| Name | Phenformin |
| Description | Phenformin (BRN 1977317) is a biguanide compound with anticancer and anti-glycemic activity, inhibits skin tumor growth and promotes keratinocyte differentiation and apoptosis. |
| In vitro | Phenformin acts by promoting phosphorylation and activation of AMPKalpha1 and AMPKalpha2 without altering the activity of the LKB1 gene [1]. In isolated hearts, Phenformin increased AMPK activity and phosphorylation levels, which correlated with increased AMPK activity and increased intracellular [AMP] [2].Phenformin was 50 times more potent than Metformin and was able to inhibit mitochondrial complex I. In LKB1-deficient non-small cell lung cancer cell lines, the Phenformin was able to induce apoptosis.Phenformin (2 mM) also induced AMPK signaling and increased levels of P-AMPK and P-Raptor.Phenformin induced higher levels of cellular stress, which in turn triggered the induction of P-Ser51 eIF2α and its downstream target CHOP, which are late stage molecular markers of apoptosis. In chronically treated KLluc mice, Phenformin induced survival and treatment response [3]. In H441 cells, Phenformin and AICAR increased AMPK activity in a dose-dependent manner, maximizing activation of the kinase at 5-10 mM and 2 mM concentrations. In H441 cell monolayers, Phenformin significantly reduced basal ion migration (measured as short-circuit current) by approximately 50%. Phenformin and AICAR significantly reduced amiloride-sensitive transmembrane Na ion transport compared to controls. Phenformin and AICAR inhibited amiloride-sensitive transmembrane Na ion transport in H441 cells by activating AMPK and inducing inhibition of sodium ion entry at the terminal and basolateral sides of ENaC cells via the Na+, K+ ATPase [4]. In rats treated with Phenformin, their blood insulin levels tend to decrease (radioimmunoassay) [5]. |
| Storage | keep away from direct sunlight,store at low temperature,keep away from moisture,store under nitrogen | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : Soluble
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| Keywords | Phenformin | BRN-1977317 | BRN1977317 | Apoptosis |
| Inhibitors Related | Stavudine | Aceglutamide | Urea | Tamoxifen | Cysteamine hydrochloride | Metronidazole | Citric Acid Triammonium | Formamide | Dimethyl phthalate | Alginic acid | Chitosan oligosaccharide | Sildenafil citrate |
| Related Compound Libraries | Apoptosis Compound Library | Bioactive Compound Library | ReFRAME Related Library | Epigenetics Compound Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library | AMPK-Targeted Compound Library |
United States
