| S1208 |
Doxorubicin (Adriamycin) Hydrochloride
|
Doxorubicin (DOX) HCl is an antibiotic agent that inhibits human DNA topoisomerase II with IC50 of 2.67 μM. 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.This product may precipitate when dissolved in PBS solution. It is recommended to prepare the stock solution in pure water and dilute with either pure water or saline to obtain the working solution.Doxorubicin (Adriamycin) HCl can be used to induce animal models of kidney disease.
|
-
Cell Res, 2025, 35(6):437-452.
-
Nat Commun, 2025, 16(1):8873
-
Nat Commun, 2025, 16(1):509
|
|
| S7306 |
Dorsomorphin Dihydrochloride
|
Dorsomorphin 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. Dorsomorphin induces autophagy in cancer cell line. |
-
J Clin Invest, 2025, e190215
-
Redox Biol, 2025, 81:103532
-
Redox Biol, 2025, 82:103606
|
|
| S7840 |
Dorsomorphin
|
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. This compound selectively inhibits the BMP type I receptors ALK2, ALK3 and ALK6. It is used in promoting specific cell differentiation and inducing cancer cell line autophagy. For cell testing, the water-soluble S7306 Dorsomorphin (Compound C) 2HCl is recommended. |
-
Theranostics, 2025, 15(12):5931-5952
-
EMBO Mol Med, 2025, 17(10):2735-2761
-
Stem Cell Res Ther, 2025, 16(1):104
|
|
| 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. This compound induces mitophagy. Phase 3. |
-
Nat Commun, 2025, 16(1):8478
-
Theranostics, 2025, 15(15):7567-7583
-
Glia, 2025, 73(11):2253-2272
|
|
| S1033 |
Nilotinib
|
Nilotinib is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells. This compound induces autophagy through AMPK activition. |
-
Blood Adv, 2025, bloodadvances.2024015364
-
Cell Death Discov, 2025, 11(1):62
-
Immunology, 2025, NONE
|
|
| 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. This compound also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. It affects Unc-51-like autophagy activating kinase 1 (ULK1) activity, robustly inhibits STING-dependent IRF3 activation. Phase 1. |
-
Theranostics, 2025, 15(18):9819-9837
-
Cell Rep, 2025, 44(7):115947
-
Front Cell Infect Microbiol, 2025, 15:1543186
|
|
| S1950 |
Metformin Hydrochloride
|
Metformin Hydrochloride (1,1-Dimethylbiguanide Hydrochloride) is a highly effective Antihyperglycemic Agent, which primarily decreases hyperglycemia in hepatocytes by suppressing hepatic gluconeogenesis (glucose production by the liver). It also promotes mitophagy in mononuclear cells and induces apoptosis of lung cancer cells through activating the JNK/p38 MAPK pathway and GADD153.
|
-
mBio, 2025, e0063425
-
Placenta, 2025, 165:50-61
-
Sci Adv, 2025, 11(17):eads1875
|
|
| 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. |
-
FEBS J, 2025, 10.1111/febs.70247
-
Arch Biochem Biophys, 2025, 769:110433
-
J Clin Invest, 2024, 134(22)e181314
|
|
| S1396 |
Resveratrol
|
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. This compound induces mitophagy/autophagy and autophagy-dependent apoptosis. |
-
Aging Cell, 2025, e70075
-
Biomed Pharmacother, 2025, 190:118393
-
Breast Cancer Res, 2025, 27(1):186
|
|
| S5958 |
Metformin
|
Metformin (1,1-Dimethylbiguanide), a widely used drug for treatment of type 2 diabetes, activates AMP-activated protein kinase (AMPK) in hepatocytes. This compound promotes mitophagy in mononuclear cells. It induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153. |
-
Signal Transduct Target Ther, 2025, 10(1):271
-
Theranostics, 2025, 15(17):9029-9046
-
Int J Biol Sci, 2025, 21(9):4231-4251
|
|
| 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. This compound inhibits AMPKK activity and inhibits autophagy. |
-
Redox Rep, 2025, 30(1):2447721
-
PLoS One, 2025, 20(8):e0330282
-
Cell Genom, 2025, 5(3):100782
|
|
| S7898 |
GSK621
|
GSK621 is a specific and potent AMPK activator. |
-
Front Pharmacol, 2024, 15:1453647
-
Sci Rep, 2024, 14(1):5205
-
Nat Commun, 2023, 14(1):2994
|
|
| 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. |
-
Cell Rep, 2024, 43(7):114446
-
Int J Mol Sci, 2024, 25(3):1411.
-
Int J Mol Sci, 2024, 25(3)1411
|
|
| 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. |
-
Nat Commun, 2024, 15(1):2089
-
J Pharm Sci, 2022, 111(8):2180-2190
-
EMBO Mol Med, 2021, e11814
|
|
| S8654 |
ex229 (compound 991)
|
A potent AMPK activator that is 5-10-fold more potent than A769662 in activating AMPK, EX229 (compound 991) is this compound. |
-
Neuron, 2025, S0896-6273(25)00247-8
-
Autophagy, 2024, 1-24.
-
bioRxiv, 2024, 2024.09.26.615290
|
|
| S2542 |
Phenformin HCl
|
Phenformin HCl is a hydrochloride salt of phenformin that is an anti-diabetic drug from the biguanide class. It activates AMPK, increasing activity and phosphorylation. |
-
Nat Commun, 2024, 15(1):1721
-
BMC Cancer, 2024, 24(1):116
-
bioRxiv, 2024, 2024.09.16.613317
|
|
| 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
|
|
| S7953 |
Bempedoic acid (ETC-1002)
|
Bempedoic acid (ETC-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. It is an activator of hepatic AMP-activated protein kinase (AMPK) and has potent inhibitory activity against hepatic ATP-citrate lyase(IC50=29 uM). |
-
Cancer Cell, 2025, 43(4):776-796.e14
-
iScience, 2023, 26(12):108532
-
Oncol Rep, 2023, 49(2)32
|
|
| 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. |
-
Cell Rep Med, 2025, S2666-3791(25)00231-9
-
Cell Rep, 2024, 43(7):114446
-
J Cell Sci, 2021, jcs.258685
|
|
| S9833 |
BAY-3827
|
BAY-3827 is a potent AMPK inhibitor which inhibits AMPK kinase activity with IC50 values of 1.4 nM at a low, 10 μM ATP concentration and 15 nM at a high, 2 mM ATP concentration. |
-
Int J Mol Sci, 2025, 26(15)7624
-
Mol Neurobiol, 2025, 62(10):13786-13806
-
Autophagy, 2024, 1-24.
|
|
| 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. This compound induces apoptosis through mitochondrial dysfunction and inhibition of P13k/Akt signalling pathway in HepG2 cancer cells. It exerts anti-osteoporotic and bone resorption attenuating effects via activating the AMPK signaling pathway. |
-
Evid Based Complement Alternat Med, 2023, 2023:9428241
|
|
| S0795 |
O-304
|
O-304 (O-304X) is an orally available pan-activator of AMPK activated protein kinase (AMPK). This compound exhibits a great potential as a novel drug to treat type 2 diabetes (T2D) and associated cardiovascular complications. |
-
Front Pharmacol, 2024, 15:1457817
-
Biomed Pharmacother, 2021, 144:112325
|
|
| 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
|
|
| 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. This compound is also a potent AMPK activator. It attenuates transportation-induced apoptosis in iPS-differentiated retinal tissue. |
-
Neuroscience, 2012, 223:238-45
|
|
| S4561 |
Danthron
|
Danthron (Chrysazin, Antrapurol) functions in regulating glucose and lipid metabolism by activating AMPK. This compound is a natural product extracted from the traditional Chinese medicine rhubarb. It 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
|
|
| F0269 |
AMPKα Antibody [G6M15]
|
5'-AMP-activated protein kinase catalytic subunit alpha-1, AMPK subunit alpha-1, Acetyl-CoA carboxylase kinase, ACACA kinase, Hydroxymethylglutaryl-CoA reductase kinase, HMGCR kinase, Tau-protein kinase PRKAA1, PRKAA1, AMPK1, 5'-AMP-activated protein kinase catalytic subunit alpha-2, AMPK subunit alpha-2, PRKAA2, AMPK2 |
|
|
| F0591 |
Phospho-AMPKα1 (Ser485) Antibody [E13G1]
|
|
|
|
| F1561 |
Phospho-AMPK α1/α2 (Thr183/172) Antibody [C21K7]
|
|
|
|
| F2859New |
AMPK α1 Antibody [A7G1]
|
|
|
|
| F0371 |
AMPKβ1/2 Antibody [G1M7]
|
5'-AMP-activated protein kinase subunit beta-1, AMPK beta-1, AMPK β-1, AMPKb, AMPK beta-2, AMPK β-2, PRKAB1, AMPK, PRKAB2, AMPK subunit beta-1, 5'-AMP-activated protein kinase subunit beta-2, AMPK subunit beta-2 |
|
|
| F1072 |
AMPK β1 Antibody [N21N14]
|
AMPK beta 1,AMPKβ1 |
|
|
| F2393New |
AMPK α2 Antibody [H3J11]
|
AMPK alpha 2,AMPKα2 |
|
|
| 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). |
|
|
| S8335 |
PF-06409577
|
PF-06409577 is an 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. |
|
|
| E1031 |
MK-8722
|
MK-8722 is a potent, direct, allosteric activator of all 12 mammalian pan-AMPK complexes. |
-
Mol Cell, 2024, S1097-2765(24)00865-7
|
|
| E2032 |
MOTS-c
|
MOTS-c, a mitochondria-derived peptide (MDP), exerts antinociceptive and anti-inflammatory effects through activating AMPK pathway and inhibiting MAP kinases-c-fos signaling pathway. |
|
|
| E3652 |
Rehmanniae radix praeparata Extract
|
Rehmanniae radix praeparata Extract is extracted from Rehmanniae radix praeparata, which can improve diabetes through AMPK-mediated NF-κB/NLRP3 signaling pathway. |
|
|
| E2371 |
YLF-466D
|
YLF-466D is an AMPK activator that inhibits platelet aggregation. |
|
|
| 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. This compound 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. |
|
|
| S8953 |
ASP4132
|
ASP4132 is a potent and orally active activator of Adenosine Monophosphate-Activated Protein Kinase (AMPK) with EC50 of 0.018 μM. This compound is used as a clinical candidate for the treatment of human cancer. |
|
|
| E2818 |
MARK4 inhibitor 1
|
MARK4 inhibitor 1 is a potent microtubule affinity-regulating kinase 4 (MARK4) inhibitor, with an IC50 of 1.54 μM for MARK4 inhibition assay. |
|
|
| E0022 |
Ophiopogonin D
|
Ophiopogonin D (OJV-VI, Deacetylophiopogonin C) is a steroidal glycoside isolated from Chinese herb Radix ophiopogonis and shows anti-tumor property. This compound could suppress TGF-β1-mediated metastatic behavior of MDA-MB-231 cells by regulating ITGB1/FAK/Src/AKT/β-catenin/MMP-9 signaling axis. It also attenuates PM2.5-induced inflammation via suppressing the AMPK/NF-κB pathway in mouse pulmonary epithelial cells. |
|
|
| E5784New |
AICAR phosphate
|
|
|
|
| E0653 |
Trans-ferulic acid
|
Trans-ferulic acid is a potent activator of AMPK under high glucose condition. |
|
|
| E3041 |
Alpiniae Katsumadai Extract
|
Alpiniae Katsumadai Extract is extracted from Alpiniae Katsumadai, which can induce growth inhibition and autophagy‑related apoptosis by regulating the AMPK and Akt/mTOR/p70S6K signaling pathways in cancer cells. |
|
|
| E0795 |
COH-SR4
|
COH-SR4 suppresses adipogenesis in 3T3-L1 cells through indirect activation of AMPK and downstream modulation of the Mammalian target of rapamycin complex 1 (mTORC1) signaling pathway, which blocks important regulators involved in protein synthesis, cell cycle progression, and expression of key transcription factors and their target adipogenic genes involved in lipid synthesis. |
|
|
| E1323New |
Aldometanib
|
Aldometanib (LXY-05-029) is a selective inhibitor of aldolase (ALDOA) with an IC50 of 50 uM in in vitro enzymatic assays. It also activates lysosomal AMPK by blocking FBP-aldolase binding, mimicking glucose starvation and improving metabolic health without causing hypoglycemia. |
|
|
| S3341 |
Palmitoleic acid
|
Palmitoleic acid (POA, Palmitoleate) stimulates the uptake of glucose in liver through activation of AMPK and FGF-21, dependent on PPARα. |
