.
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| S2542 |
Phenformin HClPhenformin HCl是一种Phenformin的盐酸盐，是一种双胍类的抗糖尿病药。它能激活AMPK，提高其活性和磷酸化。 |
a set of RNAi-resistant rescue forms of Cdc37 plasmids were transfected into stable Cdc37-RNAi HCT116 cells. 24 h after transfection cells were treated with phenformin and then subjected to FLAG immunoprecipitation.
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| S8803New |
MK-3903MK-3903是一种有效的选择性AMPK激活剂，对α1 β1 γ1亚基的EC50值为8 nM。它能激活12种pAMPK复合体中的10种，EC50值在8-40 nM。 |
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| S8654New |
ex229 (compound 991)EX229 (compound 991)是一种有效的AMPK激活剂，其效力是A769662的5-10倍。 |
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| S9096New |
ligustroflavoneLigustroflavone, isolated from the leaves of Turpinia montana, shows high antioxidant capacity and is reported to be an AMPK activator. |
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| S5284New |
Adenosine 5'-monophosphate monohydrateAdenosine 5'-monophosphate monohydrate (5'-AMP) is an activator of a class of protein kinases known as AMP-activated protein kinase (AMPK). |
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| S8335 |
PF-06409577PF-06409577是具有口服活性的AMPK激活剂，在TR-FRET实验中，对AMPK α1β1γ1的EC50为7 nM。在patchBclamp实验中，100μM的PF-06409577对hERG没有可观测到的抑制作用，对主要的人源细胞色素P450亚型的微粒体活性也没有抑制活性（IC50 > 100 μM）。 |
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| S7898 |
GSK621GSK621是一种特异性且有效的AMPK激活剂。 |
GSK621 dose-dependent activation of AMPK in erythroblasts. Western Blot analysis of PT172 AMPKα1, PS79 ACC and PS555 ULK1 in primary erythroblasts incubated for 3 h with increasing doses of GSK621. Anti-HSC70 was used as a loading control.
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| S7953 |
ETC-1002ETC-1002是一种可用于口服、降低LDL-C的小分子，是肝脏AMPK的激活剂。 |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S7306 |
Dorsomorphin (Compound C) 2HClDorsomorphin (Compound C) 2HCl是一种有效的，可逆的，选择性AMPK抑制剂，在无细胞试验中Ki为109 nM，对一些结构相关的激酶，包括ZAPK， SYK， PKCθ，PKA和JAK3没有显著的抑制作用。也会抑制I型BMP受体。 |
AMPK inhibition by compound C(Dorsomorphin) inhibited autophagy activation and neuroprotection induced by IPC in PC12 cells. (A) Compound C (Comp C) abolished IPC induced neuroprotection in PC12 cells. Cells were incubated with compound C 5 μM 60 min before the onset of IPC. Twelve hours after IPC, the cells were subjected to OGD for 10 h and cell viability was examined with CCK-8 kit. (B) Compound C reduced LC3II/LC3I ratio. The cells were incubated with compound C 5 μM 60 min before the onset of IPC. Then the cells were harvested 12 h after IPC and subjected to Western blot analysis. Bar represents mean ± SD, n = 3. *P < 0.05, ***P < 0.001 compared with the control group; $$$ P < 0.001 compared with the OGD group; %%% P < 0.001 compared with the IPC + OGD group; # P < 0.05 compared with the IPC group. |
|
| S7317 |
WZ4003WZ4003是高特异性的NUAK kinase抑制剂，细胞试验中作用于NUAK1和NUAK2的IC50分别为20 nM和100 nM，对其他139个激酶没有显著抑制作用。 |
Indicated cells were treated with LPS (200 ng/ml) in the absence or presence of indicated AMPK activators (AICAR [100 μM] and A-769662 [2 μM]) or inhibitors (compound C [200 nM] and WZ4003 [100 nM]) for 24 hours. OCR and ECAR were monitored (n=3, *p < 0.05 versus single LPS group).
|
|
| S7318 |
HTH-01-015HTH-01-015 是一种有效的选择性 NUAK1 抑制剂，其IC50 为100 nM，比作用于NUAK2的选择性高100多倍。 |
Mouse BMDMs and human THP1 cells were treated with LPS (200 ng/ml) in the absence or presence of indicated AMPK activators (metformin, quercetin, resveratrol, AICAR, A-769662, and salicylate), AMPK inhibitors (compound C, WZ4003, and HTH-01-015), or HMGB1 inhibitor (glycyrrhizin) for 24 h. HMGB1 release in cell medium was assayed using ELISA kit, respectively (n = 3, *p < .05 versus LPS or Escherichia coli group).
|
|
| S7840 |
Dorsomorphin (Compound C)Dorsomorphin (Compound C)是一种有效的，可逆选择性 AMPK 抑制剂，无细胞试验中 Ki 为 109 nM，对几个结构相关的激酶，包括ZAPK，SYK，PKCθ，PKA，和 JAK3没有显著的抑制作用。 也会抑制 I型 BMP receptor 活性。 |
(A) Cells were pre-treated with 10 ng/ml TGF-β for 24 h, then 5 mM metformin and/or 1 uM (μM) dorsomorphin were added to the medium for another 24 h. Immunofluorescence staining showed that AMPK inhibition abolished metformin's effect of decreasing TGF-β-induced α-actin expression in HFL-1 cells. The nucleus were stained with 4', 6-diamidino-2-phenylindole in the merged images. Scale bars: 150 μm.
|
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2697 |
A-769662A-769662是一种有效的，可逆的AMPK激活剂，在无细胞试验中EC50为0.8 μM，对GPPase/FBPase活性几乎没有作用。 |
2017, 19(6):724-731 2016, 12(2):432-8 2014, 74(1):298-308 |
Cells were treated with CP, DOXO, SRT1720 (100 nM), EX527 (100 nM), A769662 (10 μM) and Compound C (1 μM) under normoxic or hypoxic conditions for 48 hours, and then their viabilities were measured by MTT. |
| S1802 |
AICAR (Acadesine)AICAR (Acadesine)是AMPK的激活剂，引起ZMP积累，模拟AMP对AMPK和AMPKK的刺激作用。Phase 3。 |
2018, 10.1172/JCI122064 2015, 10.1111/bph.13120 2014, 111(8):1562-71 |
(E) LDLR blocks the translocation of ALDH2 even AMPK activation. Scale bars: 5 μm.
|
| S2542 |
Phenformin HClPhenformin HCl是一种Phenformin的盐酸盐，是一种双胍类的抗糖尿病药。它能激活AMPK，提高其活性和磷酸化。 |
2017, 292(7):2830-2841 2016, 470(2):453-9 |
a set of RNAi-resistant rescue forms of Cdc37 plasmids were transfected into stable Cdc37-RNAi HCT116 cells. 24 h after transfection cells were treated with phenformin and then subjected to FLAG immunoprecipitation.
|
| S8803New |
MK-3903MK-3903是一种有效的选择性AMPK激活剂，对α1 β1 γ1亚基的EC50值为8 nM。它能激活12种pAMPK复合体中的10种，EC50值在8-40 nM。 |
||
| S8654New |
ex229 (compound 991)EX229 (compound 991)是一种有效的AMPK激活剂，其效力是A769662的5-10倍。 |
||
| S9096New |
ligustroflavoneLigustroflavone, isolated from the leaves of Turpinia montana, shows high antioxidant capacity and is reported to be an AMPK activator. |
||
| S5284New |
Adenosine 5'-monophosphate monohydrateAdenosine 5'-monophosphate monohydrate (5'-AMP) is an activator of a class of protein kinases known as AMP-activated protein kinase (AMPK). |
||
| S8335 |
PF-06409577PF-06409577是具有口服活性的AMPK激活剂，在TR-FRET实验中，对AMPK α1β1γ1的EC50为7 nM。在patchBclamp实验中，100μM的PF-06409577对hERG没有可观测到的抑制作用，对主要的人源细胞色素P450亚型的微粒体活性也没有抑制活性（IC50 > 100 μM）。 |
||
| S7898 |
GSK621GSK621是一种特异性且有效的AMPK激活剂。 |
2016, 11(8):e0161017 2018, 10.3324/haematol.2018.191403 2018, 10.1111/jcmm.13975 |
GSK621 dose-dependent activation of AMPK in erythroblasts. Western Blot analysis of PT172 AMPKα1, PS79 ACC and PS555 ULK1 in primary erythroblasts incubated for 3 h with increasing doses of GSK621. Anti-HSC70 was used as a loading control.
|
| S7953 |
ETC-1002ETC-1002是一种可用于口服、降低LDL-C的小分子，是肝脏AMPK的激活剂。 |
