AMPK Inhibitors

Cat.No.	Product Name	Information	Product Use Citations
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
S8654	Ex229 (Compound 991)	EX229 (compound 991) is a potent AMPK activator that is 5-10-fold more potent than A769662 in activating AMPK.	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
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.
S7953	Bempedoic acid (ETC-1002)	Bempedoic acid (ETC-1002) is an orally available, once-daily LDL-C lowering small molecule designed to reduce elevated levels of LDL-C and to avoid side effects associated with existing LDL-C lowering therapies. This compound 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
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
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
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
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
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
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
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.
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.
E5784	AICAR phosphate
E0653	Trans-ferulic acid	Trans-ferulic acid is a potent activator of AMPK under high glucose condition.
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.
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.
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.
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.
S1323	7-Methoxyisoflavone	7-Methoxyisoflavone (MIF) is a potent activator of adenosine monophosphate-activated protein kinase (AMPK).
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.
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.
S1033	Nilotinib (AMN-107)	Nilotinib is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells. Nilotinib 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. 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.	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
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
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
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
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.
E1323^New	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.
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.
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.
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).
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.
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.