|
|
| S9096 |
ligustroflavone
|
Ligustroflavone (Nuezhenoside), isolated from the leaves of Turpinia montana, shows high antioxidant capacity and is reported to be an AMPK activator. |
|
|
| S0177 |
XMD-17-51
|
XMD-17-51 (XMD17-51) is a potent and highly selective inhibitor of NUAK1. |
|
|
| S2942 |
EB-3D
|
EB-3D is a potent and selective inhibitor of choline kinase α (ChoKα) with IC50 of 1 μM for ChoKα1. This compound induces deregulation of the AMPK-mTOR pathway and apoptosis in leukemia T-cells. |
|
|
| S9860 |
BC1618
|
BC1618 is an orally active Fbxo48 inhibitor that stimulates adenosine monophosphate (AMP)-activated protein kinase (Ampk)-dependent signaling. This compound promotes mitochondrial fission, facilitates autophagy and improves hepatic insulin sensitivity. |
|
|
| S4460 |
IMM-H007
|
IMM-H007, an adenosine derivative, is an activator of AMP-Activated Protein Kinase (AMPK). This compound is a potential drug for treating cardiac dysfunction. It negatively regulates endothelium inflammation through inactivating NF-κB and JNK/AP1 signaling. This chemical inhibits ABCA1 (ATP binding cassette subfamily a member 1) degradation and facilitates its cell-surface localization in macrophages, thereby promotes cholesterol efflux. |
|
|
| S9604 |
Lixumistat (IM156)
|
Lixumistat (IM156) is a potent activator of AMPK that increases AMPK phosphorylation. It blocks oxidative phosphorylation (OXPHOS) through the inhibition of complex I and increases apoptosis. This compound ameliorates various types of fibrosis and inhibits tumors. |
-
bioRxiv, 2024, 2024.09.16.613317
|
|
| 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. This compound is a novel AMPK activator. |
|
|
| E0204 |
Poricoic acid A
|
Poricoic acid A is isolated from the surface layer of Poria cocos. This compound activates AMPK to attenuate fibroblast activation and abnormal extracellular matrix remodelling in renal fibrosis. It also is a modulator of tryptophan hydroxylase-1 (TPH-1). |
|
|
| S0888 |
Rsva 405
|
Rsva 405, a novel small-molecule activator of AMPK, is a potent inhibitor of adipogenesis and thus may have therapeutic potential against obesity. |
|
|
| E2661 |
Chitosan oligosaccharide
|
Chitosan oligosaccharide (COS) is an oligomer of β-(1➔4)-linked d-glucosamine, of which actions involve the modulation of several important pathways including the suppression of nuclear factor kappa B (NF-κB) and mitogen-activated protein kinases (MAPK) and the activation of AMP-activated protein kinase (AMPK). |
|
|
| S1323 |
7-Methoxyisoflavone
|
7-Methoxyisoflavone (MIF) is a potent activator of adenosine monophosphate-activated protein kinase (AMPK). |
|
|
| S1321 |
Urolithin B
|
Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα. This compound suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. It is also a regulator of skeletal muscle mass. |
-
PLoS Pathog, 2025, 21(8):e1013401
|
|
| E3011 |
Sarsaparilla Extract
|
Sarsaparilla Extract is extracted from Smilax china L., which can stimulate 3T3-L1 Adipocytes to Brown-like Adipocytes Via β3-AR/AMPK Signaling Pathway. |
|
|
| S1273 |
Amarogentin
|
Amarogentin (AG), a secoiridoid glycoside mainly extracted from Swertia and Gentiana roots, exhibits anti-oxidative, anti-tumour, and anti-diabetic activities. This compound is an agonist for the bitter taste receptor TAS2R1 and inhibits in LAD-2 cells substance P-induced production of newly synthesized TNF-α. It induces apoptosis in human gastric cancer cells (SNU-16) through G2/M cell cycle arrest and PI3K/Akt signalling pathway. This chemical interacts with the α2 subunit of AMP-activated protein kinase (AMPK) and activates the trimeric kinase with EC50 of 277 pM. |
