amp-activated protein kinase

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.

MK8722 is an effective and systemic activator of pan-AMPK.

Dorsomorphin (BML-275) is an AMPK inhibitor (Ki=109 nM) that is selective and ATP-competitive. Dorsomorphin inhibits the BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin induces autophagy, and possesses antitumor activity.

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.

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

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.

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

AICAR (Acadesine) is an AMPK activator. AICAR has the functions of metabolic regulation, muscle function regulation, anti-cancer effect, neuroprotection and anti-aging.

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.

Bempedoic acid (ETC1002) 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. Bempedoic acid(ETC1002) is absorbed rapidly in the small intestine and enters the liver through cell surface receptors different from those transporters that selectively take up statins. Bempedoic acid(ETC1002) is a regulator of lipid and carbohydrate metabolism.

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

GSK-690693 is a pan-Akt inhibitor targeting Akt1 2 3 with IC50 of 2 nM 13 nM 9 nM, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. Phase 1.

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.

TMPA is a nuclear receptor Nur77 and LKB1 interaction antagonist.

Doxorubicin (Adriamycin) is a fluorescent anthracycline antitumor antibiotic that inhibits Topoisomerase I/II, induces apoptosis and autophagy, downregulates the AMPK signaling pathway, and is commonly used in cancer chemotherapy as well as in models of nephritis and heart failure.

MT 63-78 is a specific and effective direct AMPK activator (EC50: 25 μM) that blocks prostate cancer growth by inhibiting the lipogenesis and mTORC1 pathways. It has antitumor effects and induces cell mitotic arrest and apoptosis.

Karanjin is a flavonoid obtained from the seeds of the karanja tree.Karanjin induces GLUT4 translocation in skeletal muscle cells by increasing AMPK activity. Karanjin can induce cancer cell death through cell cycle arrest and enhance apoptosis.

STO-609 is a specific and cell-permeable inhibitor of the Ca2+/calmodulin-dependent protein kinase kinase (CaM-KK) for recombinant CaM-KKα/KKβ (Ki: 80/15 ng/mL).

Platycodin D may stimulate TNF-α synthesis or inhibit degradation of TNF-α mRNA. Platycodin D (10/30 μM) suppresses prostaglandin E2 production in rat peritoneal macrophages stimulated by the protein kinase C activator 12-O-tetradecanoyl phorbol 13-acetate (TPA). Platycodin D and D3 are useful as expectorant agents in the treatment of various airway diseases, they can increase mucin release from rat and hamster tracheal surface epithelial cell culture and also from intact rat trachea upon nebulization.

Gomisin J is a natural product and have vasodilatory activity. Gomisin J suppresses lipid accumulation by regulating the expression of lipogenic and lipolytic enzymes and inflammatory molecules through activation of AMPK, LKB1 and Ca2+/calmodulin-dependent protein kinase II and inhibition of fetuin-A in HepG2 cells.

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

Dorsomorphin dihydrochloride (BML-275 2HCl) is a potent, selective and ATP-competitive AMPK inhibitor (Ki: 109 nM) and does not exhibit significant activity on structurally related kinases.

WZ4003, a highly selective NUAK kinase inhibitor, is with IC50 of 20 nM and 100 nM for NUAK1 and NUAK2, respectively. It is no significant inhibition on 139 other kinases.

O-304 is a pan-activator of AMP-activated protein kinase (AMPK).