dorsomorphin (Compound C) / EMD Serono - LARVOL DELTA

Ad-VT Oncolytic Adenovirus Suppresses Bladder Cancer via cAMP-Dependent AMPK-Raptor Activation and G2/M Arrest. (PubMed, Tumour Virus Res) - "This was confirmed by pathway inhibitors (Dorsomorphin, ESI-09) and siRNA knockdown, which reversed cell cycle arrest and reduced cytotoxicity...Crucially, AMPK inhibition attenuated Ad-VT's antitumor effects. These results demonstrate that Ad-VT exerts potent, tumor-selective activity against bladder cancer by inducing cAMP-dependent AMPK-Raptor-mTOR signaling and G2/M arrest, supporting its therapeutic potential."

Journal • Bladder Cancer • Genito-urinary Cancer • Oncology • Solid Tumor • AMPK • CCNB1 • CDK1 • CDKN1A

Integrated bioactivity-guided isolation, network pharmacology, and experimental validation to reveal the key constituents and potential mechanisms of Tectona grandis against diabetes and lipid disorders. (PubMed, J Ethnopharmacol) - "This study demonstrated that TG1 from T. grandis exerted dual mechanisms: Firstly, it directly binds to and activates AMPK, thereby mediating the translocation of GLUT4 to the plasma membrane and enhancing glucose uptake in 3T3-L1 adipocytes; secondly, it acts as a mixed-type inhibitor of PL, effectively suppressing its catalytic activity via a static quenching mechanism. These findings provide a scientific validation for the traditional use of T. grandis in Indian medicine and identify TG1 as a promising multi-target lead candidate for the treatment of diabetes and lipid disorders."

Journal • Diabetes • Dyslipidemia • Metabolic Disorders • SLC2A4

Micheliolide reduces the damage, pyroptosis and oxidative stress of cardiomyocytes caused by OGD/R by regulating the AMPK signaling pathway. (PubMed, J Clin Biochem Nutr) - "Moreover, MCL inhibited OGD/R-induced oxidative stress and pyroptosis while enhancing AMPK pathway activation. Importantly, the protective effect of MCL was attenuated in the presence of the AMPK inhibitor Compound C, indicating that activation of the AMPK signaling pathway is required for MCL-mediated cytoprotection."

Journal • Cardiovascular • Myocardial Infarction • Myocardial Ischemia • Reperfusion Injury

Atractylenolide III Attenuated Neurotoxicity in Alzheimer's Disease via AMPK/GSK3β/Nrf2/HO-1 Signaling Pathway. (PubMed, Mol Neurobiol) - "However, the protective effects of AT-III were partially abolished by Compound C (an AMPK inhibitor). Our study demonstrates that AT-III mitigated neurodegenerative damage in AD by suppressing microglial activation and neuroinflammation through the AMPK/GSK3β/Nrf2/HO-1 signaling, which suggests that AT-III might be a novel therapeutic strategy for the inhibition of AD."

Journal • Alzheimer's Disease • CNS Disorders • Inflammation

Neuroprotective Effects of the SIRT3/AMPK Axis in Experimental Glaucoma. (PubMed, Front Biosci (Landmark Ed)) - "This study provides the first comprehensive in vivo and in vitro evidence in glaucoma models that SIRT3 confers neuroprotection in experimental glaucoma, primarily through activation of the AMPK signaling pathway. These findings identify the SIRT3/AMPK axis as a novel mechanistic target and suggest a promising therapeutic strategy for IOP-independent neuroprotection in glaucoma."

Journal • Cardiovascular • CNS Disorders • Glaucoma • Ophthalmology • AMPK • SIRT3

Novel Dorsomorphin Derivatives: Molecular Modeling, Synthesis, and Bioactivity Evaluation. (PubMed, Biomolecules) - "In the same context, the carbamate derivative 6 was determined as a potent inhibitor of endothelial cell proliferation in BAECs at a low micromolar range. In conclusion, the presented work not only reveals promising antiproliferative dorsomorphin derivatives but also sets the basis for further exploitation of dorsomorphin's bioactive portfolio, based on bioactivity results and molecular modeling calculations."

