A novel potent, pan-AMPK activator with similar potency for all AMPK heterotrimers.

A potent, allosteric, α1-selective small molecule activator of AMPK (EC50=20 nM).

A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM, little effect on GPPase/FBPase activity.

Acadesine results in accumulation of ZMP, which mimics the stimulating effect of AMP on AMPK and AMPK kinase. Phase 3.

AMPK activator 991 is an allosteric AMPK activator, activates non-phosphorylated Thr172 AMPK in vitro binds to α1β1γ1 and α2β1γ1 with Kd of 0.13 and 0.17 uM, respectively..

AMPK activator SC4 is a potent, specific activator of α2β2-AMPK complexes with EC50 of 17.2 and 82.1 nM for α2β2γ1 and α2β2γ3, the predominant AMPK isoform complexes in human skeletal muscle.

BAY-3827 (BAY3827) is a potent, selective inhibitor of AMPK as tool compound to evaluate the therapeutic potential of AMPK inhibition in MYC-dependent tumors; strongly inhibits Acetyl-CoA carboxylase (ACC) phosphorylation in COLO 320DM and IMR-32 cells, but fails to inhibit the proliferation of cells with dysregulated c-MYC or N-MYC.

Dorsomorphin 2Hcl (Compound C; BML-275) has been shown to act as a potent and selective inhibitor of AMPK (AMP-activated protein kinase; Ki = 109 nM), induced by AICAR and metformin; also inhibits ALK2, ALK3, and ALK 6 .

ETC-1002(ESP-55016) is a novel, first-in-class, orally available, once-daily LDL-C lowering small molecule; activator of hepatic AMP-activated protein kinase (AMPK); also has potent inhibitory activity against hepatic ATP-citrate lyase(IC50=29 uM).

EX229 is a small molecule AMPK activator that dose-dependently increases AMPK activity of α1-, α2-, β1- and β2-containing complexes at 50 uM

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

MK-3903 is a potent and selective AMP-activated protein kinase (AMPK) activator with an EC50 of 8 nM. generation of catalytically active enzyme.

MK-8722 is a systemic, Direct Pan-Activator of AMP-Activated Protein Kinase.

PF-06409577 is a potent and selective allosteric activator of AMPK α1β1γ1 isoform with an EC50 of 7 nM.

ZLN024 Hcl is a novel AMPK allosteric activator; activated α1β1γ1 and α2β1γ1 by around 2–2.5 fold with an EC50 of about 1–2 uM. IC50 value: 1-2 uM (EC50) [1] Target: AMPK activator ZLN024 activated AMPK in L6 myotubes and stimulated glucose uptake and

Dorsomorphin(Compound C; BML-275) has been shown to act as a potent and selective inhibitor of AMPK (AMP-activated protein kinase; Ki = 109 nM), induced by AICAR and metformin; also inhibits the bone morphogenetic protein type 1 receptors ACTR-I (ALK2), B

GSK621 (GSK-621) is a potent, specific AMPK agonist (activator), induces cytotoxicity in AML (IC50=13-30 uM) but not in normal hematopoietic cells; GSK621 is more potent than A-769662 at inducing AMPK activation, as measured by the level of ACC phosphoryl

IM156, a metformin derivative, is a potent activator of AMPK that increases AMPK phosphorylation. IM156 blocks oxidative phosphorylation (OXPHOS) through the inhibition of complex I and increases apoptosis. IM156 ameliorates various types of fibrosis and

RSVA405 is a potent, orally active activator of AMPK, with an EC50 of 1 μM. RSVA405 facilitates CaMKKβ-dependent activation of AMPK, inhibits mTOR, and promotes autophagy to increase Aβ degradation. RSVA405 has anti-inflammatory effects through the inhibition of STAT3 function. RSVA405 also can be used for the research of obesity.

Metformin D6 hydrochloride is a deuterium labeled Metformin hydrochloride. Metformin hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to activation of AMPK, enhancing insulin sensitivity for type 2 diabetes research. Metformin hydrochloride triggers autophagy.

Buformin (1-Butylbiguanide) is a potent and orally active biguanide antidiabetic agent, an?AMPK?activator. Buformin decreases hepatic gluconeogenesis and lowers blood glucose production in vivo. Buformin also has anti-cancer activities and is applied in cancer study (such as, cervical cancer and breast cancer, et al).

Marein has the neuroprotective effect due to a reduction of damage to mitochondria function and activation of the AMPK signal pathway. Marein improves insulin resistance induced by high glucose in HepG2 cells through CaMKK/AMPK/GLUT1 to promote glucose uptake, through IRS/Akt/GSK-3β to increase glycogen synthesis, and through Akt/FoxO1 to decrease gluconeogenesis. Marein is a HDAC inhibitor with an IC50 of 100 μM. Marein has beneficial antioxidative, antihypertensive, antihyperlipidemic and antidiabetic effects.

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.

AMPK activator 4 is a potent AMPK activator without inhibition of mitochondrial complex I. AMPK activator 4 selectively activates AMPK in the muscle tissues. AMPK activator 4 dose-dependently improves glucose tolerance in normal mice, and significantly lowers fasting blood glucose level and ameliorates insulin resistance in db/db diabetic mice. Anti-hyperglycemic effect.

Metformin (1,1-Dimethylbiguanide), a widely used drug for treatment of type 2 diabetes, activates AMP-activated protein kinase (AMPK) in hepatocytes. Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells throu

Galegine hydrochloride, a guanidine derivative, contributes to weight loss in mice. Guanidine hydrochloride is the compound derived from G. officinalis, which gave rise to the biguanides, metformin and phenformin. Galegine hydrochloride activates AMPK in 3T3-L1 adipocytes and L6 myotubes, as well as in the H4IIE rat hepatoma and HEK293 human kidney cell lines. Galegine hydrochloride has antibacterial activity, with minimum inhibitory concentration of 4 mg/L against Staphylococcus aureus strains.

Malvidin-3-O-arabinoside chloride ameliorates ethyl carbamate-induced oxidative damage by stimulating AMPK-mediated autophagy.

MARK-IN-4 is a potent microtubule affinity regulating kinase (MARK) inhibitor with an IC50 of 1 nM. Inhibition of microtubule affinity regulating kinase (MARK) represents a potentially attractive means of arresting neurofibrillary tangle pathology in Alzheimer's disease.

Kazinol U inhibits melanogenesis through the inhibition of tyrosinase-related proteins via AMPK activation.

10Z-Hymenialdisine ((Z)-Hymenialdisine) is a natural bioactive pyrrole alkaloid. 10Z-Hymenialdisine is a pan kinase inhibitor, and has anticancer activities.

HTH-02-006 is a potent, selective reversible inhibitor of NUAK1/2 with binding IC50 of 8/126 nM, respectively.HTH-02-006 reduces MYPT1(S445) phosphorylation in HuCCT-1 cells, suggesting NUAK1/2 inhibition.HTH-02-006 ameliorates YAP(S127A)-induced hepatomegaly, and reduces MYPT1(S445) phosphorylation.HTH-02-006 delays the outgrowth of YAP-induced HuCCT-1 xenograft tumors in nude mice.HTH-02-006 downregulated E2F, EMT, and MYC hallmark gene sets after NUAK2 inhibition in PC cells.HTH-02-006 slowed tumor growth and proliferation rates in a syngeneic allograft model and in radical prostatectomy patient derived explants.HTH-02-006 treatment led to inactivation of YAP and the downregulation of NUAK2 and MYC protein levels.

MOTS-c, a mitochondria-derived peptide (MDP), exerts antinociceptive and anti-inflammatory effects through activating AMPK pathway and inhibiting MAP kinases-c-fos signaling pathway.

AMPK activator 7 (compound I-3-24) is a an AMPK activator with the EC50 of 8.8 nM. AMPK activator 7 can be used for the research of diseases involving AMPK, particularly diseases such as type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia and/or hypertension.

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

AMPK activator 8 (Compound 2) is an AMP-activated protein kinase (AMPK) activator with EC50s of 11, 27, 4, 2, and 4 nM for rAMPK α1β1γ1, rAMPK α2β1γ1, rAMPK α1β2γ1, rAMPK α2β2γ1, rAMPK α2β2γ3, respectively. AMPK activator 8 can be used for the research of type 2 diabetes.

Aldometanib (LXY-05-029) is an orally active aldolase inhibitor. Aldometanib can activate lysosomal adenosine monophosphate-activated protein kinase (AMPK) and decreases blood glucose. Aldometanib can be used for the research of metabolic homeostasis.

YLF-466D is an AMPK activator that inhibits platelet aggregation with IC50 of 84 μM.

BI-9774 (BI 9774) is a potent pan-AMPK activator with EC50 of 64 nM in an ADP-Glo kinase assay with human AMPK (α1β1γ1) and EC50 of 8 nM in a cellular GLUT4 translocation assay.

KI-301670 is a novel potent, specific NUAK1 inhibitor, disturbs NUAK1 signaling by targeting its ATP binding site, effectively inhibits the PI3K/AKT pathway in pancreatic cancer cells.

MSG011 is a potent, pan AMPK isoform activator with EC50 of 140.4 nM, 248.9 nM, 553.4 nM, and 472.9 nM for α1β1γ1, α1β2γ1, α2β1γ1, and α2β2γ1, respectively.

PXL770 is a novel orally bioavailable, small-molecule direct AMPK activator with EC50 of 16.2, 42.1 and 64 nM for α1β1γ1, α1β1γ2 and α1β1γ3, directly increases AMPK activity by both allosteric activation and protection from dephosphorylation.

PXL770 is a novel orally bioavailable, small-molecule direct AMPK activator with EC50 of 16.2, 42.1 and 64 nM for α1β1γ1, α1β1γ2 and α1β1γ3, directly increases AMPK activity by both allosteric activation and protection from dephosphorylation.

RX-375 (RX375) is an indirect small-molecule activator of AMPK by directly binds to Prohibitins (PHB1 and PHB2), induces dissociation of AMPK-PHBs complex.

ZLN-024 hydrochloride is a potent, allosteric AMPK activator that has no effect on mitochondrial function or the ADP/ATP ratio, directly activate recombinant AMPK α1β1γ1 and its homologue α2β1γ1 with EC50 of 0.42 uM and 0.95 uM, respectively.