AMPK

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AMPK Signaling Pathway Map

AMPK Signaling Pathways

AMPK Products

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  • AMPK Activators (34)
  • New AMPK Products
Catalog No. Product Name Information Product Use Citations Product Validations
E0022New Ophiopogonin D Ophiopogonin D (OJV-VI, Deacetylophiopogonin C) is a steroidal glycoside isolated from Chinese herb Radix ophiopogonis and shows anti-tumor property. Ophiopogonin D could suppress TGF-β1-mediated metastatic behavior of MDA-MB-231 cells by regulating ITGB1/FAK/Src/AKT/β-catenin/MMP-9 signaling axis. Ophiopogonin D attenuates PM2.5-induced inflammation via suppressing the AMPK/NF-κB pathway in mouse pulmonary epithelial cells.
S0177 XMD-17-51 XMD-17-51 (XMD17-51) is a potent and highly selective inhibitor of NUAK1.
S1113 GSK690693 GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. GSK690693 affects Unc-51-like autophagy activating kinase 1 (ULK1) activity, robustly inhibits STING-dependent IRF3 activation. Phase 1.
Am J Cancer Res, 2022, 12(4):1535-1555
Cell Death Discov, 2022, 8(1):197
Mech Ageing Dev, 2022, 202:111633
S1208 Doxorubicin (Adriamycin) HCl Doxorubicin (Adriamycin, NSC 123127, DOX, Hydroxydaunorubicin) HCl is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage, mitophagy and apoptosis in tumor cells. Doxorubicin reduces basal phosphorylation of AMPK. Doxorubicin is used in the concomitant treatment of HIV-infected patients but is found to be at high risk of HBV reactivation.
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
Bioact Mater, 2022, 18:459-470
EMBO Mol Med, 2022, 14(2):e14903
S7306 Dorsomorphin (Compound C) 2HCl Dorsomorphin 2HCl (BML-275, Compound C) 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. Dorsomorphin induces autophagy in cancer cell line.
Signal Transduct Target Ther, 2022, 7(1):66
Redox Biol, 2022, 52:102288
Brain Behav Immun, 2022, S0889-1591(22)00041-1
S7317 WZ4003 WZ4003 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.
Mol Cell, 2020, 77(6):1322-1339
Cell Death Dis, 2020, 11(8):712
J Recept Signal Transduct Res, 2020, 1-8
S7318 HTH-01-015 HTH-01-015 is a potent and selective NUAK1 inhibitor with IC50 of 100 nM, >100-fold selectivity over NUAK2.
Mol Cell, 2020, 77(6):1322-1339
Cell Chem Biol, 2019, 10.1016/j.chembiol.2019.10.005
Breast Cancer Res, 2018, 20(1):22
S7840 Dorsomorphin (Compound C) Dorsomorphin (Compound C, BML-275) 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. Dorsomorphin selectively inhibits the BMP type I receptors ALK2, ALK3 and ALK6. Dorsomorphin is used in promoting specific cell differentiation and inducing cancer cell line autophagy. For animal testing, the water-soluble S7306 Dorsomorphin (Compound C) 2HCl is recommended.
Signal Transduct Target Ther, 2022, 7(1):66
Adv Sci (Weinh), 2022, e2105208
Brain Behav Immun, 2022, S0889-1591(22)00041-1
S8161 ON123300 ON123300 is a potent and multi-targeted kinase inhibitor with IC50 of 3.9 nM, 5 nM, 26 nM, 26 nM, 9.2 nM and 11nM for CDK4, Ark5/NUAK1, PDGFRβ, FGFR1, RET (c-RET), and Fyn, respectively.
J Cell Sci, 2021, jcs.258685
Molecules, 2020, 8;25(9) pii: E2220
S8274 STO-609 STO-609 is a specific inhibitor of the Ca2+/Calmodulin-dependent protein kinase kinase(CaM-KK) that inhibits the activities of recombinant CaM-KKα and CaM-KKβ isoforms, with Ki values of 80 and 15 ng/ml, respectively, and also inhibits their autophosphorylation activities. STO-609 inhibits AMPKK activity and inhibits autophagy.
EMBO Rep, 2022, e53373
Cell Res, 2021, 10.1038/s41422-021-00565-y
Autophagy, 2021, 1-14
E0204New Poricoic acid A Poricoic acid A is isolated from the surface layer of Poria cocos. Poricoic acid A activates AMPK to attenuate fibroblast activation and abnormal extracellular matrix remodelling in renal fibrosis. Poricoic acid A also is a modulator of tryptophan hydroxylase-1 (TPH-1).
E0653New Trans-ferulic acid Trans-ferulic acid is a potent activator of AMPKunder high glucose condition.
E1031New MK-8722

MK-8722 is a potent, direct, allosteric activator of all 12 mammalian pan-AMPK complexes.

S0411 BAM 15 BAM 15 is a novel mitochondrial protonophore uncoupler capable of protecting mammals from acute renal ischemic-reperfusion injury and cold-induced microtubule damage. BAM 15 is also a potent AMPK activator. BAM 15 attenuates transportation-induced apoptosis in iPS-differentiated retinal tissue.
Neuroscience, 2012, 223:238-45
S0795 O-304 O-304 (O-304X) is an orally available pan-activator of AMPK activated protein kinase (AMPK). O-304 (O-304X) exhibits a great potential as a novel drug to treat type 2 diabetes (T2D) and associated cardiovascular complications.
Biomed Pharmacother, 2021, 144:112325
S1033 Nilotinib (AMN-107) Nilotinib (AMN-107) is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Cell Rep Med, 2022, 3(1):100492
Cancer Cell, 2021, S1535-6108(21)00659-0
S1273 Amarogentin

Amarogentin (AG), a secoiridoid glycoside mainly extracted from Swertia and Gentiana roots, exhibits anti-oxidative, anti-tumour, and anti-diabetic activities. Amarogentin is an agonist for the bitter taste receptor TAS2R1 and inhibits in LAD-2 cells substance P-induced production of newly synthesized TNF-α. Amarogentin induces apoptosis in human gastric cancer cells (SNU-16) through G2/M cell cycle arrest and PI3K/Akt signalling pathway. Amarogentin (AG) interacts with the α2 subunit of AMP-activated protein kinase (AMPK) and activates the trimeric kinase with EC50 of 277 pM.

S1321 Urolithin B Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα. Urolithin B suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass.
S1323 7-Methoxyisoflavone 7-Methoxyisoflavone (MIF) is a potent activator of adenosine monophosphate-activated protein kinase (AMPK).
S1396 Resveratrol (SRT501) Resveratrol (SRT501, trans-Resveratrol) has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases(LOX, IC50=2.7 μM), kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis.
Int Immunopharmacol, 2022, 103:108489
Eur J Neurosci, 2022, 10.1111/ejn.15596
Adv Sci (Weinh), 2021, e2103360
S1802 AICAR (Acadesine) AICAR (Acadesine, NSC105823, AICA Riboside), an AMPK activator, results in accumulation of ZMP, which mimics the stimulating effect of AMP on AMPK and AMPK kinase. AICAR (Acadesine) induces mitophagy. Phase 3.
Signal Transduct Target Ther, 2022, 7(1):66
Food Funct, 2022, 10.1039/d1fo03752h
Cell Res, 2021, 10.1038/s41422-021-00565-y
S2542 Phenformin (NSC-756501) HCl Phenformin HCl (NSC-756501, Phenethylbiguanide) is a hydrochloride salt of phenformin that is an anti-diabetic drug from the biguanide class. It activates AMPK, increasing activity and phosphorylation.
cell, 2019, 178(5):1102-1114
Nat Commun, 2019, 10(1):3856
Cancers (Basel), 2018, 10(10)E385
S2697 A-769662 A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM in cell-free assays, little effect on GPPase/FBPase activity.
Ecotoxicol Environ Saf, 2022, 236:113467
J Biol Chem, 2022, S0021-9258(22)00292-7
Cell Signal, 2022, S0898-6568(22)00031-6
S2942 EB-3D EB-3D is a potent and selective inhibitor of choline kinase α (ChoKα) with IC50 of 1 μM for ChoKα1. EB-3D induces deregulation of the AMPK-mTOR pathway and apoptosis in leukemia T-cells.
S3296 Hispidulin Hispidulin (Dinatin), an active natrual ingredient in a number of traditional Chinese medicinal herbs, exhibits inhibitory activity against the oncogenic protein kinase Pim-1 with IC50 of 2.71 μM. Hispidulin induces apoptosis through mitochondrial dysfunction and inhibition of P13k/Akt signalling pathway in HepG2 cancer cells. Hispidulin exerts anti-osteoporotic and bone resorption attenuating effects via activating the AMPK signaling pathway.
S3299 Demethyleneberberine Demethyleneberberine (DMB), a component of Cortex Phellodendri Chinensis (CPC), significantly alleviates the weight loss and diminishes myeloperoxidase (MPO) activity, while significantly reduces the production of pro-inflammatory cytokines, such as interleukin (IL)-6 and tumor necrosis factor-α (TNF-α), and inhibits the activation of NF-κB signaling pathway. Demethyleneberberine (DMB) potentially ameliorates NAFLD (Non-alcoholic fatty liver disease) by activating AMPK pathways.
S3341 Palmitoleic acid