Journal • Cervical Cancer • Hematological Malignancies • Leukemia • Oncology • Solid Tumor

Rg1 activates the AMPK/mTOR-autophagy axis and inhibits the NOD-like receptor 3 inflammasome to alleviate pyroptosis in periodontal ligament fibroblasts. (PubMed, Odontology) - "Levels of pyroptosis-related cytokines, NOD-like receptor 3 (NLRP3) mRNA expression, and protein levels of NLRP3 inflammasome-related markers, pyroptosis-related markers, autophagy-related markers, and the AMP-activated protein kinase (AMPK)/mechanistic target of rapamycin (mTOR) pathway were determined by ELISA, RT-qPCR, and western blot...HPDLFs were transfected with NLRP3-overexpression plasmids, or co-treated with LPS + Rg1 and the autophagy inhibitor (3-MA), AMPK inhibitor (BML-275), or mTOR activator (MHY1485)...AMPK inhibition or mTOR activation partially averted Rg1's regulatory effects. Rg1 activates AMPK/mTOR-autophagy axis and inhibits NLRP3 inflammasome, thereby alleviating LPS-induced HPDLF pyroptosis."

Journal • Dental Disorders • Periodontitis • BECN1 • IL18 • IL1B • NLRP3

Indomethacin alleviates acute pancreatitis by restoring autophagic flux via the AMPK signaling pathway. (PubMed, Pathol Res Pract) - "Critically, the protective effects of IND were abolished by either the autophagy inhibitor chloroquine or the AMPK inhibitor Compound C (CC). In conclusion, our findings suggest that IND may serve as a promising therapeutic candidate for the treatment of AP."

Journal • Pancreatitis

NIPSNAP3B elevates mitochondrial biogenesis to attenuate lipid accumulation in childhood obesity via AMPK pathway. (PubMed, Gene) - "NIPSNAP3B enhances mitochondrial biogenesis to attenuate lipid accumulation via AMPK pathway in CO."

Journal • Genetic Disorders • Obesity • ACACB • NRF1 • PPARG • TFAM

Empagliflozin improves renal injury of diabetic nephropathy complicated with hyperuricemia through AMPK by promoting autophagy and inhibiting apoptosis. (PubMed, Saudi Pharm J) - "Empagliflozin alleviates renal injury in diabetic nephropathy with hyperuricemia by activating AMPK, promoting autophagy, and inhibiting apoptosis, suggesting its potential therapeutic value in managing this complication."

Journal • Diabetes • Diabetic Nephropathy • Fibrosis • Immunology • Nephrology • Renal Disease • AMPK • CASP3

Mechanisms of Danggui Buxue Decoction in alleviating myocardial injury caused by chronic intermittent hypoxia by activating AMPK/mTOR signaling pathway (PubMed, Zhongguo Zhong Yao Za Zhi) - "The AMPK activator A769662 exerted therapeutic effects similar to those of DBD, whereas the AMPK inhibitor compound C significantly suppressed the therapeutic effect of DBD-containing serum. These findings suggest that DBD alleviates CIH-induced myocardial injury by activating the AMPK/mTOR signaling pathway, thereby promoting mitophagy and inhibiting mitochondria-mediated apoptosis."

IO biomarker • Journal • BCL2 • BECN1 • CASP3

Astragalus polysaccharide improves canine sperm quality after chilled storage via promoting AMPK phosphorylation. (PubMed, BMC Vet Res) - "The supplementation of APS to the extender protects canine sperm after chilled storage via promoting AMPK phosphorylation for enhancing the antioxidant capacity of sperm. These findings provide novel insight into the mechanism of APS in protecting canine sperm after chilled storage, and reveal the feasibility of APS supplementation to sperm extender for canine sperm preservation."

Journal • AMPK

AdipoRon Suppresses Multiple Myeloma Proliferation Through AMPK-Mediated Metabolic Reprogramming and Apoptosis Induction. (PubMed, IUBMB Life) - "Specifically, AdipoRon preferentially suppressed ACC1 expression and subsequently downregulated CPT1A, indicating disruption of fatty acid metabolism. These findings establish that AdipoRon suppresses MM progression through AMPK-driven metabolic reprogramming and apoptosis induction, positioning adiponectin receptor agonism as a promising therapeutic strategy for multiple myeloma."

