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In vitro: Phenformin stimulates the phosphorylation and activation of AMPKalpha1 and AMPKalpha2 without altering LKB1 activity. Phenformin increases AMPK activity and phosphorylation in the isolated heart, the increase in AMPK activity is always preceded by and correlated with increased cytosolic [AMP]. Phenformin is a 50-fold more potent inhibitor of mitochondrial complex I than metformin. Phenformin robustly induces apoptosis in LKB1 deficient NSCLC cell lines. Phenformin at 2 mM similarly induces AMPK signaling as shown by increased P-AMPK and P-Raptor levels. Phenformin induces higher levels of cellular stress, triggering induction of P-Ser51 eIF2α and its downstream target CHOP, and markers of apoptosis at later times. Phenformin and AICAR increases AMPK activity in H441 cells in a dose-dependent fashion, stimulating the kinase maximally at 5-10 mm and 2 mm, respectively. Phenformin significantly decreases basal ion transport (measured as short circuit current) across H441 monolayers by approximately 50% compared with that of controls. Phenformin and AICAR significantly reduce amiloride-sensitive transepithelial Na+ transport compared with controls. Phenformin and AICAR suppress amiloride-sensitive Na+ transport across H441 cells via a pathway that includes activation of AMPK and inhibition of both apical Na+ entry through ENaC and basolateral Na+ extrusion via the Na+,K+-ATPase.
In vivo: Phenformin also increases levels of P-eIF2α and its target BiP/Grp78 in normal lung as well as in lung tumors of mice. Phenformin induces a significant increase in survival and therapeutic response in KLluc mice following long-term treatment. Phenformin-treated rats reveals a tendency towards a decrease in blood insulin level (radioimmunoassay).
| Molecular Weight | 241.72 |
| Formula | C10H15N5.HCl |
| CAS Number | 834-28-6 |
| Solubility (25°C) | Water 12 mg/mL DMSO 9 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related AMPK Products |
|---|
| Dorsomorphin dihydrochloride
Dorsomorphin (BML-275; Compound C) dihydrochloride is a potent inhibitor of AMP-activated protein kinase (AMPK), with a Ki of 109 nM. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6. Dorsomorphin dihydrochloride induces autophagy. |
| OTSSP167
OTSSP167 is a highly potent MELK (maternal embryonic leucine zipper kinase) inhibitor with IC50 of 0.41 nM. |
| WZ4003
WZ4003 is a highly specific NUAK kinase inhibitor with IC50 of 20 nM and 100 nM for NUAK1 and NUAK2, respectively, without significant inhibition on 139 other kinases. |
| Geniposide
Geniposide is an iridoid glycoside isolated from the fruit of Gardenia jasminoides Ellis. |
| Metformin
Metformin (1, 1-dimethylbiguanide) inhibits mitochondrial respiratory chains in the liver, leads to AMPK activation and enhances insulin sensitivity, and can be used in type 2 diabetes research. Metformin can cross the blood-brain barrier and induce autophagy, and Metformin is a CD47 inhibitor in vitro. |
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