- Cat. No.
- A11071
A-769662
A-769662 is a new activator of AMP-activated protein kinase (AMPK).
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AMPK activators and inhibitors act on adenosine monophosphate-activated protein kinase (AMPK), an energy sensor. The enzyme is a heterotrimer of a catalytic α subunit with regulatory β and γ subunits. When cellular energy falls, AMPK switches off anabolic pathways such as fatty acid synthesis and switches on catabolic processes. A 2001 study linked AMPK activation to the actions of metformin and introduced compound C, also known as dorsomorphin, as an inhibitor. A-769662, reported in 2006, was among the first direct small-molecule AMPK activators. MK8722 and ex229 also activate the kinase directly, whereas acadesine acts through a cellular metabolite that mimics adenosine monophosphate.
A-769662 is a new activator of AMP-activated protein kinase (AMPK).
Synonyms: BML275
BML-275 is a cell-permeable pyrazolopyrimidine compound shown to be an AMP-activated protein kinase (AMPK) and fatty acid synthase inhibitor.
Synonyms: AICA-riboside; Aicar; NSC 105823
Acadesine is a selective activator of AMPK in both hepatocytes and adipocytes.
Synonyms: Compound C; BML-275
Dorsomorphin, also known as BML-275, is a selective small molecule inhibitor of BMP signaling, which promotes cardiomyogenesis in embryonic stem cells. Dorsomorphin reverses the mesenchymal phenotype of breast cancer initiating cells by inhibition of bone morphogenetic protein signaling.
Synonyms: 1,1-Dimethylbiguanide
Metformin is an AMP-activated protein kinase (AMPK) activator that improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose.
Synonyms: compound 991
EX229 (compound 991) is a potent AMPK activator that is 5-10-fold more potent than A769662 in activating AMPK.
Phenformin hydrochloride is a hydrochloride salt of phenformin from the biguanide drug class that displays anti-diabetic activity.
WZ4003 is a highly specific NUAK kinase inhibitor with IC50 of 20 nM and 100 nM for NUAK1 and NUAK2
10-Gingerol is an AMPK agonist derived from ginger oleoresin, exhibiting notable anti-inflammatory, antioxidant, and anti-proliferative properties. It effectively suppresses neointimal hyperplasia and inhibits the proliferation of vascular smooth muscle cells. Demonstrating significant radical scavenging activities, 10-Gingerol has IC50 values of 10.47 μM against DPPH, 1.68 μM against superoxide, and 1.35 μM against hydroxyl radicals. This compound also inhibits MDA-MB-231 tumor cell line proliferation with an IC50 of 12.1 μM, while targeting the PI3K/Akt signaling pathway to suppress proliferation, migration, invasion, and promote apoptosis. It holds potential for research applications in ulcerative colitis.
Vaccarin, a flavonoid glycoside, is considered one of the major active constituents of Vaccaria segetalis.
Synonyms: Dantron; Chrysazin; 1,8-Dihydroxyanthraquinone
Danthron is an AMPK activator that plays a critical role in regulating glucose and lipid metabolism. Derived from the traditional Chinese medicinal plant Salvia miltiorrhiza Bunge, Danthron has demonstrated potential in enhancing cellular energy balance. Its biological activity makes it a valuable reagent for research in metabolic disorders and related therapeutic applications.
Synonyms: ESP-55016
ETC-1002 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).
HTH-01-015 is a potent and selective inhibitor of NUAK1 (IC50 = 100 nM) and does not affect the activity of a panel of 139 other kinases, including additional AMPK family members.
Synonyms: C24
YLF-466D is an allosteric AMPK activator.
PF-06409577 is orally bioavailable AMPK activator with EC50 of 7 nM for α1β1γ1 in the TR-FRET assay and it shows no detectable inhibition of hERG in a patch-clamp assay (100 μM) and was not an inhibitor (IC50 > 100 μM) of the microsomal activities of major human cytochrome P450 isoforms.
MK-3903 is a potent and selective AMPK activator (EC50 = 8 nM). MK-3903 exhibited robust target engagement in mouse liver following oral dosing, leading to improved lipid metabolism and insulin sensitization in mice.
7-Methoxyisoflavone is an isoflavone derivative and also an activator of adenosine monophosphate-activated protein kinase (AMPK).
MARK-IN-2 is a potent microtubule affinity regulating kinase (MARK) inhibitor with an IC50 of 5 nM.
MARK-IN-1 is a potent microtubule affinity regulating kinase (MARK) inhibitor with an IC50 of
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O-304 is a first-in-class, orally available pan-AMPK activator, which increases AMPK activity by suppressing the dephosphorylation of pAMPK.
Synonyms: COS
Chitosan oligosaccharide (COS) is an oligomer of β-(1→4)-linked D-glucosamine. Chitosan oligosaccharide (COS) activates AMPK and inhibits inflammatory signaling pathways including NF-κB and MAPK pathways.
STO-609 is a selective and cell-permeable inhibitor of the Ca2+/calmodulin-dependent protein kinase kinase (CaM-KK), with Ki values of 80 and 15 ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively.