ampk

AMPK activator 2 hydrochloride is a fluoroguanidine-containing derivative that up-regulates the AMPK signaling pathway and down-regulates mTOR/4EBP1/p70S6K.AMPK activator 2 hydrochloride inhibits the proliferation and migration of human cancer cell lines (UMUC3, T24, A549).

AMPK activator 4 is a potent and selective AMPK activator that does not inhibit mitochondrial complex I. It selectively activates AMPK in muscle tissue, dose-dependently improves glucose tolerance in normal mice, significantly reduces fasting glucose levels, and improves insulin resistance in db db diabetic mice. [AMPK activator 4 has hypoglycemic effects.]

AMPK activator 12 is an AMPK activator and GDF15 inducer that elevates the expression level of GDF15 protein in human hepatocytes, which can be used for cancer research.

AMPK Activator 13 is a potent activator of the AMPK pathway, effectively inhibiting mitotic clonal expansion in 3T3-L1 cells and enhancing mitochondrial oxygen consumption rates. This compound is utilized in the study of obesity [1].

AMPK activator 1 is an AMPK activator (compound No.1-75) with an EC50 of less than 0.1 μM.

AMPK activator C2 is an AMPK allosteric activator.

AMPK activator 7 (compound I-3-24) is an AMPK activator with an EC50 of 8.8 nM, useful in studies involving AMPK disorders such as type 2 diabetes, hyperglycaemia, metabolic syndrome, obesity, hypercholesterolaemia, and hypertension.

AMPK activator 2 is a chloroformin derivative with potential anticancer activity, which can up-regulate AMPK signaling pathway and down-regulate mTOR/4EBP1/p70S6K, and inhibit proliferation and migration of human cancer cell lines (UMUC3, T24, A549).

AMPK-α1β1γ1 activator 1 (M1), an acyl glucuronide metabolite derived from an Indole-3-carboxylic Acid-based AMPK activator, selectively activates the β1 isoforms of human AMPK with an EC50 of 38.1 nM through direct binding to the human AMPK α1β1γ1 isoform; it is utilized in diabetic nephropathy research [1].

AMPK activator 8 (Compound 2) is an AMP-activated protein kinase (AMPK) activator that acts on rAMPK α1β1γ1 (EC50: 11 nM), rAMPK α2β1γ1 (EC50: 27 nM), rAMPK α1β2γ1 (EC50: 4 nM), rAMPK α2β2 AMPK activator 8 can be used to study type 2 diabetes.

AMPK Activator 11 is a nanomolar potent inhibitor of cell proliferation in various colorectal carcinomas (CRCs), acting through the selective activation of AMP-activated protein kinase (AMPK) and enhancement of oxidative phosphorylation (OXPHOS) (mitochondrial metabolism). This compound demonstrates particular efficacy in inhibiting RKO xenograft growth, rendering it useful for anti-tumor and metabolic disease research [1].

AMPK Activator 9 (ZM-6), a potent activator of AMPK (α2β1γ1), demonstrates an EC50 of 1.1 µM, indicating its strong efficacy in activating AMPK. This compound holds promise for type 2 diabetes research, highlighting its potential application in understanding and possibly treating this condition.

SC4 is a potent, direct AMPK activator. SC4 preferentially activates α2 complexes and stimulates skeletal muscle glucose uptake.

Compound 38-S is an orally active CB1R/AMPK modulator with a K i of 0.81 nM and an IC50 of 3.9 nM for CB1R. This compound activates AMPK and has been shown to decrease food intake and body weight, in addition to enhancing glucose tolerance and insulin sensitivity [1].

AMPK activator

AMPK-IN-1 is an activator of the AMP-activated protein kinase (AMPK) enzyme, targeting the α2β2γ1 isoform with an EC50 of 551 nM, and induces phosphorylation of eEF2 independent of the mTORC1 pathway.

AMPK-IN-3 is a novel, selective and potent AMPK inhibitor with inhibitory effects on AMPK (α2), AMPK (α1) and KDR, with IC50 values of 60.7, 107 and 3820 nM, respectively.AMPK-IN-3 showed anticancer activity in K562 cells.

AMPK activator 6 (Compound GC) activates the AMPK pathway and reduces lipid content in HepG2 and 3T3-L1 cells. It significantly suppresses increases in total cholesterol (TC), low-density lipoprotein-C (LDL-C), triglyceride (TG), and other biochemical indices in blood serum, holding research value in non-alcoholic fatty liver disease (NAFLD) and metabolic syndrome.

Flufenamic acid (Arlef) is an anthranilic acid derivative with analgesic, anti-inflammatory, and antipyretic properties. It is used in musculoskeletal and joint disorders and administered by mouth and topically.

Methyl cinnamate, a tyrosinase inhibitor and a flavoring compound, has antimicrobial, antiadipogenic, vasorelaxant, and anti-inflammatory effects.

Glabridin (KB-289522) may serve as an anti-inflammatory agent in diabetes-related vascular dysfunction, through regulating the synthesis and activity of iNOS under high-glucose levels; may possess a therapeutic effect on metabolic disorders( such as diabetes and hyperglycemia), by modulating glucose metabolism through AMPK in skeletal muscle cells. Glabridin may have potential as a chemopreventive agent against liver Y metastasis, by inhibiting the invasion of human HCC cells.

AICAR (Acadesine) is an AMPK activator that causes ZMP accumulation, thereby mimicking the stimulatory effect of AMP on both AMPK and AMPKK. It is commonly used in research related to diabetes, cardiovascular diseases, and tumors.

Daphnetin (7,8-Dihydroxycoumarin), a natural coumarin derivative, is a protein kinase inhibitor with inhibitory for EGFR (IC50: 7.67 μM), PKA (IC50: 9.33 μM), and PKC (IC50: 25.01 μM), also exhibit anti-oxidant and anti-inflammatory activities.

Buformin hydrochloride (NSC-528218) is a potent AMPK activator,an oral antidiabetic drug of the biguanide class. Buformin delays the absorption of glucose from the gastrointestinal tract increases insulin sensitivity and glucose uptake into cells and inhibits synthesis of glucose by the liver. Biguanides may antagonize the action of glucagon, thus reducing fasting glucose levels.

Sesamol (1,3-Benzodioxol-5-ol) could decrease lung inflammation and lipopolysaccharide (LPS)-induced lung injury in rats. Sesamol ameliorates inflammatory and oxidative damage by upregulating AMPK activation and Nrf2 signaling and blocking the NF-κB and MAPK signaling pathways and inhibits melanin biosynthesis by down-regulating tyrosinase activity and melanin production via regulation of gene expression of melanogenesis-related proteins through modulation of MITF activity, which promotes phosphorylation of p38 and JNK in melan-a cells.

Urolithin B is one of the gut microbial metabolites of ellagitannins and is found in diverse plant foods, including pomegranates, berries, walnuts, tropical fruits, and medicinal herbs. Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα, and suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass. Urolithin B has anti-inflammatory and antioxidant effects.

RGX-202 (β-GPA) is a creatine analog that alters skeletal muscle energy expenditure. It reduces cellular ATP, creatine, and phosphocreatine levels and stimulates AMP-activated protein kinase (AMPK), activating PPARγ coactivator 1α (PGC-1α).

Chitosan oligosaccharide (COS) is an oligomer of β-(1→4)-linked D-glucosamine that activates AMPK while inhibiting inflammatory signaling pathways, including NF-κB and MAPK.

Danthron (Antrapurol) is a natural product, regulates glucose, and lipid metabolism by activating AMPK.

Metformin (1,1-Dimethylbiguanide) is an AMPK activator with blood-brain barrier permeability. Metformin may improve glycemic control by increasing insulin sensitivity and decreasing intestinal glucose uptake, and is commonly used in type 2 diabetes research.

Phenformin hydrochloride (Phenformin HCl) is an agent belonging to the biguanide class of antidiabetics with antihyperglycemic activity.

Metformin hydrochloride (1,1-Dimethylbiguanide hydrochloride), a widely used anti-diabetic drug, exhibits potential anti-Y properties by inhibiting the proliferation of various Y cells, including colon and prostate.

1. Berberine (Umbellatine) is a potent oral hypoglycemic agent with beneficial effects on lipid metabolism. 2. Berberine may as a broad-spectrum anti-microbial medicine, a complementary therapeutic agent for HIV/AIDS. 3. Berberine seems to act as an herbal antidepressant and a neuroprotector against neurodegenerative disorders. 4. Berberine is used in histology for staining heparin in mast cells. As a natural dye, berberine has a colour index of 7516. 5. Berberine reduces hepatic fat content in rats with nonalcoholic fatty liver disease; also prevents proliferation of hepatic stellate cells (HSCs), which are central for the development of fibrosis during liver injury. 6. Berberine can ameliorate proinflammatory cytokines-induced intestinal epithelial tight junction damage in vitro, and berberine may be one of the targeted therapeutic agents that can restore barrier function in intestinal disease states. 7. Berberine has antineoplastic effects, including breast cancer, leukemia, melanoma, epidermoid carcinoma, hepatoma, pancreatic cancer, oral carcinoma, tongue carcinoma, glioblastoma, prostate carcinoma and gastric carcinoma, etc.

1. Nootkatone can provide effective tick control. 2. (+)-Nootkatone has antiallergic, anti-inflammatory, and antiplatelet activities. 3. Nootkatone can prevent obesity and improve physical performance through AMPK activation in skeletal muscle and liver.

Doxorubicin hydrochloride (Adriamycin) belongs to the anthracycline class of antibiotics and is an inhibitor of human DNA topoisomerase I II (IC50=0.8 2.67 μM). Doxorubicin hydrochloride exhibits cytotoxicity and antitumor activity. Doxorubicin hydrochloride reduces the phosphorylation of AMPK and its downstream target protein acetyl coenzyme A carboxylase, and induces apoptosis and autophagy.

Sakamototide substrate peptide acetate is a peptide substrate of AMPK kinase family and can be used for the determination of kinase activity.

N,N-Didesethyl Sunitinib Hydrochloride is a potent AMPK inhibitor with IC50 of 393 nM and 141 nM for AMPKα1 and AMPK2,respectively.

Mefloquine (Ro 215998), a quinoline antimalarial agent, is an anti-SARS-CoV-2 entry inhibitor. Mefloquine is also a K+ channel (KvQT1/minK) antagonist with an IC50 of ~1 μM. Mefloquine can be used for malaria, systemic lupus erythematosus, and cancer research.

MOTS-c(Human) Acetate is a mitochondrial-derived peptide. MOTS-c(human) acetate induces the accumulation of AMP analog AICAR, increases activation of AMPK and expression of its downstream GLUT4. MOTS-c(human) acetate induces glucose uptake and improves insulin sensitivity. MOTS-c(human) acetate has implications in the regulation of obesity, diabetes, exercise, and longevity.

AMARA peptide acetate is a substrate for SIK and AMPK.AMARA peptide is a minimal substrate of several members of the protein kinases family. It consists of the phosphorylation site for AMP-activated Protein Kinase (AMPK).

TCS-PIM-1-4a (SMI-4a), a Pim inhibitor, blocks mTORC1 activity through activation of AMPK and kills a wide range of both myeloid and lymphoid cell lines (IC50=0.8-40 μM).

Annaosanchun (YC-6) is potentially for the treatment of acute ischemic stroke (AIS).

MRT199665 is an effective and ATP-competitive, selective MARK/SIK/AMPK inhibitor (IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively). MRT199665 suppresses the phosphorylation of S

HTH-01-015 is a selective NUAK1 inhibitor with an IC50 of 100 nM.

Ampkinone is an indirect AMPK activator.

IM156 (HL156A; HL271 acetate) is a chemical derivative of Metformin. IM156 is a potent and orally active AMPK activator that increases AMPK phosphorylation. IM156 attenuates aging-associated cognitive impairment in animal model [1] [2]. IM156 is a potent oxidative phosphorylation (OXPHOS) inhibitor which is able to be used for the research of solid tumors [3].

Amarogentin is mainly extracted from Swertia and Gentiana roots. It plays cemopreventive therapeutic role during liver carcinogenesis through modulation of cell cycle and apoptosis

A-769662 is an effective, reversible AMPK activator(EC50=0.8 μM).

Chikusetsusaponin IVa (Calenduloside F) is a novel AMPK activator, can induce insulin secretion from βTC3 cells via GPR4 mediated calcium and PKC pathways, may be developed into a new potential for therapeutic agent used in T2DM patients.