Palmitoleic acid (POA, Palmitoleate) stimulates the uptake of glucose in liver through activation of AMPK and FGF-21, dependent on PPARα.

S3832 Euphorbiasteroid Euphorbiasteroid (Euphorbia factor L1), a component of Euphorbia lathyris L., inhibits adipogenesis of 3T3-L1 cells through activation of the AMPK pathway and induces HL-60 cells to apoptosis via promoting Bcl-2/Bax apoptotic signaling pathway in a dose-dependent manner. Euphorbiasteroid is a tricyclic diperpene of Euphorbia lathyris L., inhibits tyrosinase, and increases the phosphorylation of AMPK, with anti-cancer, anti-virus, anti-obesity and multidrug resistance-modulating effect.
S4460 IMM-H007 IMM-H007, an adenosine derivative, is an activator of AMP-Activated Protein Kinase (AMPK). IMM-H007 is a potential drug for treating cardiac dysfunction. IMM-H007 negatively regulates endothelium inflammation through inactivating NF-κB and JNK/AP1 signaling. IMM-H007 inhibits ABCA1 (ATP binding cassette subfamily a member 1) degradation and facilitates its cell-surface localization in macrophages, thereby promotes cholesterol efflux.
S4561 Danthron Danthron (Chrysazin, Antrapurol) functions in regulating glucose and lipid metabolism by activating AMPK. Danthron is a natural product extracted from the traditional Chinese medicine rhubarb. Danthron used to be a laxativa and now is currently used as an antioxidant in synthetic lubricants, in the synthesis of experimental antitumor agents, as a fungicide and as an intermediate for making dyes.
Biomed Pharmacother, 2021, 144:112325
S4895 Nilotinib hydrochloride monohydrate Nilotinib (AMN-107, Tasigna) hydrochloride monohydrate is a selective and orally bioavailable inhibitor of Bcr-Abl with IC50 < 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition.
EMBO Mol Med, 2021, e11814
Mol Metab, 2021, 55:101410
Cancers (Basel), 2021, 13(21)5543
S5284 Adenosine 5'-monophosphate monohydrate Adenosine 5'-monophosphate monohydrate (5'-Adenylic acid, 5'-AMP) is an activator of a class of protein kinases known as AMP-activated protein kinase (AMPK).
S5958 Metformin Metformin (1,1-Dimethylbiguanide), a widely used drug for treatment of type 2 diabetes, activates AMP-activated protein kinase (AMPK) in hepatocytes. Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153.
Front Mol Biosci, 2022, 9:780200
Cell Death Discov, 2022, 8(1):204
Int Immunopharmacol, 2022, 108:108683
S6221 Methyl cinnamate Methyl cinnamate, an active component of Zanthoxylum armatum, is a widely used natural flavor compound with antimicrobial and tyrosinase inhibitor activities. Methyl Cinnamate Inhibits Adipocyte Differentiation via Activation of the CaMKK2--AMPK Pathway in 3T3-L1 Preadipocytes.
S7898 GSK621 GSK621 is a specific and potent AMPK activator.
Cell Rep, 2022, 38(1):110197
Cell Death Dis, 2021, 13(1):1
Front Physiol, 2021, 12:657378
S7953 ETC-1002 ETC-1002 (Bempedoic acid, ESP-55016),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).
Biomed Pharmacother, 2021, 144:112325
J Cell Mol Med, 2020, 25
S8335 PF-06409577 PF-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.
S8654 ex229 (compound 991) EX229 (compound 991) is a potent AMPK activator that is 5-10-fold more potent than A769662 in activating AMPK.
Cell Rep, 2019, 29(10):3331-3348
CHINESE JOURNAL OF COMPARATIVE MEDICINE, 2019, 29(12): 39-44
S8803 MK-3903 MK-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%.
Biomed Pharmacother, 2021, 144:112325
S8953 ASP4132 ASP4132 is a potent and orally active activator of Adenosine Monophosphate-Activated Protein Kinase (AMPK) with EC50 of 0.018 μM. ASP4132 is used as a clinical candidate for the treatment of human cancer.
S9096 ligustroflavone Ligustroflavone (Nuezhenoside), isolated from the leaves of Turpinia montana, shows high antioxidant capacity and is reported to be an AMPK activator.
S9116 Chikusetsusaponin IVa Chikusetsusaponin IVa (Calenduloside F), a major active ingredient of triterpenoid saponins, has numerous pharmacological activities, including cytotoxic activity against various cancer cells, anti-inflammatory activity, prevention of dental caries and induction of genta-micin nephrotoxicity. Chikusetsusaponin IVa is a novel AMPK activator.
