Phenformin HCl

Catalog No.S2542

Phenformin HCl Chemical Structure

Molecular Weight(MW): 241.72

Phenformin HCl is a hydrochloride salt of phenformin that is an anti-diabetic drug from the biguanide class.

Size Price Stock Quantity  
In DMSO USD 130 In stock
USD 97 In stock

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description Phenformin HCl is a hydrochloride salt of phenformin that is an anti-diabetic drug from the biguanide class.
Targets
AMPK [1]
(Cell-free assay)
In vitro

Phenformin stimulates the phosphorylation and activation of AMPKalpha1 and AMPKalpha2 without altering LKB1 activity. [1] 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]. [2] 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 induces a significant increase in survival and therapeutic response in KLluc mice following long-term treatment. [3] 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. [4] Phenformin-treated rats reveals a tendency towards a decrease in blood insulin level (radioimmunoassay). [5]

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. [3]

Protocol

Solubility (25°C)

In vitro DMSO 48 mg/mL (198.57 mM)
Water 48 mg/mL (198.57 mM)
Ethanol 12 mg/mL (49.64 mM)
In vivo

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 241.72
Formula

C10H15N5.HCl

CAS No. 834-28-6
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03026517 Recruiting Melanoma Memorial Sloan Kettering Cancer Center|Massachusetts General Hospital|Weill Medical College of Cornell University January 2017 Phase 1

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AMPK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID