866405-64-3 | Dorsomorphin

Packsize	Purity	Availability	Price	Discounted Price
1mg	99%	in stock	$10.00	$7.00
5mg	99%	in stock	$19.00	$14.00
10mg	99%	in stock	$28.00	$19.00

Description

• Catalog Number: AB69555
• Chemical Name: Dorsomorphin
• CAS Number: 866405-64-3
• Molecular Formula: C24H25N5O
• Molecular Weight: 399.4882
• MDL Number: MFCD08705402
• SMILES: C1CCN(CC1)CCOc1ccc(cc1)c1cnc2n(c1)ncc2c1ccncc1

Computed Properties

• Complexity: 514
• Covalently-Bonded Unit Count: 1
• Heavy Atom Count: 30
• Hydrogen Bond Acceptor Count: 5
• Rotatable Bond Count: 6
• XLogP3: 3.4

Literature

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• Salidroside stimulates osteoblast differentiation through BMP signaling pathway.

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• Resveratrol attenuates vascular endothelial inflammation by inducing autophagy through the cAMP signaling pathway.

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• Flavanoids induce expression of the suppressor of cytokine signalling 3 (SOCS3) gene and suppress IL-6-activated signal transducer and activator of transcription 3 (STAT3) activation in vascular endothelial cells.

  The Biochemical journal 20130901

• S-allyl cysteine attenuates free fatty acid-induced lipogenesis in human HepG2 cells through activation of the AMP-activated protein kinase-dependent pathway.

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• Autophagic cell death induced by resveratrol depends on the Ca(2+)/AMPK/mTOR pathway in A549 cells.

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• Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe.

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• Reversal of P-glycoprotein-mediated multidrug resistance is induced by mollugin in MCF-7/adriamycin cells.

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  American journal of physiology. Gastrointestinal and liver physiology 20120915

• The chemokine CCL5 regulates glucose uptake and AMP kinase signaling in activated T cells to facilitate chemotaxis.

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  American journal of hypertension 20120201

• Ginsenoside Rg2 induces orphan nuclear receptor SHP gene expression and inactivates GSK3β via AMP-activated protein kinase to inhibit hepatic glucose production in HepG2 cells.

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• The adenosine derivative 2',3',5'-tri-O-acetyl-N6-(3-hydroxylaniline) adenosine activates AMPK and regulates lipid metabolism in vitro and in vivo.

  Life sciences 20120102

• AMP-activated protein kinase regulates PDGF-BB-stimulated interleukin-6 synthesis in osteoblasts: involvement of mitogen-activated protein kinases.

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• Effect of the AMP-kinase modulators AICAR, metformin and compound C on insulin secretion of INS-1E rat insulinoma cells under standard cell culture conditions.

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• Compound C prevents the unfolded protein response during glucose deprivation through a mechanism independent of AMPK and BMP signaling.

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• Compound C independent of AMPK inhibits ICAM-1 and VCAM-1 expression in inflammatory stimulants-activated endothelial cells in vitro and in vivo.

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• Dorsomorphin stimulates neurite outgrowth in PC12 cells via activation of a protein kinase A-dependent MEK-ERK1/2 signaling pathway.

  Genes to cells : devoted to molecular & cellular mechanisms 20111101

• Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity.

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• Supplementation of pyruvate prevents palmitate-induced impairment of glucose uptake in C2 myotubes.

  Molecular and cellular endocrinology 20111015

• Resveratrol prevents norepinephrine induced hypertrophy in adult rat cardiomyocytes, by activating NO-AMPK pathway.

  European journal of pharmacology 20111001

• Application of small organic molecules reveals cooperative TGFβ and BMP regulation of mesothelial cell behaviors.

  ACS chemical biology 20110916

• Cadmium induces autophagy through ROS-dependent activation of the LKB1-AMPK signaling in skin epidermal cells.

  Toxicology and applied pharmacology 20110915

• Acute rosiglitazone treatment is cardioprotective against ischemia-reperfusion injury by modulating AMPK, Akt, and JNK signaling in nondiabetic mice.

  American journal of physiology. Heart and circulatory physiology 20110901

• Resveratrol activates AMPK and suppresses LPS-induced NF-κB-dependent COX-2 activation in RAW 264.7 macrophage cells.

  Anatomy & cell biology 20110901

• Compound C stimulates heme oxygenase-1 gene expression via the Nrf2-ARE pathway to preserve human endothelial cell survival.

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• Chemical 'Jekyll and Hyde's: small-molecule inhibitors of developmental signaling pathways.

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• AICAR and Compound C regulate food intake independently of AMP-activated protein kinase in lines of chickens selected for high or low body weight.

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• Ischemia-induced stimulation of Na-K-Cl cotransport in cerebral microvascular endothelial cells involves AMP kinase.

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• Compound C inhibits vascular smooth muscle cell proliferation and migration in an AMP-activated protein kinase-independent fashion.

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• Resveratrol-activated AMPK/SIRT1/autophagy in cellular models of Parkinson's disease.

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• Post-stroke hypothermia provides neuroprotection through inhibition of AMP-activated protein kinase.

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• Anti-tumor effect of luteolin is accompanied by AMP-activated protein kinase and nuclear factor-κB modulation in HepG2 hepatocarcinoma cells.

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  Metabolism: clinical and experimental 20110401

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  British journal of pharmacology 20110401

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  Tissue engineering. Part A 20110401

• Genistein, resveratrol, and 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside induce cytochrome P450 4F2 expression through an AMP-activated protein kinase-dependent pathway.

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• Leptin controls ketone body utilization in hypothalamic neuron.

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• meso-Dihydroguaiaretic acid inhibits hepatic lipid accumulation by activating AMP-activated protein kinase in human HepG2 cells.

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  Pharmacological reports : PR 20110101

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  Journal of stem cells 20110101

• Astrocyte elevated gene-1 induces protective autophagy.

  Proceedings of the National Academy of Sciences of the United States of America 20101221

• Calcitonin gene-related peptide promotes angiogenesis via AMP-activated protein kinase.

  American journal of physiology. Cell physiology 20101201

• Differential roles of AMPKα1 and AMPKα2 in regulating 4-HNE-induced RPE cell death and permeability.

  Experimental eye research 20101201

• The rational design of a novel potent analogue of the 5'-AMP-activated protein kinase inhibitor compound C with improved selectivity and cellular activity.

  Bioorganic & medicinal chemistry letters 20101115

• AMP-activated protein kinase is required for induction of apoptosis and epithelial-to-mesenchymal transition.

  Cellular signalling 20101101

• Dorsomorphin and LDN-193189 inhibit BMP-mediated Smad, p38 and Akt signalling in C2C12 cells.

  The international journal of biochemistry & cell biology 20101101

• AMP kinase acts as a negative regulator of RANKL in the differentiation of osteoclasts.

  Bone 20101101

• A role for AMPK in increased insulin action after serum starvation.

  American journal of physiology. Cell physiology 20101101

• Nordihydroguaiaretic acid protects against high-fat diet-induced fatty liver by activating AMP-activated protein kinase in obese mice.

  Biochemical and biophysical research communications 20101008

• Adiponectin-mediated heme oxygenase-1 induction protects against iron-induced liver injury via a PPARα dependent mechanism.

  The American journal of pathology 20101001

• High-efficiency induction of neural conversion in human ESCs and human induced pluripotent stem cells with a single chemical inhibitor of transforming growth factor beta superfamily receptors.

  Stem cells (Dayton, Ohio) 20101001

• Role of AMPK throughout meiotic maturation in the mouse oocyte: evidence for promotion of polar body formation and suppression of premature activation.

  Molecular reproduction and development 20101001

• Ionizing radiation activates AMP-activated kinase (AMPK): a target for radiosensitization of human cancer cells.

  International journal of radiation oncology, biology, physics 20100901

• Intersegmental vessel formation in zebrafish: requirement for VEGF but not BMP signalling revealed by selective and non-selective BMP antagonists.

  British journal of pharmacology 20100901

• Identification of early requirements for preplacodal ectoderm and sensory organ development.

  PLoS genetics 20100901

• Rosiglitazone inhibits monocyte/macrophage adhesion through de novo adiponectin production in human monocytes.

  Journal of cellular biochemistry 20100815

• AMP-activated protein kinase mediates activity-dependent regulation of peroxisome proliferator-activated receptor gamma coactivator-1alpha and nuclear respiratory factor 1 expression in rat visual cortical neurons.

  Neuroscience 20100811

• Compound C sensitizes Caki renal cancer cells to TRAIL-induced apoptosis through reactive oxygen species-mediated down-regulation of c-FLIPL and Mcl-1.

  Experimental cell research 20100801

• A pharmacological activator of AMP-activated protein kinase protects hypoxic neurons in a concentration-dependent manner.

  Neurochemical research 20100801

• AMPK enhances the expression of pancreatic duodenal homeobox-1 via PPARalpha, but not PPARgamma, in rat insulinoma cell line INS-1.

  Acta pharmacologica Sinica 20100801

• The antioxidant effects of genistein are associated with AMP-activated protein kinase activation and PTEN induction in prostate cancer cells.

  Journal of medicinal food 20100801

• [Genetic basis for skeletal disease. Establishment of novel treatments for fibrodysplasia ossificans progressiva (FOP)].

  Clinical calcium 20100801

• Inhibition of AMP-activated protein kinase pathway sensitizes human leukemia K562 cells to nontoxic concentration of doxorubicin.

  Molecular and cellular biochemistry 20100701

• Adenosine monophosphate activated protein kinase regulates ABCG1-mediated oxysterol efflux from endothelial cells and protects against hypercholesterolemia-induced endothelial dysfunction.

  Arteriosclerosis, thrombosis, and vascular biology 20100701

• SU11248 (sunitinib) directly inhibits the activity of mammalian 5'-AMP-activated protein kinase (AMPK).

  Cancer biology & therapy 20100701

• Activation of AMPK inhibits cardiomyocyte hypertrophy by modulating of the FOXO1/MuRF1 signaling pathway in vitro.

  Acta pharmacologica Sinica 20100701

• Activation of AMP-activated protein kinase by 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside in the muscle microcirculation increases nitric oxide synthesis and microvascular perfusion.

  Arteriosclerosis, thrombosis, and vascular biology 20100601

• Metformin-induced regulation of the intestinal D-glucose transporters.

  Journal of physiology and pharmacology : an official journal of the Polish Physiological Society 20100601

• Acadesine inhibits tissue factor induction and thrombus formation by activating the phosphoinositide 3-kinase/Akt signaling pathway.

  Arteriosclerosis, thrombosis, and vascular biology 20100501

• AMP-activated protein kinase signaling activation by resveratrol modulates amyloid-beta peptide metabolism.

  The Journal of biological chemistry 20100319

• Glycolysis inhibition sensitizes tumor cells to death receptors-induced apoptosis by AMP kinase activation leading to Mcl-1 block in translation.

  Oncogene 20100318

• BMP Inhibition with dorsomorphin limits adipogenic potential of preadipocytes.

  The Journal of veterinary medical science 20100301

• In vivo structure-activity relationship study of dorsomorphin analogues identifies selective VEGF and BMP inhibitors.

  ACS chemical biology 20100219

• Resveratrol modulates tumor cell proliferation and protein translation via SIRT1-dependent AMPK activation.

  Journal of agricultural and food chemistry 20100210

• Activation of SIRT1 by resveratrol induces KLF2 expression conferring an endothelial vasoprotective phenotype.

  Cardiovascular research 20100201

• Expression and role of adiponectin receptor 1 in lipopolysaccharide-induced proliferation of cultured rat adventitial fibroblasts.

  Cell biology international 20100201

• BMP4 regulates vascular progenitor development in human embryonic stem cells through a Smad-dependent pathway.

  Journal of cellular biochemistry 20100201

• Metformin increases phagocytosis and acidifies lysosomal/endosomal compartments in AMPK-dependent manner in rat primary microglia.

  Naunyn-Schmiedeberg's archives of pharmacology 20100201

• Transitory activation of AMPK at reperfusion protects the ischaemic-reperfused rat myocardium against infarction.

  Cardiovascular drugs and therapy 20100201

• Beta-adrenergic-AMPK pathway phosphorylates acetyl-CoA carboxylase in a high-epinephrine rat model, SPORTS.

  Obesity (Silver Spring, Md.) 20100101

• Bone morphogenetic protein receptors and signal transduction.

  Journal of biochemistry 20100101

• AICAR (5-aminoimidazole-4-carboxamide-1-beta-4-ribofuranoside) increases the production of toxic molecules and affects the profile of cytokines release in LPS-stimulated rat primary microglial cultures.

  Neurotoxicology 20100101

• Ambivalent effects of compound C (dorsomorphin) on inflammatory response in LPS-stimulated rat primary microglial cultures.

  Naunyn-Schmiedeberg's archives of pharmacology 20100101

• The novel function of nesfatin-1: anti-hyperglycemia.

  Biochemical and biophysical research communications 20100101

• Suppression effects of AICAR on insulin secretion involved in peroxisome proliferator-activated receptor gamma changes in INS-1 cells.

  Journal of endocrinological investigation 20100101

• Metabolic regulation of neuronal plasticity by the energy sensor AMPK.

  PloS one 20100101

• The role of hypothalamic AMP-activated protein kinase in ovariectomy-induced obesity in rats.

  Menopause (New York, N.Y.) 20100101

• The zebrafish embryo as a model for assessing off-target drug effects.

  Disease models & mechanisms 20100101

• Metformin has adenosine-monophosphate activated protein kinase (AMPK)-independent effects on LPS-stimulated rat primary microglial cultures.

  Pharmacological reports : PR 20100101

• Carbon monoxide (from CORM-2) inhibits high glucose-induced ICAM-1 expression via AMP-activated protein kinase and PPAR-gamma activations in endothelial cells.

  Atherosclerosis 20091201

• AMPK inhibitor Compound C stimulates ceramide production and promotes Bax redistribution and apoptosis in MCF7 breast carcinoma cells.

  Journal of lipid research 20091201

• AMP-activated protein kinase activator A-769662 is an inhibitor of the Na(+)-K(+)-ATPase.

  American journal of physiology. Cell physiology 20091201

• Adiponectin downregulates galectin-3 whose cellular form is elevated whereas its soluble form is reduced in type 2 diabetic monocytes.

  FEBS letters 20091119

• Adenosine monophosphate-activated protein kinase inhibits cardiac hypertrophy through reactivating peroxisome proliferator-activated receptor-alpha signaling pathway.

  European journal of pharmacology 20091012

• Resveratrol protects mitochondria against oxidative stress through AMP-activated protein kinase-mediated glycogen synthase kinase-3beta inhibition downstream of poly(ADP-ribose)polymerase-LKB1 pathway.

  Molecular pharmacology 20091001

• Vitamin D3 induces autophagy in human monocytes/macrophages via cathelicidin.

  Cell host & microbe 20090917

• Fenofibrate differentially regulates plasminogen activator inhibitor-1 gene expression via adenosine monophosphate-activated protein kinase-dependent induction of orphan nuclear receptor small heterodimer partner.

  Hepatology (Baltimore, Md.) 20090901

• Central AMPK contributes to sleep homeostasis in mice.

  Neuropharmacology 20090901

• Eicosapentaenoic acid stimulates AMP-activated protein kinase and increases visfatin secretion in cultured murine adipocytes.

  Clinical science (London, England : 1979) 20090814

• The AMPK agonist AICAR inhibits the growth of EGFRvIII-expressing glioblastomas by inhibiting lipogenesis.

  Proceedings of the National Academy of Sciences of the United States of America 20090804

• Pioglitazone acutely reduces insulin secretion and causes metabolic deceleration of the pancreatic beta-cell at submaximal glucose concentrations.

  Endocrinology 20090801

• AMPK inhibits myoblast differentiation through a PGC-1alpha-dependent mechanism.