S9604 IM156 IM156 (HL156A), a metformin derivative, is a potent activator of AMPK that increases AMPK phosphorylation. IM156 blocks oxidative phosphorylation (OXPHOS) through the inhibition of complex I and increases apoptosis. IM156 ameliorates various types of fibrosis and inhibits tumors.
S9860 BC1618 BC1618 is an orally active Fbxo48 inhibitor that stimulates adenosine monophosphate (AMP)-activated protein kinase (Ampk)-dependent signaling. BC1618 promotes mitochondrial fission, facilitates autophagy and improves hepatic insulin sensitivity.
E0022New Ophiopogonin D Ophiopogonin D (OJV-VI, Deacetylophiopogonin C) is a steroidal glycoside isolated from Chinese herb Radix ophiopogonis and shows anti-tumor property. Ophiopogonin D could suppress TGF-β1-mediated metastatic behavior of MDA-MB-231 cells by regulating ITGB1/FAK/Src/AKT/β-catenin/MMP-9 signaling axis. Ophiopogonin D attenuates PM2.5-induced inflammation via suppressing the AMPK/NF-κB pathway in mouse pulmonary epithelial cells.
S0177 XMD-17-51 XMD-17-51 (XMD17-51) is a potent and highly selective inhibitor of NUAK1.
S1113 GSK690693 GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. GSK690693 affects Unc-51-like autophagy activating kinase 1 (ULK1) activity, robustly inhibits STING-dependent IRF3 activation. Phase 1.
Am J Cancer Res, 2022, 12(4):1535-1555
Cell Death Discov, 2022, 8(1):197
Mech Ageing Dev, 2022, 202:111633
S1208 Doxorubicin (Adriamycin) HCl Doxorubicin (Adriamycin, NSC 123127, DOX, Hydroxydaunorubicin) HCl is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage, mitophagy and apoptosis in tumor cells. Doxorubicin reduces basal phosphorylation of AMPK. Doxorubicin is used in the concomitant treatment of HIV-infected patients but is found to be at high risk of HBV reactivation.
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
Bioact Mater, 2022, 18:459-470
EMBO Mol Med, 2022, 14(2):e14903
S7306 Dorsomorphin (Compound C) 2HCl Dorsomorphin 2HCl (BML-275, Compound C) 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. Dorsomorphin induces autophagy in cancer cell line.
Signal Transduct Target Ther, 2022, 7(1):66
Redox Biol, 2022, 52:102288
Brain Behav Immun, 2022, S0889-1591(22)00041-1
S7317 WZ4003 WZ4003 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.
Mol Cell, 2020, 77(6):1322-1339
Cell Death Dis, 2020, 11(8):712
J Recept Signal Transduct Res, 2020, 1-8
S7318 HTH-01-015 HTH-01-015 is a potent and selective NUAK1 inhibitor with IC50 of 100 nM, >100-fold selectivity over NUAK2.
Mol Cell, 2020, 77(6):1322-1339
Cell Chem Biol, 2019, 10.1016/j.chembiol.2019.10.005
Breast Cancer Res, 2018, 20(1):22
S7840 Dorsomorphin (Compound C) Dorsomorphin (Compound C, BML-275) 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. Dorsomorphin selectively inhibits the BMP type I receptors ALK2, ALK3 and ALK6. Dorsomorphin is used in promoting specific cell differentiation and inducing cancer cell line autophagy. For animal testing, the water-soluble S7306 Dorsomorphin (Compound C) 2HCl is recommended.
Signal Transduct Target Ther, 2022, 7(1):66
Adv Sci (Weinh), 2022, e2105208
Brain Behav Immun, 2022, S0889-1591(22)00041-1
S8161 ON123300 ON123300 is a potent and multi-targeted kinase inhibitor with IC50 of 3.9 nM, 5 nM, 26 nM, 26 nM, 9.2 nM and 11nM for CDK4, Ark5/NUAK1, PDGFRβ, FGFR1, RET (c-RET), and Fyn, respectively.
J Cell Sci, 2021, jcs.258685
Molecules, 2020, 8;25(9) pii: E2220
S8274 STO-609 STO-609 is a specific inhibitor of the Ca2+/Calmodulin-dependent protein kinase kinase(CaM-KK) that inhibits the activities of recombinant CaM-KKα and CaM-KKβ isoforms, with Ki values of 80 and 15 ng/ml, respectively, and also inhibits their autophosphorylation activities. STO-609 inhibits AMPKK activity and inhibits autophagy.
EMBO Rep, 2022, e53373
Cell Res, 2021, 10.1038/s41422-021-00565-y
Autophagy, 2021, 1-14
E0204New Poricoic acid A Poricoic acid A is isolated from the surface layer of Poria cocos. Poricoic acid A activates AMPK to attenuate fibroblast activation and abnormal extracellular matrix remodelling in renal fibrosis. Poricoic acid A also is a modulator of tryptophan hydroxylase-1 (TPH-1).
E0653New Trans-ferulic acid Trans-ferulic acid is a potent activator of AMPKunder high glucose condition.
E1031New MK-8722

MK-8722 is a potent, direct, allosteric activator of all 12 mammalian pan-AMPK complexes.

S0411 BAM 15 BAM 15 is a novel mitochondrial protonophore uncoupler capable of protecting mammals from acute renal ischemic-reperfusion injury and cold-induced microtubule damage. BAM 15 is also a potent AMPK activator. BAM 15 attenuates transportation-induced apoptosis in iPS-differentiated retinal tissue.
Neuroscience, 2012, 223:238-45
S0795 O-304 O-304 (O-304X) is an orally available pan-activator of AMPK activated protein kinase (AMPK). O-304 (O-304X) exhibits a great potential as a novel drug to treat type 2 diabetes (T2D) and associated cardiovascular complications.
Biomed Pharmacother, 2021, 144:112325
S1033 Nilotinib (AMN-107) Nilotinib (AMN-107) is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Cell Rep Med, 2022, 3(1):100492
Cancer Cell, 2021, S1535-6108(21)00659-0
S1273 Amarogentin

Amarogentin (AG), a secoiridoid glycoside mainly extracted from Swertia and Gentiana roots, exhibits anti-oxidative, anti-tumour, and anti-diabetic activities. Amarogentin is an agonist for the bitter taste receptor TAS2R1 and inhibits in LAD-2 cells substance P-induced production of newly synthesized TNF-α. Amarogentin induces apoptosis in human gastric cancer cells (SNU-16) through G2/M cell cycle arrest and PI3K/Akt signalling pathway. Amarogentin (AG) interacts with the α2 subunit of AMP-activated protein kinase (AMPK) and activates the trimeric kinase with EC50 of 277 pM.

S1321 Urolithin B Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα. Urolithin B suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass.
S1323 7-Methoxyisoflavone 7-Methoxyisoflavone (MIF) is a potent activator of adenosine monophosphate-activated protein kinase (AMPK).
S1396 Resveratrol (SRT501) Resveratrol (SRT501, trans-Resveratrol) has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases(LOX, IC50=2.7 μM), kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis.
Int Immunopharmacol, 2022, 103:108489
Eur J Neurosci, 2022, 10.1111/ejn.15596
Adv Sci (Weinh), 2021, e2103360
S1802 AICAR (Acadesine) AICAR (Acadesine, NSC105823, AICA Riboside), an AMPK activator, results in accumulation of ZMP, which mimics the stimulating effect of AMP on AMPK and AMPK kinase. AICAR (Acadesine) induces mitophagy. Phase 3.
Signal Transduct Target Ther, 2022, 7(1):66
Food Funct, 2022, 10.1039/d1fo03752h
Cell Res, 2021, 10.1038/s41422-021-00565-y
S2542 Phenformin (NSC-756501) HCl Phenformin HCl (NSC-756501, Phenethylbiguanide) is a hydrochloride salt of phenformin that is an anti-diabetic drug from the biguanide class. It activates AMPK, increasing activity and phosphorylation.
cell, 2019, 178(5):1102-1114
Nat Commun, 2019, 10(1):3856
Cancers (Basel), 2018, 10(10)E385
S2697 A-769662 A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM in cell-free assays, little effect on GPPase/FBPase activity.
Ecotoxicol Environ Saf, 2022, 236:113467
J Biol Chem, 2022, S0021-9258(22)00292-7
Cell Signal, 2022, S0898-6568(22)00031-6
S2942 EB-3D EB-3D is a potent and selective inhibitor of choline kinase α (ChoKα) with IC50 of 1 μM for ChoKα1. EB-3D induces deregulation of the AMPK-mTOR pathway and apoptosis in leukemia T-cells.
S3296 Hispidulin Hispidulin (Dinatin), an active natrual ingredient in a number of traditional Chinese medicinal herbs, exhibits inhibitory activity against the oncogenic protein kinase Pim-1 with IC50 of 2.71 μM. Hispidulin induces apoptosis through mitochondrial dysfunction and inhibition of P13k/Akt signalling pathway in HepG2 cancer cells. Hispidulin exerts anti-osteoporotic and bone resorption attenuating effects via activating the AMPK signaling pathway.
S3299 Demethyleneberberine Demethyleneberberine (DMB), a component of Cortex Phellodendri Chinensis (CPC), significantly alleviates the weight loss and diminishes myeloperoxidase (MPO) activity, while significantly reduces the production of pro-inflammatory cytokines, such as interleukin (IL)-6 and tumor necrosis factor-α (TNF-α), and inhibits the activation of NF-κB signaling pathway. Demethyleneberberine (DMB) potentially ameliorates NAFLD (Non-alcoholic fatty liver disease) by activating AMPK pathways.
S3341 Palmitoleic acid

Palmitoleic acid (POA, Palmitoleate) stimulates the uptake of glucose in liver through activation of AMPK and FGF-21, dependent on PPARα.

