Home PI3K/Akt/mTOR AMPK activator Phenformin HCl For research use only.

Phenformin HCl

Synonyms: NSC-756501, Phenethylbiguanide

Phenformin HCl is a hydrochloride salt of phenformin that is an anti-diabetic drug from the biguanide class. It activates AMPK, increasing activity and phosphorylation.

Phenformin HCl Chemical Structure

Phenformin HCl Chemical Structure

CAS No. 834-28-6

Purity & Quality Control

Phenformin HCl Related Products

Signaling Pathway

AMPK Signaling Pathways

AMPK Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHO Function assay TP_TRANSPORTER: uptake in OCT1-expressing CHO cells, Km=15.6μM 12130709
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
HCT116 Function assay 0.5 mM 24 hrs Effect on mitochondrial respiration in human HCT116 cells expressing carbonic anhydrase 9 assessed as reduction in oxygen consumption rate at 0.5 mM after 24 hrs under hypoxic condition by Western blot analysis 27823879
Click to View More Cell Line Experimental Data

Biological Activity

Description Phenformin HCl is a hydrochloride salt of phenformin that is an anti-diabetic drug from the biguanide class. It activates AMPK, increasing activity and phosphorylation.
Targets
AMPK [1]
(Cell-free assay)
In vitro
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 1,1-Dimethylbiguanide. 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 MK-870-sensitive transepithelial Na+ transport compared with controls. Phenformin and AICAR suppress MK-870-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]
Experimental Result Images Methods Biomarkers Images PMID
Western blot E-cadherin / Vimentin / Snail / Slug / Twist1 p-ErbB2 / ErbB2 / p-AKT / AKT / p-mTOR / mTOR / p-ERK / ERK p-AMPKα / AMPK IRβ / p-IRS1 / IRS1 / p-IGF1Rβ / IGF1R 28947975
Immunofluorescence E-cadherin / Vimentin 28947975
Growth inhibition assay Cell viability 29245964
In Vivo
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]

Chemical Information & Solubility

Molecular Weight 241.72 Formula

C10H15N5.HCl
CAS No. 834-28-6 SDF Download Phenformin HCl SDF
Smiles C1=CC=C(C=C1)CCN=C(N)N=C(N)N.Cl
Storage (From the date of receipt)

In vitro
Batch:

Water : 48 mg/mL

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : Insoluble


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In vivo
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