AMPK
Signaling Pathway Map
Research Area
Inhibitory Selectivity
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. |
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 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. |
(E) LDLR blocks the translocation of ALDH2 even AMPK activation. Scale bars: 5 μm.
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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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| S8803New |
MK-3903MK-3903 is a potent and selective AMPK activator with an EC50 of 8 nM for α1 β1 γ1 subunit. It activates 10 of the 12 pAMPK complexes with EC50 values in the range of 8-40 nM and maximal activation >50%. |
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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. |
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,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). |
| 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. |
|
| 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. |
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 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).
|
|
| 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.
|
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| 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. |
|
| 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. |
(E) LDLR blocks the translocation of ALDH2 even AMPK activation. Scale bars: 5 μm.
|
|
| 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.
|
|
| S8803New |
MK-3903MK-3903 is a potent and selective AMPK activator with an EC50 of 8 nM for α1 β1 γ1 subunit. It activates 10 of the 12 pAMPK complexes with EC50 values in the range of 8-40 nM and maximal activation >50%. |
||
| S8654New |
ex229 (compound 991)EX229 (compound 991) is a potent AMPK activator that is 5-10-fold more potent than A769662 in activating AMPK. |
||
| 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 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. |
||
| S7898 |
GSK621GSK621 is a specific and potent AMPK activator. |
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,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). |