  American journal of physiology. Endocrinology and metabolism 20090801

• Kidney bean husk extracts exert antitumor effect by inducing apoptosis involving AMP-activated protein kinase signaling pathway.

  Annals of the New York Academy of Sciences 20090801

• Regulatory effect of the AMPK-COX-2 signaling pathway in curcumin-induced apoptosis in HT-29 colon cancer cells.

  Annals of the New York Academy of Sciences 20090801

• Regulation of visceral and subcutaneous adipocyte lipolysis by acute AICAR-induced AMPK activation.

  Obesity (Silver Spring, Md.) 20090701

• AMP-activated protein kinase influences metabolic remodeling in H9c2 cells hypertrophied by arginine vasopressin.

  American journal of physiology. Heart and circulatory physiology 20090601

• AMP-activated protein kinase-dependent and -independent mechanisms underlying in vitro antiglioma action of compound C.

  Biochemical pharmacology 20090601

• Metformin prevents progression of heart failure in dogs: role of AMP-activated protein kinase.

  Circulation 20090519

• Insulin blunts the response of glucose-excited neurons in the ventrolateral-ventromedial hypothalamic nucleus to decreased glucose.

  American journal of physiology. Endocrinology and metabolism 20090501

• Regulation of erythrocyte survival by AMP-activated protein kinase.

  FASEB journal : official publication of the Federation of American Societies for Experimental Biology 20090401

• AMP kinase/cyclooxygenase-2 pathway regulates proliferation and apoptosis of cancer cells treated with quercetin.

  Experimental & molecular medicine 20090331

• Constitutively activated ALK2 and increased SMAD1/5 cooperatively induce bone morphogenetic protein signaling in fibrodysplasia ossificans progressiva.

  The Journal of biological chemistry 20090313

• AMP-activated protein kinase is involved in neural stem cell growth suppression and cell cycle arrest by 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside and glucose deprivation by down-regulating phospho-retinoblastoma protein and cyclin D.

  The Journal of biological chemistry 20090306

• Regulation of Cl(-) secretion by AMPK in vivo.

  Pflugers Archiv : European journal of physiology 20090301

• AMP-activated protein kinase functionally phosphorylates endothelial nitric oxide synthase Ser633.

  Circulation research 20090227

• Leptin regulates tau phosphorylation and amyloid through AMPK in neuronal cells.

  Biochemical and biophysical research communications 20090227

• Caloric restriction stimulates revascularization in response to ischemia via adiponectin-mediated activation of endothelial nitric-oxide synthase.

  The Journal of biological chemistry 20090116

• Applications of small molecule BMP inhibitors in physiology and disease.

  Cytokine & growth factor reviews 20090101

• A unique mutation of ALK2, G356D, found in a patient with fibrodysplasia ossificans progressiva is a moderately activated BMP type I receptor.

  Biochemical and biophysical research communications 20081219

• Differential regulation of AMP-activated kinase and AKT kinase in response to oxygen availability in crucian carp (Carassius carassius).

  American journal of physiology. Regulatory, integrative and comparative physiology 20081201

• AMPK mediates curcumin-induced cell death in CaOV3 ovarian cancer cells.

  Oncology reports 20081201

• BMP type I receptor inhibition reduces heterotopic [corrected] ossification.

  Nature medicine 20081201

• Triiodothyronine (T3) stimulates food intake via enhanced hypothalamic AMP-activated kinase activity.

  Regulatory peptides 20081129

• Leptin reduces Alzheimer's disease-related tau phosphorylation in neuronal cells.

  Biochemical and biophysical research communications 20081121

• Compound C inhibits clonal expansion of preadipocytes by increasing p21 level irrespectively of AMPK inhibition.

  Archives of biochemistry and biophysics 20081101

• AMP-activated protein kinase and hypoxic pulmonary vasoconstriction.

  European journal of pharmacology 20081024

• AMP-activated protein kinase promotes the differentiation of endothelial progenitor cells.

  Arteriosclerosis, thrombosis, and vascular biology 20081001

• Effects of an AMP-activated protein kinase inhibitor, compound C, on adipogenic differentiation of 3T3-L1 cells.