|
|
| 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. |
|
|
| E3029 |
White Paeony Root Extract
|
White Paeony Root Extract is extracted from Paeonia lactiflora Pall., which can alleviate liver injury in hypercholesterolemic rats through the ROCK/AMPK pathway. |
|
|
| E3032 |
Atractyloides Macrocephala Root Extract
|
Atractyloides Macrocephala Root Extract is extracted from Atractylodes macrocephala Koidz., which can regulate lysophagy based on LKB1-AMPK-TFEB 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. This compound potentially ameliorates NAFLD (Non-alcoholic fatty liver disease) by activating AMPK pathways. |
|
|
| S1208 |
Doxorubicin (Adriamycin) Hydrochloride
|
Doxorubicin (DOX) HCl is an antibiotic agent that inhibits human DNA topoisomerase II with IC50 of 2.67 μM. 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.This product may precipitate when dissolved in PBS solution. It is recommended to prepare the stock solution in pure water and dilute with either pure water or saline to obtain the working solution.Doxorubicin (Adriamycin) HCl can be used to induce animal models of kidney disease.
|
- Cell Res, 2025, 35(6):437-452.
- Nat Commun, 2025, 16(1):8873
- Nat Commun, 2025, 16(1):509
|
|
| S7306 |
Dorsomorphin Dihydrochloride
|
Dorsomorphin 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. Dorsomorphin induces autophagy in cancer cell line. |
- J Clin Invest, 2025, e190215
- Redox Biol, 2025, 81:103532
- Redox Biol, 2025, 82:103606
|
|
| S7840 |
Dorsomorphin
|
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. This compound selectively inhibits the BMP type I receptors ALK2, ALK3 and ALK6. It is used in promoting specific cell differentiation and inducing cancer cell line autophagy. For cell testing, the water-soluble S7306 Dorsomorphin (Compound C) 2HCl is recommended. |
- Theranostics, 2025, 15(12):5931-5952
- EMBO Mol Med, 2025, 17(10):2735-2761
- Stem Cell Res Ther, 2025, 16(1):104
|
|
| 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. This compound also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. It affects Unc-51-like autophagy activating kinase 1 (ULK1) activity, robustly inhibits STING-dependent IRF3 activation. Phase 1. |
- Theranostics, 2025, 15(18):9819-9837
- Cell Rep, 2025, 44(7):115947
- Front Cell Infect Microbiol, 2025, 15:1543186
|
|
| 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. This compound inhibits AMPKK activity and inhibits autophagy. |
- Redox Rep, 2025, 30(1):2447721
- PLoS One, 2025, 20(8):e0330282
- Cell Genom, 2025, 5(3):100782
|
|
| 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. |
- Cell Rep, 2024, 43(7):114446
- Int J Mol Sci, 2024, 25(3):1411.
- Int J Mol Sci, 2024, 25(3)1411
|
|
| 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
|
|
| 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. |
- Cell Rep Med, 2025, S2666-3791(25)00231-9
- Cell Rep, 2024, 43(7):114446
- J Cell Sci, 2021, jcs.258685
|
|
| S9833 |
BAY-3827
|
BAY-3827 is a potent AMPK inhibitor which inhibits AMPK kinase activity with IC50 values of 1.4 nM at a low, 10 μM ATP concentration and 15 nM at a high, 2 mM ATP concentration. |
- Int J Mol Sci, 2025, 26(15)7624
- Mol Neurobiol, 2025, 62(10):13786-13806
- Autophagy, 2024, 1-24.