Journal • Hematological Disorders • Hematological Malignancies • Multiple Myeloma • Oncology • ACACA • AMPK • CASP9 • CPT1A

POs-Ca Drives Osteogenic Differentiation of Human Dental Pulp Stem Cells Via AMPK-Dependent Autophagy Activation and Reciprocal Calcium-Autophagy Crosstalk. (PubMed, Stem Cells Int) - "Mechanistic studies employed verapamil (Ca2+ channel blocker), Compound C (CC;AMPK inhibitor), and chloroquine (CQ;autophagy inhibitor)...In conclusion, POs-Ca might promote hDPSCs osteogenesis via a calcium influx-driven AMPK-autophagy axis, providing a foundation for novel biomaterials that exploit physiological calcium signaling. These findings offer immediate translational potential for developing minimally invasive, cost-effective strategies in dental pulp regeneration and bone defect repair."

Journal • AMPK • RUNX2

Electroacupuncture ameliorates glycolipid metabolism disorder in skeletal muscle of type 2 diabetic rats via modulation of the AMPK/PGC-1α/TFAM signaling pathway. (PubMed, Diabetol Metab Syndr) - "EA improves glycolipid metabolism and alleviates insulin resistance in T2DM rats, potentially via activation of the AMPK/PGC-1α/TFAM pathway. These effects may be linked to improved skeletal muscle function and glucose utilization. EA shows promise as a therapeutic strategy for T2DM, warranting further investigation into its mechanisms and clinical relevance."

Journal • Preclinical • Diabetes • Dyslipidemia • Metabolic Disorders • Type 2 Diabetes Mellitus • TFAM

Spermidine Alleviates Sepsis-Induced Acute Lung Injury through AMPK-Mediated Improvement of Necroptosis. (PubMed, Inflammation) - "Our findings evidence that SPD significantly ameliorates SALI via the regulation of AMPK-mediated necroptosis. SPD supplementation may serve as a complementary therapeutic approach, warranting further investigation in subsequent clinical trials for sepsis treatment."

Journal • Acute Lung Injury • Infectious Disease • Respiratory Diseases • Septic Shock • AMPK • RIPK1

The potential mechanism of celastrol attenuating atherosclerosis by promoting macrophage autophagy via AMPK/ULK1 pathway. (PubMed, Front Pharmacol) - "Mechanistically, Cel-induced autophagy was mediated by the AMPK/ULK1 pathway, and this effect was reversed by the AMPK inhibitor Compound C. Cel exerts anti-atherosclerotic effects by activating macrophage autophagy via the AMPK/ULK1 pathway, thereby improving lipid metabolism, reducing inflammation, and stabilizing plaques. These findings highlight the therapeutic potential of Cel and provide new insights into autophagy-targeted strategies against AS."

Journal • Atherosclerosis • Cardiovascular • Dyslipidemia • Inflammation • Metabolic Disorders • APOE

Metabolic reprogramming is implicated in the differential response of the CAL-1 plasmacytoid dendritic cell line to autophagy inhibitors. (PubMed, Biochim Biophys Acta Mol Cell Res) - "These changes were consistent with AMPK activation, and pharmacological inhibition of AMPK with dorsomorphin (compound C) abolished cytokine production in VPS34-IN1-treated cells. Together, these results indicate that differential cytokine responses to autophagy inhibition are driven primarily by metabolic rewiring rather than autophagic flux per se, highlighting the interplay between metabolism, mitochondrial ROS, and signaling pathways in pDC activation."

Journal • Preclinical • Immunology • Metabolic Disorders • Oncology • IFNB1 • TNFA

A Novel Sesquiterpene from Callistephus chinensis Improves Alcohol-Induced Liver Disease by Regulating the AMPK/NF-κB Signaling Pathway and Gut Flora. (PubMed, Molecules) - "In vitro, by adding inhibitors of TLR4 (TAK-242) and AMPK (Dorsomorphin), it was confirmed that CA alleviates ALD by inhibiting TLR4 and activating AMPK. This study is the first to demonstrate that CA protects against alcoholic liver disease through the regulation of the gut flora and modulation of the AMPK/NF-κB pathway. In conclusion, CA can effectively improve alcoholic liver disease and can be used as an effective candidate drug with liver-protective effects."

