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: 834-28-6

Selleck's Phenformin HCl has been cited by 9 Publications

2 Customer Reviews

Purity & Quality Control

Batch: Purity: 99.86%
99.86

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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
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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 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]
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 lnformation & 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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