dorsomorphin (Compound C) / EMD Serono - LARVOL DELTA

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

Effect and Mechanisms of Yiqi Jianpi Xiaoyu Prescription on Kidney Fibrosis on the Basis of Metabolomics and Experimental Validation. (PubMed, Food Sci Nutr) - "We established a unilateral ureteral obstruction (UUO) kidney fibrosis mouse model, dividing mice into sham, model, YQJPXY-treated (7.28, 14.56, 29.12 g/kg/day), and Losartan groups. Among these, Adenosine, which attenuated fibrosis via A2BR/cAMP/AMPK-mediated autophagy, was inhibited by CQ, PSB1115, and Dorsomorphin. YQJPXY's antifibrotic mechanism involves adenosine-activated A2BR/cAMP/AMPK autophagy pathways."

Journal • Fibrosis • Immunology • TGFB1

Jianpi Qiangji Granule ameliorates aging-associated sarcopenia via AMPK/PGC-1α axis in SAMP8 mice. (PubMed, Phytomedicine) - "Our results demonstrate that JQG ameliorates age-related sarcopenia by enhancing muscle mass and function, reversing pathological fiber-type transition, and attenuating muscle senescence. Critically, the AMPK/PGC-1α axis plays an essential role in mediating these therapeutic effects. Collectively, these findings suggest that JQG represents a promising candidate for the prevention and treatment of sarcopenia in aging models."

Journal • Preclinical • Musculoskeletal Diseases • Orthopedics • Sarcopenia • AMPK • FBXO32

TRAIL-Mediated Increased Insulin Secretion in Insulin-Producing Cells Generated from Induced Pluripotent Stem Cells (ESGCT 2024) - "TRAIL was included in its soluble form in the last stage of the differentiation process, along with the combination of small molecules necessary to induce definitive endoderm (activin A, CHIR99021) and pancreatic differentiation stages (dorsomorphin, retinoic acid, SB431542, forskolin, dexamethasone, ALK5 inhibitor II, nicotinamide, sodium chromoglycate). We are currently investigating the mechanism of this effect via correlated analysis of predominantly the canonical insulin secretion pathways. Further investigation into TRAIL's mechanisms of action in increased insulin secretion and beta cell proliferation may unveil new therapeutic avenues for diabetes management (TUBITAK Grant No: 218S617)."

Diabetes • Metabolic Disorders • KLF4 • POU5F1 • SOX2 • TGFBR1

Growth differentiation factor 15 protects against diabetic endothelial dysfunction by AMP-activated protein kinase mediation. (PubMed, Vascul Pharmacol) - "Our findings demonstrate that GDF15 ameliorates diabetic endothelial dysfunction and oxidative stress by AMPK-dependent pathways in endothelial cells. These results highlight GDF15 as a promising therapeutic target for mitigating oxidative stress and preserving diabetic endothelial dysfunction."

Journal • Cardiovascular • Diabetes • Metabolic Disorders • ACE2 • GDF15

The study of beneficial effect and mechanism of propofol on TNF-α-induced p-Tau increase in HT22 hippocampal neurons. (PubMed, Neuroscience) - "Propofol may attenuate TNF-α-induced p-Tau expression in HT22 cells through modulation of the AMPK/AKT signaling pathway, and may inhibit TNF-α-enhanced mitophagy by affecting the AMPK/SIRT3 signaling pathway."

Journal • Inflammation • SIRT3 • TNFA

Lujiao Formula attenuates cardiac hypertrophy by modulating AMPK-SIRT1 and PI3K-Akt signaling pathways. (PubMed, Bioorg Chem) - "Importantly, these beneficial effects were partially abrogated by co-treatment with Compound C (CC, an AMPK inhibitor) or LY294002 (a PI3K inhibitor) in vitro. Collectively, our findings demonstrated that LJF exerted significant anti-hypertrophic effects through coordinated modulation of the AMPK-SIRT1 and PI3K-Akt cascades, offering a strong mechanistic basis for its clinical utility in managing CH."

Journal • Cardiovascular • Congestive Heart Failure • Heart Failure • SIRT1

Cordycepin deteriorates 5' fluorouracil-induced anaemia by AMPK activation. (PubMed, Eur J Pharmacol) - "COR treatment substantially delayed reticulocyte recovery in the peripheral blood and reduced the number of erythroblasts in the spleen following 5-FU-induced anaemia. The mechanism of action of COR involves inhibiting erythroid differentiation via activating AMPK."

Journal • Anemia • Hematological Disorders • EPB42 • GATA1 • MTHFD2

Melatonin Activates AMPK Pathway to Regulate the Regeneration of Slow Muscle Fibers in Skeletal Muscle Injury Repair. (PubMed, FASEB J) - "The results indicate that melatonin facilitates the formation of slow-twitch fibers during muscle repair by augmenting mitochondrial function through the AMPK/PGC-1α signaling pathway. Consequently, these findings imply that melatonin improves mitochondrial function via AMPK/PGC-1α signaling, thereby promoting the regeneration of slow muscle fibers and facilitating the repair of skeletal muscle damage."