S3832 Euphorbiasteroid Euphorbiasteroid (Euphorbia factor L1), a component of Euphorbia lathyris L., inhibits adipogenesis of 3T3-L1 cells through activation of the AMPK pathway and induces HL-60 cells to apoptosis via promoting Bcl-2/Bax apoptotic signaling pathway in a dose-dependent manner. Euphorbiasteroid is a tricyclic diperpene of Euphorbia lathyris L., inhibits tyrosinase, and increases the phosphorylation of AMPK, with anti-cancer, anti-virus, anti-obesity and multidrug resistance-modulating effect.
S4460 IMM-H007 IMM-H007, an adenosine derivative, is an activator of AMP-Activated Protein Kinase (AMPK). IMM-H007 is a potential drug for treating cardiac dysfunction. IMM-H007 negatively regulates endothelium inflammation through inactivating NF-κB and JNK/AP1 signaling. IMM-H007 inhibits ABCA1 (ATP binding cassette subfamily a member 1) degradation and facilitates its cell-surface localization in macrophages, thereby promotes cholesterol efflux.
S4561 Danthron Danthron (Chrysazin, Antrapurol) functions in regulating glucose and lipid metabolism by activating AMPK. Danthron is a natural product extracted from the traditional Chinese medicine rhubarb. Danthron used to be a laxativa and now is currently used as an antioxidant in synthetic lubricants, in the synthesis of experimental antitumor agents, as a fungicide and as an intermediate for making dyes.
Biomed Pharmacother, 2021, 144:112325
S4895 Nilotinib hydrochloride monohydrate Nilotinib (AMN-107, Tasigna) hydrochloride monohydrate is a selective and orally bioavailable inhibitor of Bcr-Abl with IC50 < 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition.
EMBO Mol Med, 2021, e11814
Mol Metab, 2021, 55:101410
Cancers (Basel), 2021, 13(21)5543
S5284 Adenosine 5'-monophosphate monohydrate Adenosine 5'-monophosphate monohydrate (5'-Adenylic acid, 5'-AMP) is an activator of a class of protein kinases known as AMP-activated protein kinase (AMPK).
S5958 Metformin Metformin (1,1-Dimethylbiguanide), a widely used drug for treatment of type 2 diabetes, activates AMP-activated protein kinase (AMPK) in hepatocytes. Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153.
Front Mol Biosci, 2022, 9:780200
Cell Death Discov, 2022, 8(1):204
Int Immunopharmacol, 2022, 108:108683
S6221 Methyl cinnamate Methyl cinnamate, an active component of Zanthoxylum armatum, is a widely used natural flavor compound with antimicrobial and tyrosinase inhibitor activities. Methyl Cinnamate Inhibits Adipocyte Differentiation via Activation of the CaMKK2--AMPK Pathway in 3T3-L1 Preadipocytes.
S7898 GSK621 GSK621 is a specific and potent AMPK activator.
Cell Rep, 2022, 38(1):110197
Cell Death Dis, 2021, 13(1):1
Front Physiol, 2021, 12:657378
S7953 ETC-1002 ETC-1002 (Bempedoic acid, ESP-55016),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).
Biomed Pharmacother, 2021, 144:112325
J Cell Mol Med, 2020, 25
S8335 PF-06409577 PF-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.
S8654 ex229 (compound 991) EX229 (compound 991) is a potent AMPK activator that is 5-10-fold more potent than A769662 in activating AMPK.
Cell Rep, 2019, 29(10):3331-3348
CHINESE JOURNAL OF COMPARATIVE MEDICINE, 2019, 29(12): 39-44
S8803 MK-3903 MK-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%.
Biomed Pharmacother, 2021, 144:112325
S8953 ASP4132 ASP4132 is a potent and orally active activator of Adenosine Monophosphate-Activated Protein Kinase (AMPK) with EC50 of 0.018 μM. ASP4132 is used as a clinical candidate for the treatment of human cancer.
S9096 ligustroflavone Ligustroflavone (Nuezhenoside), isolated from the leaves of Turpinia montana, shows high antioxidant capacity and is reported to be an AMPK activator.
S9116 Chikusetsusaponin IVa Chikusetsusaponin IVa (Calenduloside F), a major active ingredient of triterpenoid saponins, has numerous pharmacological activities, including cytotoxic activity against various cancer cells, anti-inflammatory activity, prevention of dental caries and induction of genta-micin nephrotoxicity. Chikusetsusaponin IVa is a novel AMPK activator.
S9604 IM156 IM156 (HL156A), a metformin derivative, is a potent activator of AMPK that increases AMPK phosphorylation. IM156 blocks oxidative phosphorylation (OXPHOS) through the inhibition of complex I and increases apoptosis. IM156 ameliorates various types of fibrosis and inhibits tumors.
S9860 BC1618 BC1618 is an orally active Fbxo48 inhibitor that stimulates adenosine monophosphate (AMP)-activated protein kinase (Ampk)-dependent signaling. BC1618 promotes mitochondrial fission, facilitates autophagy and improves hepatic insulin sensitivity.
E0022New Ophiopogonin D Ophiopogonin D (OJV-VI, Deacetylophiopogonin C) is a steroidal glycoside isolated from Chinese herb Radix ophiopogonis and shows anti-tumor property. Ophiopogonin D could suppress TGF-β1-mediated metastatic behavior of MDA-MB-231 cells by regulating ITGB1/FAK/Src/AKT/β-catenin/MMP-9 signaling axis. Ophiopogonin D attenuates PM2.5-induced inflammation via suppressing the AMPK/NF-κB pathway in mouse pulmonary epithelial cells.
E0204New Poricoic acid A Poricoic acid A is isolated from the surface layer of Poria cocos. Poricoic acid A activates AMPK to attenuate fibroblast activation and abnormal extracellular matrix remodelling in renal fibrosis. Poricoic acid A also is a modulator of tryptophan hydroxylase-1 (TPH-1).
E0653New Trans-ferulic acid Trans-ferulic acid is a potent activator of AMPKunder high glucose condition.
E1031New MK-8722

MK-8722 is a potent, direct, allosteric activator of all 12 mammalian pan-AMPK complexes.

Tags: AMPK inhibition | AMPK activation | AMPK phosphorylation | AMPK activity | AMP-activated protein kinase pathway | AMPK activity assay | AMPK activators review | AMPK activity assay | AMPK inhibitor cancer | AMPK agonists | AMPK antagonist | AMPK inhibitor review