AMPK

亜型選択性的な製品

AMPK-related protein kinase

シグナル伝達経路

AMPK製品

All (52)
AMPK阻害剤 (12)
AMPK活性剤(40)
新製品

製品コード	製品名称	製品説明	文献中Selleckの製品使用例
S1208	Doxorubicin (DOX) HCl	ドキソルビチン塩酸塩 (Doxorubicin (Adriamycin, NSC 123127, DOX, Hydroxydaunorubicin) HCl) は抗生物質の一種であり、DNA トポイソメラーゼ (topoisomerase) II を阻害することで DNA 損傷を引き起こし、がん細胞中においてマイトファジー (mitophagy) およびアポトーシス (apoptosis) を誘導します。ドキソルビシンは AMPK の基底状態におけるリン酸化を減弱します。また、ドキソルビシンは HIV 感染患者の併用療法において使用されますが、同時に HBV 再活性化のリスクを伴うことが分かっています。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.	Cell Metab, 2024, S1550-4131(24)00371-1 Nat Cancer, 2024, 10.1038/s43018-024-00814-0 Nucleic Acids Res, 2024, gkae811
S7306	Dorsomorphin 2HCl	Dorsomorphin 2HCl is a potent, reversible, selective AMPK inhibitor with K_i 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.	Nat Commun, 2024, 15(1):4124 Nat Commun, 2024, 15(1):4124 Adv Sci (Weinh), 2024, 11(4):e2304987
S7840	Dorsomorphin	Dorsomorphin is a potent, reversible, selective AMPK inhibitor with K_i 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.	Nat Commun, 2024, 15(1):8547 J Clin Invest, 2024, 134(22)e181314 Nucleic Acids Res, 2024, gkae707
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.	J Clin Invest, 2024, 134(22)e181314 J Clin Invest, 2024, e175023 Research (Wash D C), 2024, 7:0400
S1033	Nilotinib	Nilotinib is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition.	Nat Commun, 2024, 15(1):651 Nat Commun, 2024, 15(1):2089 Elife, 2024, 12RP92324
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.	EMBO J, 2024, 10.1038/s44318-024-00244-9 EMBO Mol Med, 2024, 10.1038/s44321-024-00136-9 CNS Neurosci Ther, 2024, 30(8):e14913
S1950	Metformin HCl	Metformin HCl (1,1-Dimethylbiguanide HCl) decreases hyperglycemia in hepatocytes primarily by suppressing glucose production by the liver (hepatic gluconeogenesis). Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153.	Nat Commun, 2024, 15(1):1785 J Clin Invest, 2024, e175023 EBioMedicine, 2024, 102:105090
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.	J Clin Invest, 2024, 134(22)e181314 Nat Commun, 2023, 14(1):5913 Nat Commun, 2023, 14(1):5913
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. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis.	Biochem Biophys Res Commun, 2024, 723:150186 J Hazard Mater, 2023, 10.1016/j.jhazmat.2023.132932 Cell Death Dis, 2023, 14(6):367
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.	J Clin Invest, 2024, 134(22)e181314 Adv Healthc Mater, 2024, e2303785. Cell Rep, 2024, 43(10):114775
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.	Acta Pharm Sin B, 2024, 14(8):3576-3590 J Adv Res, 2024, S2090-1232(24)00555-1 J Transl Med, 2024, 22(1):844
S7898	GSK621	GSK621 is a specific and potent AMPK activator.	Sci Rep, 2024, 14(1):5205 Nat Commun, 2023, 14(1):2994 Research Square, 2023, 10.21203/rs.3.rs-3727864/v1
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)	EX229 (compound 991) is a potent AMPK activator that is 5-10-fold more potent than A769662 in activating AMPK.	Autophagy, 2024, 1-24. bioRxiv, 2024, 2024.09.26.615290 Nature, 2023, 621(7977):188-195
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.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).	iScience, 2023, 26(12):108532 Oncol Rep, 2023, 49(2)32 Biomed Pharmacother, 2021, 144:112325
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, 2024, 43(7):114446 J Cell Sci, 2021, jcs.258685 Molecules, 2020, 8;25(9) pii: E2220
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.	Autophagy, 2024, 1-24. Int J Biol Sci, 2024, 20(1):312-330 Int J Mol Sci, 2024, 25(17)9612
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.	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). 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
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. BAM 15 is also a potent AMPK activator. BAM 15 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. 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
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.
E2371	YLF-466D	YLF-466D is an AMPK activator that inhibits platelet aggregation with IC50 of 84 μM.
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.
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.
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. 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.
E0653	Trans-ferulic acid	Trans-ferulic acid is a potent activator of AMPKunder 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.
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.
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.
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.
S9604	Lixumistat (IM156)	Lixumistat (IM156), 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.	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. Chikusetsusaponin IVa is a novel AMPK activator.
E0204	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).
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. 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.
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.
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. Demethyleneberberine (DMB) potentially ameliorates NAFLD (Non-alcoholic fatty liver disease) by activating AMPK pathways.