  Biological & pharmaceutical bulletin 20080901

• In vitro metformin anti-neoplastic activity in epithelial ovarian cancer.

  Gynecologic oncology 20080801

• Structure-activity relationship study of bone morphogenetic protein (BMP) signaling inhibitors.

  Bioorganic & medicinal chemistry letters 20080801

• Small molecule antagonizes autoinhibition and activates AMP-activated protein kinase in cells.

  The Journal of biological chemistry 20080606

• Activation of AMP-activated protein kinase, inhibition of pyruvate dehydrogenase activity, and redistribution of substrate partitioning mediate the acute insulin-sensitizing effects of troglitazone in skeletal muscle cells.

  Journal of cellular physiology 20080501

• Globular adiponectin, acting via adiponectin receptor-1, inhibits leptin-stimulated oesophageal adenocarcinoma cell proliferation.

  Molecular and cellular endocrinology 20080326

• AMP-activated protein kinase phosphorylates transcription factors of the CREB family.

  Journal of applied physiology (Bethesda, Md. : 1985) 20080201

• Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism.

  Nature chemical biology 20080101

• Small-molecule dissection of BMP signaling.

  Nature chemical biology 20080101

• Macropinocytosis is decreased in diabetic mouse macrophages and is regulated by AMPK.

  BMC immunology 20080101

• Dorsomorphin, a selective small molecule inhibitor of BMP signaling, promotes cardiomyogenesis in embryonic stem cells.

  PloS one 20080101

• The selectivity of protein kinase inhibitors: a further update.

  The Biochemical journal 20071215

• Compound C inhibits hypoxic activation of HIF-1 independent of AMPK.

  FEBS letters 20071211

• The relationship between p38 mitogen-activated protein kinase and AMP-activated protein kinase during myocardial ischemia.

  Cardiovascular research 20071201

• Polyphenolic compounds from Artemisia dracunculus L. inhibit PEPCK gene expression and gluconeogenesis in an H4IIE hepatoma cell line.

  American journal of physiology. Endocrinology and metabolism 20071201

• Rosiglitazone reduces glucose-induced oxidative stress mediated by NAD(P)H oxidase via AMPK-dependent mechanism.

  Arteriosclerosis, thrombosis, and vascular biology 20071201

• Adiponectin suppresses IkappaB kinase activation induced by tumor necrosis factor-alpha or high glucose in endothelial cells: role of cAMP and AMP kinase signaling.

  American journal of physiology. Endocrinology and metabolism 20071201

• Nicotine-induced activation of AMP-activated protein kinase inhibits fatty acid synthase in 3T3L1 adipocytes: a role for oxidant stress.

  The Journal of biological chemistry 20070914

• Possible role of 5'AMP-activated protein kinase in the metformin-mediated arrest of bovine oocytes at the germinal vesicle stage during in vitro maturation.

  Biology of reproduction 20070901

• Resveratrol stimulates AMP kinase activity in neurons.

  Proceedings of the National Academy of Sciences of the United States of America 20070424

• Apoptotic effect of EGCG in HT-29 colon cancer cells via AMPK signal pathway.

  Cancer letters 20070308

• Critical role of 5'-AMP-activated protein kinase in the stimulation of glucose transport in response to inhibition of oxidative phosphorylation.

  American journal of physiology. Cell physiology 20070101

• The changing AMPK expression profile in differentiating mouse skeletal muscle myoblast cells helps confer increasing resistance to apoptosis.

  Experimental physiology 20070101

• Inhibition by glucose or leptin of hypothalamic neurons expressing neuropeptide Y requires changes in AMP-activated protein kinase activity.

  Diabetologia 20070101

• AMP-activated protein kinase and the regulation of autophagic proteolysis.

  The Journal of biological chemistry 20061117

• Role of AMP-activated protein kinase in mechanism of metformin action.

  The Journal of clinical investigation 20011015

• Noncanonical BMP signaling regulates cyclooxygenase-2 transcription.

  Molecular endocrinology (Baltimore, Md.)