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| E3652 |
Rehmanniae radix praeparata Extract
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Rehmanniae radix praeparata Extract is extracted from Rehmanniae radix praeparata, which can improve diabetes through AMPK-mediated NF-κB/NLRP3 signaling pathway. |
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| E2818 |
MARK4 inhibitor 1
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MARK4 inhibitor 1 is a potent microtubule affinity-regulating kinase 4 (MARK4) inhibitor, with an IC50 of 1.54 μM for MARK4 inhibition assay. |
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| E0022 |
Ophiopogonin D
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Ophiopogonin D (OJV-VI, Deacetylophiopogonin C) is a steroidal glycoside isolated from Chinese herb Radix ophiopogonis and shows anti-tumor property. This compound could suppress TGF-β1-mediated metastatic behavior of MDA-MB-231 cells by regulating ITGB1/FAK/Src/AKT/β-catenin/MMP-9 signaling axis. It also attenuates PM2.5-induced inflammation via suppressing the AMPK/NF-κB pathway in mouse pulmonary epithelial cells. |
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| S0177 |
XMD-17-51
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XMD-17-51 (XMD17-51) is a potent and highly selective inhibitor of NUAK1. |
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| E3029 |
White Paeony Root Extract
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White Paeony Root Extract is extracted from Paeonia lactiflora Pall., which can alleviate liver injury in hypercholesterolemic rats through the ROCK/AMPK pathway. |
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| S1802 |
AICAR (Acadesine)
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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. This compound induces mitophagy. Phase 3. |
- Nat Commun, 2025, 16(1):8478
- Theranostics, 2025, 15(15):7567-7583
- Glia, 2025, 73(11):2253-2272
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| S1033 |
Nilotinib
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Nilotinib is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells. This compound induces autophagy through AMPK activition. |
- Blood Adv, 2025, bloodadvances.2024015364
- Cell Death Discov, 2025, 11(1):62
- Immunology, 2025, NONE
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| S1950 |
Metformin Hydrochloride
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Metformin Hydrochloride (1,1-Dimethylbiguanide Hydrochloride) is a highly effective Antihyperglycemic Agent, which primarily decreases hyperglycemia in hepatocytes by suppressing hepatic gluconeogenesis (glucose production by the liver). It also promotes mitophagy in mononuclear cells and induces apoptosis of lung cancer cells through activating the JNK/p38 MAPK pathway and GADD153.
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- mBio, 2025, e0063425
- Placenta, 2025, 165:50-61
- Sci Adv, 2025, 11(17):eads1875
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| S2697 |
A-769662
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A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM in cell-free assays, little effect on GPPase/FBPase activity. |
- FEBS J, 2025, 10.1111/febs.70247
- Arch Biochem Biophys, 2025, 769:110433
- J Clin Invest, 2024, 134(22)e181314
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| S1396 |
Resveratrol
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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. This compound induces mitophagy/autophagy and autophagy-dependent apoptosis. |
- Aging Cell, 2025, e70075
- Biomed Pharmacother, 2025, 190:118393
- Breast Cancer Res, 2025, 27(1):186
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| S5958 |
Metformin
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Metformin (1,1-Dimethylbiguanide), a widely used drug for treatment of type 2 diabetes, activates AMP-activated protein kinase (AMPK) in hepatocytes. This compound promotes mitophagy in mononuclear cells. It induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153. |
- Signal Transduct Target Ther, 2025, 10(1):271
- Theranostics, 2025, 15(17):9029-9046
- Int J Biol Sci, 2025, 21(9):4231-4251
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| S7898 |
GSK621
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GSK621 is a specific and potent AMPK activator. |
- Front Pharmacol, 2024, 15:1453647
- Sci Rep, 2024, 14(1):5205
- Nat Commun, 2023, 14(1):2994
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| S4895 |
Nilotinib hydrochloride monohydrate
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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. |
- Nat Commun, 2024, 15(1):2089
- J Pharm Sci, 2022, 111(8):2180-2190
- EMBO Mol Med, 2021, e11814
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| S8654 |
ex229 (compound 991)
|
A potent AMPK activator that is 5-10-fold more potent than A769662 in activating AMPK, EX229 (compound 991) is this compound. |
- Neuron, 2025, S0896-6273(25)00247-8
- Autophagy, 2024, 1-24.
- bioRxiv, 2024, 2024.09.26.615290
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| S2542 |
Phenformin HCl
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Phenformin HCl is a hydrochloride salt of phenformin that is an anti-diabetic drug from the biguanide class. It activates AMPK, increasing activity and phosphorylation. |
- Nat Commun, 2024, 15(1):1721
- BMC Cancer, 2024, 24(1):116
- bioRxiv, 2024, 2024.09.16.613317
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| S7953 |
Bempedoic acid (ETC-1002)
|
Bempedoic acid (ETC-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. It is an activator of hepatic AMP-activated protein kinase (AMPK) and has potent inhibitory activity against hepatic ATP-citrate lyase(IC50=29 uM). |
- Cancer Cell, 2025, 43(4):776-796.e14
- iScience, 2023, 26(12):108532
- Oncol Rep, 2023, 49(2)32
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| S3296 |
Hispidulin
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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. This compound induces apoptosis through mitochondrial dysfunction and inhibition of P13k/Akt signalling pathway in HepG2 cancer cells. It exerts anti-osteoporotic and bone resorption attenuating effects via activating the AMPK signaling pathway. |
- Evid Based Complement Alternat Med, 2023, 2023:9428241
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| S0795 |
O-304
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O-304 (O-304X) is an orally available pan-activator of AMPK activated protein kinase (AMPK). This compound exhibits a great potential as a novel drug to treat type 2 diabetes (T2D) and associated cardiovascular complications. |
- Front Pharmacol, 2024, 15:1457817
- Biomed Pharmacother, 2021, 144:112325
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| S8803 |
MK-3903
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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
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| S0411 |
BAM 15
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BAM 15 is a novel mitochondrial protonophore uncoupler capable of protecting mammals from acute renal ischemic-reperfusion injury and cold-induced microtubule damage. This compound is also a potent AMPK activator. It attenuates transportation-induced apoptosis in iPS-differentiated retinal tissue. |
- Neuroscience, 2012, 223:238-45
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| S4561 |
Danthron
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Danthron (Chrysazin, Antrapurol) functions in regulating glucose and lipid metabolism by activating AMPK. This compound is a natural product extracted from the traditional Chinese medicine rhubarb. It 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
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| S5284 |
Adenosine 5'-monophosphate monohydrate
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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). |
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| S8335 |
PF-06409577
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PF-06409577 is an 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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| E1031 |
MK-8722
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MK-8722 is a potent, direct, allosteric activator of all 12 mammalian pan-AMPK complexes. |
- Mol Cell, 2024, S1097-2765(24)00865-7
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| E2032 |
MOTS-c
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MOTS-c, a mitochondria-derived peptide (MDP), exerts antinociceptive and anti-inflammatory effects through activating AMPK pathway and inhibiting MAP kinases-c-fos signaling pathway. |
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| E2371 |
YLF-466D
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YLF-466D is an AMPK activator that inhibits platelet aggregation. |
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| S3832 |
Euphorbiasteroid
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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. This compound 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. |
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| S8953 |
ASP4132
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ASP4132 is a potent and orally active activator of Adenosine Monophosphate-Activated Protein Kinase (AMPK) with EC50 of 0.018 μM. This compound is used as a clinical candidate for the treatment of human cancer. |
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| E5784New |
AICAR phosphate
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| E0653 |
Trans-ferulic acid
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Trans-ferulic acid is a potent activator of AMPK under high glucose condition. |
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| E0795 |
COH-SR4
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COH-SR4 suppresses adipogenesis in 3T3-L1 cells through indirect activation of AMPK and downstream modulation of the Mammalian target of rapamycin complex 1 (mTORC1) signaling pathway, which blocks important regulators involved in protein synthesis, cell cycle progression, and expression of key transcription factors and their target adipogenic genes involved in lipid synthesis. |
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| E1323New |
Aldometanib
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Aldometanib (LXY-05-029) is a selective inhibitor of aldolase (ALDOA) with an IC50 of 50 uM in in vitro enzymatic assays. It also activates lysosomal AMPK by blocking FBP-aldolase binding, mimicking glucose starvation and improving metabolic health without causing hypoglycemia. |
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| S3341 |
Palmitoleic acid
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Palmitoleic acid (POA, Palmitoleate) stimulates the uptake of glucose in liver through activation of AMPK and FGF-21, dependent on PPARα. |
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| S9096 |
ligustroflavone
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Ligustroflavone (Nuezhenoside), isolated from the leaves of Turpinia montana, shows high antioxidant capacity and is reported to be an AMPK activator. |
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| S2942 |
EB-3D
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EB-3D is a potent and selective inhibitor of choline kinase α (ChoKα) with IC50 of 1 μM for ChoKα1. This compound induces deregulation of the AMPK-mTOR pathway and apoptosis in leukemia T-cells. |
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| S9860 |
BC1618
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BC1618 is an orally active Fbxo48 inhibitor that stimulates adenosine monophosphate (AMP)-activated protein kinase (Ampk)-dependent signaling. This compound promotes mitochondrial fission, facilitates autophagy and improves hepatic insulin sensitivity. |
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| S4460 |
IMM-H007
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IMM-H007, an adenosine derivative, is an activator of AMP-Activated Protein Kinase (AMPK). This compound is a potential drug for treating cardiac dysfunction. It negatively regulates endothelium inflammation through inactivating NF-κB and JNK/AP1 signaling. This chemical inhibits ABCA1 (ATP binding cassette subfamily a member 1) degradation and facilitates its cell-surface localization in macrophages, thereby promotes cholesterol efflux. |
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| S9604 |
Lixumistat (IM156)
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Lixumistat (IM156) is a potent activator of AMPK that increases AMPK phosphorylation. It blocks oxidative phosphorylation (OXPHOS) through the inhibition of complex I and increases apoptosis. This compound ameliorates various types of fibrosis and inhibits tumors. |
- bioRxiv, 2024, 2024.09.16.613317
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| S9116 |
Chikusetsusaponin IVa
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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. This compound is a novel AMPK activator. |
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| E0204 |
Poricoic acid A
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Poricoic acid A is isolated from the surface layer of Poria cocos. This compound activates AMPK to attenuate fibroblast activation and abnormal extracellular matrix remodelling in renal fibrosis. It also is a modulator of tryptophan hydroxylase-1 (TPH-1). |
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| S0888 |
Rsva 405
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Rsva 405, a novel small-molecule activator of AMPK, is a potent inhibitor of adipogenesis and thus may have therapeutic potential against obesity. |
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| E2661 |
Chitosan oligosaccharide
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Chitosan oligosaccharide (COS) is an oligomer of β-(1➔4)-linked d-glucosamine, of which actions involve the modulation of several important pathways including the suppression of nuclear factor kappa B (NF-κB) and mitogen-activated protein kinases (MAPK) and the activation of AMP-activated protein kinase (AMPK). |
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| S1323 |
7-Methoxyisoflavone
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7-Methoxyisoflavone (MIF) is a potent activator of adenosine monophosphate-activated protein kinase (AMPK). |
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| S1321 |
Urolithin B
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Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα. This compound suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. It is also a regulator of skeletal muscle mass. |
- PLoS Pathog, 2025, 21(8):e1013401
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| E3011 |
Sarsaparilla Extract
|
Sarsaparilla Extract is extracted from Smilax china L., which can stimulate 3T3-L1 Adipocytes to Brown-like Adipocytes Via β3-AR/AMPK Signaling Pathway. |
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| S1273 |
Amarogentin
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Amarogentin (AG), a secoiridoid glycoside mainly extracted from Swertia and Gentiana roots, exhibits anti-oxidative, anti-tumour, and anti-diabetic activities. This compound is an agonist for the bitter taste receptor TAS2R1 and inhibits in LAD-2 cells substance P-induced production of newly synthesized TNF-α. It induces apoptosis in human gastric cancer cells (SNU-16) through G2/M cell cycle arrest and PI3K/Akt signalling pathway. This chemical interacts with the α2 subunit of AMP-activated protein kinase (AMPK) and activates the trimeric kinase with EC50 of 277 pM. |
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| 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. |
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| 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. This compound potentially ameliorates NAFLD (Non-alcoholic fatty liver disease) by activating AMPK pathways. |
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