AMPK
In eukaryotic cells AMP-activated protein kinase (AMPK) plays a major role in regulating cellular energy balance. AMPK responds to changes in intracellular adenine nucleotide levels, being activated by an increase in AMP/ADP relative to ATP.Mammalian AMPK exists as 12 different complexes composed of different subunit isoforms. AMPK is activated by phosphorylation of threonine 172 (T172) within the activation segment of the KD of the a subunit. In mammals, calcium/calmodulin dependent protein kinase kinase (CaMKK) b and liver kinase B1 (LKB1) have been identified as the two upstream kinases in the cascade.AMPK plays an important role in maintaining energy homeostasis in eukaryotic cells. In multicellular organisms, the role of AMPK has been adapted to play a role in integrating energy metabolism at an organismal level.There has been a significant development over the last few years in identifying small molecule direct AMPK activators, and we now understand the mechanism by which a major class of these drugs work to activate the kinase.
References
1.Carling D. Curr Opin Cell Biol. 2017 Apr;45:31-37.
References
1.Carling D. Curr Opin Cell Biol. 2017 Apr;45:31-37.
Membrane Transporter/Ion Channel
AMPK(58)
ASBT Transporter(6)
BCRP(10)
Beta Amyloid(69)
Carbonic Anhydrase(40)
Chloride Channel(34)
CRAC Channel(0)
CRM1(5)
Exportin-1(5)
FABP(6)
GAT(63)
GLUT(5)
Glutamate Transporter(1)
GlyT(13)
HCN Channel(5)
iGluR(52)
Monoamine Transporter(26)
Monocarboxylate Transporter(12)
MTP(1)
nAChR(5)
NADPH(35)
Na-K-ATPase(2)
NKCC(4)
NMDAR(65)
OCT(4)
Other Targets(13)
P2X Receptor(23)
P-glycoprotein(14)
Proton Pump(38)
Sodium Channel(147)
TRP/TRPV Channel(115)
URAT1(1)
AMPK
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AMPK activator 12
catalog no : M37213
cas no: 431920-24-0
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 4
catalog no : M35625
cas no: 2493239-46-4
AMPK activator 4 is a potent and selective AMPK activator that does not inhibit mitochondrial complex I. -
N,N-Didesethyl Sunitinib Hydrochloride
catalog no : M35336
cas no: 873077-70-4
N,N-Didesethyl Sunitinib Hydrochloride is a potent AMPK inhibitor with IC50 of 393 nM and 141 nM for AMPKα1 and AMPK2,respectively. -
Aldometanib
catalog no : M35330
cas no: 2904601-67-6
Aldometanib (LXY-05-029) is an orally active aldolase inhibitor that prevents FBP from binding to v-ATPase-associated aldolase and activates lysosomal AMPK, useful in metabolic homeostasis research . -
YLF-466D
catalog no : M33176
cas no: 1273323-67-3
YLF-466D (C24) is a novel AMPK activator that inhibits platelet aggregation.