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

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 .

AMPK activator SC4 is a highly specific and potent activator of the α2β2-AMPK complexes, which are the predominant AMPK isoform complexes found in human skeletal muscle. SC4 demonstrates significant efficacy with EC50 values of 17.2 nM for the α2β2γ1 complex and 82.1 nM for the α2β2γ3 complex. These low EC50 values indicate that SC4 is effective at relatively low concentrations, making it a promising compound for targeting AMPK in skeletal muscle. This specificity and potency suggest potential therapeutic applications in conditions where AMPK activation is beneficial, such as metabolic disorders, muscle function, and energy homeostasis.

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.

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

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.

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.

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.

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.

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.

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

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.

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.

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.

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

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

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

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

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

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

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

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.

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.

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 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.

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.

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

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

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).