AMPK
信号通路图
研究领域
- 抑制剂选择性比较
- 溶解性比较
| 目录号 | 产品目录 | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | 酒精 | ||
| S7306 | Dorsomorphin (Compound C) 2HCl | 94 mg/mL | <1 mg/mL | <1 mg/mL |
| S7317 | WZ4003 | <1 mg/mL | 7 mg/mL | <1 mg/mL |
| S7318 | HTH-01-015 | <1 mg/mL | 58 mg/mL | 30 mg/mL |
| S7840 | Dorsomorphin (Compound C) | <1 mg/mL | 1 mg/mL | 2 mg/mL |
| S2697 | A-769662 | <1 mg/mL | 72 mg/mL | <1 mg/mL |
| S1802 | AICAR (Acadesine) | <1 mg/mL | 51 mg/mL | <1 mg/mL |
| S2542 | Phenformin HCl | 48 mg/mL | 48 mg/mL | 12 mg/mL |
| S8654 | ex229 (compound 991) | <1 mg/mL | 12 mg/mL | <1 mg/mL |
| S9096 | ligustroflavone | 100 mg/mL | ||
| S5284 | Adenosine 5'-monophosphate monohydrate | -1 mg/mL | 9 mg/mL | -1 mg/mL |
| S8335 | PF-06409577 | <1 mg/mL | 68 mg/mL | 68 mg/mL |
| S7898 | GSK621 | <1 mg/mL | 97 mg/mL | <1 mg/mL |
| S7953 | ETC-1002 | <1 mg/mL | 68 mg/mL | <1 mg/mL |
- AMPK抑制剂（13）
- 新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。 |
The AMPK inhibitor, WZ4003, and the p38 MAPK inhibitor, SB203580, could inhibit the APN-induced overexpression of CXCL1 and CXCL8 and h-JBMMSCs chemotaxis. After treated with WZ4003 and SB203580, the expression of CXCL1 (A and B) and CXCL8 (C and D) in the cells and supernatants of h-JBMMSCs treated with or without APN was evaluated by the ELISA assay (n = 3; *P < 0.05; **P < 0.01) |
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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。 |
Cultured hepatocytes were treated with 10 μM Compound C (Comp.C) for 30 min before treatment with 10 μM SAL, 1 mM AICAR for 3 h. Cell lysates were immunoblotted for the phosphorylation of AMPK, ACC, Akt and GSK3β. *P < 0.05, **P < 0.01 versus control; ##P < 0.01 versus SAL alone; †P < 0.05, ††P < 0.01 versus AICAR alone. Values are means ± SEM (n = 4). |
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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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| 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。 |
Human glioma U87MG cells (A-C) and U251MG cells (D), as well as HCN-1a neuronal cells (D) or primary human astrocytes (“Astrocytes”, D) were either left untreated (“C”) or treated with applied concentrations of GSK621 for indicated periods of time, cell survival was tested by MTT assay (A and D) and clonogenicity assay (B); Cell death was also tested by the trypan blue staining assay (C). Experiments in this figure were repeated four times, and similar results were obtained. Data were presented as mean ± SD. * p <0.05 vs. “C”.
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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。 |
