AMPK
Signaling Pathway Map
Research Area
- Inhibitory Selectivity
- Solubility
| Catalog No. | Product Name | Solubility(25°C) | ||
|---|---|---|---|---|
| Water | DMSO | Alcohol | ||
| 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 Inhibitors (13)
- New AMPK Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S7306 |
Dorsomorphin (Compound C) 2HClDorsomorphin 2HCl is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Also inhibits type Ⅰ BMP receptor activity. |
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 is a highly specific NUAK kinase inhibitor with IC50 of 20 nM and 100 nM for NUAK1 and NUAK2 in cell-base assays, respectively, without significant inhibition on 139 other kinases. |
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 is a potent and selective NUAK1 inhibitor with IC50 of 100 nM, >100-fold selectivity over NUAK2. |
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 is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Also inhibits type I BMP receptor activity. |
(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 is a potent, reversible AMPK activator with EC50 of 0.8 μM in cell-free assays, little effect on GPPase/FBPase activity. |
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), an AMPK activator, results in accumulation of ZMP, which mimics the stimulating effect of AMP on AMPK and AMPK kinase. 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 is a hydrochloride salt of phenformin that is an anti-diabetic drug from the biguanide class. It activates AMPK, increasing activity and phosphorylation. |
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) is a potent AMPK activator that is 5-10-fold more potent than A769662 in activating AMPK. |
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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 is orally bioavailable AMPK activator with EC50 of 7 nM for α1β1γ1 in the TR-FRET assay and it shows no detectable inhibition of hERG in a patch-clamp assay (100 μM) and was not an inhibitor (IC50 > 100 μM) of the microsomal activities of major human cytochrome P450 isoforms. |
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| S7898 |
GSK621GSK621 is a specific and potent AMPK activator. |
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,also known as Bempedoic acid, is an orally available, once-daily LDL-C lowering small molecule designed to lower elevated levels of LDL-C and to avoid side effects associated with existing LDL-C lowering therapies.ETC-1002 is an activator of hepatic AMP-activated protein kinase (AMPK). It has potent inhibitory activity against hepatic ATP-citrate lyase(IC50=29 uM). |