Journal • MYH4 • MYH7

AMPK inhibition synergistically enhances the effect of fatostatin-treatment in glioblastoma cell models (EANO 2025) - "Therefore, we aimed to investigate the impact of AMP-activated protein kinase (AMPK)- and SREBP-inhibition by dorsomorphin and fatostatin on the expression of enzymes controlling de novo fatty acid synthesis (e.g.FASN) in glioblastoma (GB) cells in vitro...GB cells presenting with high levels of FASN are susceptible to fatostatin treatment, which was indicated by IC50 levels below 20µM. Combined treatment with inhibitors directed against both, the AMPK and SREBP pathway resulted in a synergistically enhanced response. Consequently, lipogenesis inhibition by attacking different axes of metabolism regulation might be a promising novel therapeutic option in glioblastoma."

Brain Cancer • Glioblastoma • Oncology • Solid Tumor • AMPK • FASN

Dorsomorphin Suppresses EMT to Reduce AR-Negative Prostate Cancer Metastasis by Synergistically Antagonizing JAK2/STAT3 and Gli2-Independent Shh Activation. (PubMed, Prostate Cancer) - "Interestingly, dorsomorphin inhibited the expression and nucleation of Gli1 and Gli3 but not affected the expression of Gli2. Thus, these findings reveal that the new mechanism of AMPK inhibitor dorsomorphin against prostate cancer metastasis is through synergistically antagonizing JAK2/STAT3 and Gli2-independent Shh activation."

Journal • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor • AMPK • AR • GLI1 • GLI2 • GLI3 • HIF1A • JAK2 • STAT3 • TGFB1

Restoration of Cementoblast Mineralization by Glutamine Under Inflammatory Conditions. (PubMed, Int Dent J) - "Glutamine supplementation restores mineralization by the cementoblasts under inflammatory conditions, which provides a novel theoretical foundation for the alleviation and treatment of periodontitis and apical periodontitis."

Journal • Dental Disorders • Infectious Disease • Inflammation • Periodontitis

Linolamide in apoptotic bodies: a key factor in mesenchymal stem cell immunotherapy for two abortion models. (PubMed, Stem Cell Res Ther) - "Appropriate doses of hucMSC-ABs induce anti-inflam Macs in the uterus and prevent fetal loss, while high doses promote the polarization of pro-inflam Macs and lead to fetal loss. The effects of hucMSC-ABs in regulating Macs and treating URSA are related to different doses of linoleamide and PA on Macs. Linoleamide activates AMPK and suppresses NF-κB via Gys1. This study revealed the effect and mechanism of hucMSC-ABs intervention in fetal loss and provided a new idea for the treatment of URSA."

Journal • Transplantation

Novel AMPK/ORP8-lipophagy axis: A therapeutic target for asiaticoside-mediated cardioprotection against ischemia-reperfusion injury in hyperlipidemia. (PubMed, Phytomedicine) - "This study demonstrates that AS mitigates myocardial I/R injury in hyperlipidemic conditions by promoting lipophagy through the AMPK/ORP8 signaling axis. The AMPK/ORP8-lipophagy pathway represents a novel therapeutic target for metabolic cardiovascular diseases, and AS emerges as a promising cardioprotective agent with significant translational potential."

Journal • Cardiovascular • Dyslipidemia • Metabolic Disorders • Myocardial Infarction • Myocardial Ischemia • Reperfusion Injury • AMPK • BECN1

Integrated Lipidomics and Network Pharmacology Reveal the AMPK-Mediated Therapeutic Mechanism of 3,3'-Diindolylmethane in Hepatic Lipid Metabolism. (PubMed, Antioxidants (Basel)) - "CC abolished all DIM-induced molecular changes in vitro. Collectively, DIM alleviates hepatic lipid accumulation and oxidative stress in MASLD models through AMPK activation, subsequently modulating PPARα and SREBP1/ACC1 pathways."

Journal • Hepatocellular Cancer • Hepatology • Metabolic Disorders • Metabolic Dysfunction-Associated Steatotic Liver Disease • Oncology • Solid Tumor • AMPK • PPARA

AMPK regulates BK-channel current in CA1 hippocampal neurons. (PubMed, Biochim Biophys Acta Gen Subj) - "Accordingly, current-clamp experiments revealed that AMPK manipulations significantly affect leptin responses on CA1 neuronal firing. These results support AMPK as a key mediator of the interplay between leptin and neuronal excitability, readily integrating metabolic signals with the computing state of firing outputs in CA1 hippocampal neurons."

Journal • AMPK • LEP

Adiponectin Receptor Agonist Ameliorates Synaptic Dysfunction in 3xTg Alzheimer's Disease Mouse Model by Activation of AMPK. (PubMed, CNS Neurosci Ther) - "Activation of adiponectin receptors restores synaptic function in an AD model in part through AMPK signaling. These results warrant further investigation into adiponectin receptor agonists as a novel approach for AD prevention or treatment."

Journal • Preclinical • Alzheimer's Disease • CNS Disorders