S1208	Doxorubicin (DOX) HCl	ドキソルビチン塩酸塩 (Doxorubicin (Adriamycin, NSC 123127, DOX, Hydroxydaunorubicin) HCl) は抗生物質の一種であり、DNA トポイソメラーゼ (topoisomerase) II を阻害することで DNA 損傷を引き起こし、がん細胞中においてマイトファジー (mitophagy) およびアポトーシス (apoptosis) を誘導します。ドキソルビシンは AMPK の基底状態におけるリン酸化を減弱します。また、ドキソルビシンは HIV 感染患者の併用療法において使用されますが、同時に HBV 再活性化のリスクを伴うことが分かっています。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.	Cell Metab, 2024, S1550-4131(24)00371-1 Nat Cancer, 2024, 10.1038/s43018-024-00814-0 Nucleic Acids Res, 2024, gkae811
S7306	Dorsomorphin 2HCl	Dorsomorphin 2HCl is a potent, reversible, selective AMPK inhibitor with K_i 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.	Nat Commun, 2024, 15(1):4124 Nat Commun, 2024, 15(1):4124 Adv Sci (Weinh), 2024, 11(4):e2304987
S7840	Dorsomorphin	Dorsomorphin is a potent, reversible, selective AMPK inhibitor with K_i 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.	Nat Commun, 2024, 15(1):8547 J Clin Invest, 2024, 134(22)e181314 Nucleic Acids Res, 2024, gkae707
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.	EMBO J, 2024, 10.1038/s44318-024-00244-9 EMBO Mol Med, 2024, 10.1038/s44321-024-00136-9 CNS Neurosci Ther, 2024, 30(8):e14913
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.	Acta Pharm Sin B, 2024, 14(8):3576-3590 J Adv Res, 2024, S2090-1232(24)00555-1 J Transl Med, 2024, 22(1):844
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, 2024, 43(7):114446 J Cell Sci, 2021, jcs.258685 Molecules, 2020, 8;25(9) pii: E2220
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.	Autophagy, 2024, 1-24. Int J Biol Sci, 2024, 20(1):312-330 Int J Mol Sci, 2024, 25(17)9612
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. 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.
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.	J Clin Invest, 2024, 134(22)e181314 J Clin Invest, 2024, e175023 Research (Wash D C), 2024, 7:0400
S1033	Nilotinib	Nilotinib is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition.	Nat Commun, 2024, 15(1):651 Nat Commun, 2024, 15(1):2089 Elife, 2024, 12RP92324
S1950	Metformin HCl	Metformin HCl (1,1-Dimethylbiguanide HCl) decreases hyperglycemia in hepatocytes primarily by suppressing glucose production by the liver (hepatic gluconeogenesis). Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153.	Nat Commun, 2024, 15(1):1785 J Clin Invest, 2024, e175023 EBioMedicine, 2024, 102:105090
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.	J Clin Invest, 2024, 134(22)e181314 Nat Commun, 2023, 14(1):5913 Nat Commun, 2023, 14(1):5913
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. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis.	Biochem Biophys Res Commun, 2024, 723:150186 J Hazard Mater, 2023, 10.1016/j.jhazmat.2023.132932 Cell Death Dis, 2023, 14(6):367
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.	J Clin Invest, 2024, 134(22)e181314 Adv Healthc Mater, 2024, e2303785. Cell Rep, 2024, 43(10):114775
S7898	GSK621	GSK621 is a specific and potent AMPK activator.	Sci Rep, 2024, 14(1):5205 Nat Commun, 2023, 14(1):2994 Research Square, 2023, 10.21203/rs.3.rs-3727864/v1
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)	EX229 (compound 991) is a potent AMPK activator that is 5-10-fold more potent than A769662 in activating AMPK.	Autophagy, 2024, 1-24. bioRxiv, 2024, 2024.09.26.615290 Nature, 2023, 621(7977):188-195
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
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.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).	iScience, 2023, 26(12):108532 Oncol Rep, 2023, 49(2)32 Biomed Pharmacother, 2021, 144:112325
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.	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). 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
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. BAM 15 is also a potent AMPK activator. BAM 15 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. 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
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.
E2371	YLF-466D	YLF-466D is an AMPK activator that inhibits platelet aggregation with IC50 of 84 μM.
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.
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.
E0653	Trans-ferulic acid	Trans-ferulic acid is a potent activator of AMPKunder 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.
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.
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.
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.
S9604	Lixumistat (IM156)	Lixumistat (IM156), 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.	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. Chikusetsusaponin IVa is a novel AMPK activator.
E0204	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).
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. 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.
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.
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. Demethyleneberberine (DMB) potentially ameliorates NAFLD (Non-alcoholic fatty liver disease) by activating AMPK pathways.

AMPK阻害剤の選択性比較