Journal • Fibrosis • Hepatology • Immunology • Inflammation • Liver Cirrhosis • Liver Failure • Metabolic Disorders • Metabolic Dysfunction-Associated Steatohepatitis • Metabolic Dysfunction-Associated Steatotic Liver Disease • MYD88 • TLR4

METTL3 promotes vascular stability in intracranial aneurysm via m6A-AMPK axis. (PubMed, Sci Rep) - "Our investigation demonstrates that METTL3 can modulate the phenotypic transformation of VSMCs by regulating the AMPK signaling pathway. This regulation results in inhibited migration, cell proliferation, promoted apoptosis, and suppression of macrophage infiltration, thereby impeding the progression of IAs."

Journal • Cardiovascular • Hematological Disorders • Subarachnoid Hemorrhage • Vascular Neurology • AMPK • CD68 • IL1B • IL6 • METTL3 • MMP3 • MMP9 • TNFA

Coenzyme Q10 ameliorates obesity by promoting white adipose tissue browning and preserving mitochondrial dynamics in ovariectomized rats fed a high-fat diet. (PubMed, J Nutr Biochem) - "In 3T3-L1 adipocytes, CoQ10-induced expression of browning markers (UCP-1, TBX1 and PRDM16) was significantly suppressed by dorsomorphin, an AMPK inhibitor, and by AMPK knockdown (p < 0.05)...AMPK activation is suggested to contribute to the browning effect and enhance the expression of proteins involved in mitochondrial dynamics. Therefore, CoQ10 supplementation could be an effective intervention for preventing postmenopausal obesity."

Journal • Preclinical • Cardiovascular • Diabetes • Genetic Disorders • Inflammation • Metabolic Disorders • Obesity • Type 2 Diabetes Mellitus • HIF1A • IL6 • MFN2 • PRDM16 • TBX1

Decoding the Anti-Obesity Mechanisms of Isoliquiritigenin: AMPK Activation Modulates Adipogenesis, Lipolysis, Oxidative Stress, and Inflammation in High-Fat Diet Rat Models. (PubMed, J Nutr Biochem) - "Dorsomorphin treatment reversed these effects in ISL + HFD rats. In conclusion, ISL demonstrates anti-obesity effects in HFD-induced rats through AMPK activation."

Journal • Preclinical • Genetic Disorders • Inflammation • Obesity • IL6 • PPARA • TNFA

Kinsenoside Regulates Ferroptosis and Enhances Osteogenic Differentiation of Bone Marrow Mesenchymal Stem Cells through the AMPK/SIRT1 Pathway. (PubMed, Ann Clin Lab Sci) - "Kin enhances BMSCs' osteogenic differentiation under HG conditions by suppressing ferroptosis via activation of the AMPK/SIRT1 signaling pathway."

Journal • Diabetes • Osteoporosis • Rheumatology

Elucidating Asprosin's Role as an Intracellular Metabolism Regulator in Diabetic Kidney Disease (KIDNEY WEEK 2025) - "Methods This study utilized type 2 diabetic db/db mice, dividing them into two groups: one received Asprosin neutralizing antibodies targeting the 28-amino acid peptide, while the other was treated with Metformin, an AMP-activated protein kinase (AMPK) activator for three weeks...Conclusion This study reveals Asprosin's role in regulating intracellular energy metabolism, with potential implications for targeted therapies in DKD. Inhibiting Asprosin suppressed lipid accumulation and inflammation by activating the AMPK-associated signaling pathway, suggesting a promising therapeutic strategy for managing DKD."

Chronic Kidney Disease • Diabetes • Diabetic Nephropathy • Inflammation • Metabolic Disorders • Nephrology • Renal Disease • Type 2 Diabetes Mellitus

Topical β-hydroxybutyrate suppresses allergic dermatitis via HCAR2-CaMKK-AMPK-mediated barrier protection. (PubMed, Biochem Biophys Res Commun) - "This suppressive effect was abrogated by mepenzolate bromide, a hydroxycarboxylic acid receptor 2 (HCAR2) antagonist, and was also reversed by dorsomorphin, a direct AMPK inhibitor, and by STO-609, a CaMKK inhibitor...These findings demonstrate that topical BHB exerts a local anti-allergic effect through HCAR2-dependent AMPK activation and barrier preservation. Our results highlight topical BHB as a potential non-steroidal strategy for protecting the skin against immediate allergic responses via HCAR2-CaMKK-AMPK-mediated barrier preservation."

Journal • Allergy • Contact Dermatitis • Dermatitis • Dermatology • Immunology • AMPK • OCLN • TJP1