Phenformin (NSC-756501) HCl

For research use only.

Catalog No.S2542 Synonyms: Phenethylbiguanide HCl

6 publications

Phenformin (NSC-756501) HCl Chemical Structure

CAS No. 834-28-6

Phenformin HCl (NSC-756501, Phenethylbiguanide) is a hydrochloride salt of phenformin that is an anti-diabetic drug from the biguanide class. It activates AMPK, increasing activity and phosphorylation.

Selleck's Phenformin (NSC-756501) HCl has been cited by 6 publications

2 Customer Reviews

  • a set of RNAi-resistant rescue forms of Cdc37 plasmids were transfected into stable Cdc37-RNAi HCT116 cells. 24 h after transfection cells were treated with phenformin and then subjected to FLAG immunoprecipitation.

    J Biol Chem, 2017, 292(7):2830-2841. Phenformin (NSC-756501) HCl purchased from Selleck.

    Quantification of SIRT1 (K) and HIF-1α (L) in phenformin treated cells.

    Biochem Biophys Res Commun, 2016, 470(2):453-459. Phenformin (NSC-756501) HCl purchased from Selleck.

Purity & Quality Control

Choose Selective AMPK Inhibitors

Biological Activity

Description Phenformin HCl (NSC-756501, Phenethylbiguanide) 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

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHO M1LXR2Z2dmO2aX;uJIF{e2G7 NYm0e4dSXFChVGLBUnNRV1KWRWK6JJVxfGGtZTDpckBQS1RzLXX4dJJme3OrbnegR2hQKGOnbHzzMEBMdT1zNT62{txO MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjF|MEewPUc,OTJzM{C3NFk9N2F-
DAOY M1nYRZFJXFNiYYPzZZk> NHf2VmJyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiRFHPXUBk\Wyucx?= M4jReFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
A673 M37z[5FJXFNiYYPzZZk> MYfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>? MnTBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
BT-12 M132UZFJXFNiYYPzZZk> M2OxXZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2xNkBk\Wyucx?= MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
OHS-50 NXXjdWNmeUiWUzDhd5NigQ>? Mm\YdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE:KUz21NEBk\Wyucx?= NEXnT3A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
HCT116 M4XhPGZ2dmO2aX;uJIF{e2G7 M3i5e|AvPSCvTR?= NUDzd2dOOjRiaILz M3fJ[GVn\mWldDDvckBucXSxY3jvcoRzcWGuIILld5BqemG2aX;uJIlvKGi3bXHuJGhEXDFzNjDj[YxteyCneIDy[ZN{cW6pIHPhdoJwdmmlIHHubJllemG|ZTC5JIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDvfJlo\W5iY3;ud5VueHSrb36gdoF1\SCjdDCwMlUhdU1iYX\0[ZIhOjRiaILzJJVv\GW{IHj5dI95cWNiY3;u[Il1cW:wIHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? MkfiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd6MkO4O|koRjJ5OEKzPFc6RC:jPh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
E-cadherin / Vimentin / Snail / Slug / Twist1 ; 

PubMed: 28947975     


Western blot analysis of EMT markers in SKBR3 and 78617 cells treated with phenformin (0, 7.5, 25, 75, or 250 μM) for 72 hours is shown.

p-ErbB2 / ErbB2 / p-AKT / AKT / p-mTOR / mTOR / p-ERK / ERK ; 

PubMed: 28947975     


Western blot analysis of ErbB2 activation and signaling in SKBR3 and 78617 cells treated with phenformin (0, 7.5, 25, 75, or 250 μM) for 72 hours.

p-AMPKα / AMPK ; 

PubMed: 28947975     


Western blot analysis of AMPK activation in SKBR3 and 78617 cells treated with phenformin (0, 7.5, 25, 75, or 250 μM) for 72 hours.

IRβ / p-IRS1 / IRS1 / p-IGF1Rβ / IGF1R ; 

PubMed: 28947975     


Western blot analysis of IRS/IGF1R activation and signaling in SKBR3 and 78617 cells treated with phenformin (0, 7.5, 25, 75, or 250 μM) for 72 hours.

28947975
Immunofluorescence
E-cadherin / Vimentin ; 

PubMed: 28947975     


An immunofluorescence assay was used to determine EMT marker (E-cadherin and vimentin) expression in SKBR3 and 78617 cells treated with phenformin (0 or 75 μM) for 24 hours. Nuclei were stained with DAPI (blue), while E-cadherin and vimentin are indicated by Fluor 488 green fluorescence in the indicated panels. 

28947975
Growth inhibition assay
Cell viability; 

PubMed: 29245964     


The comparison of metformin and phenformin in inhibition of cell proliferation was assessed after 72 hours of treatment.

29245964
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

* 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 Phenethylbiguanide HCl
Smiles C1=CC=C(C=C1)CCN=C(N)N=C(N)N.Cl

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID