Phenformin (NSC-756501) HCl

Catalog No.S2542 Synonyms: Phenethylbiguanide HCl

For research use only.

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.

Phenformin (NSC-756501) HCl Chemical Structure

CAS No. 834-28-6

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

2 Customer Reviews

Purity & Quality Control

Choose Selective AMPK Inhibitors

Other AMPK Products

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 NIn0T2tHfW6ldHnvckBie3OjeR?= MmT4WHBgXFKDTmPQU3JVTVJ8IIXweIFs\SCrbjDPR3QyNWW6cILld5NqdmdiQ1jPJINmdGy|LDDLcV0yPS54zszN M1TyVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{MUOwO|A6Lz5zMkGzNFcxQTxxYU6=
DAOY Mn62dWhVWyCjc4PhfS=> NE\6bJVyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiRFHPXUBk\Wyucx?= MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
A673 NH7SUpRyUFSVIHHzd4F6 Mm\EdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEF4N{OgZ4VtdHN? MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
BT-12 NF7M[lVyUFSVIHHzd4F6 NFnqXllyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStNVIh[2WubIO= MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
OHS-50 Mn7JdWhVWyCjc4PhfS=> M2X4e5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCRSGOtOVAh[2WubIO= NGqybnU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
HCT116 M{Sz[2Z2dmO2aX;uJIF{e2G7 MmLkNE42KG2P NVPFe5lIOjRiaILz Ml;ISYZn\WO2IH;uJI1qfG:laH;u[JJq[WxicnXzdIlz[XSrb36gbY4hcHWvYX6gTGNVOTF4IHPlcIx{KGW6cILld5NqdmdiY3HyZo9vcWNiYX7ofYRz[XOnIEmgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIH;4fYdmdiClb37zeY1xfGmxbjDyZZRmKGG2IECuOUBuVSCjZoTldkAzPCCqcoOgeY5l\XJiaInwc5hq[yClb37kbZRqd25iYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ MmLnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd6MkO4O|koRjJ5OEKzPFc6RC:jPh?=
Assay
Methods Test Index 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 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 (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 241.72
Formula

C10H15N5.HCl

CAS No. 834-28-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC=C(C=C1)CCN=C(N)N=C(N)N.Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Phenformin (NSC-756501) HCl | Phenformin (NSC-756501) HCl ic50 | Phenformin (NSC-756501) HCl price | Phenformin (NSC-756501) HCl cost | Phenformin (NSC-756501) HCl solubility dmso | Phenformin (NSC-756501) HCl purchase | Phenformin (NSC-756501) HCl manufacturer | Phenformin (NSC-756501) HCl research buy | Phenformin (NSC-756501) HCl order | Phenformin (NSC-756501) HCl mouse | Phenformin (NSC-756501) HCl chemical structure | Phenformin (NSC-756501) HCl mw | Phenformin (NSC-756501) HCl molecular weight | Phenformin (NSC-756501) HCl datasheet | Phenformin (NSC-756501) HCl supplier | Phenformin (NSC-756501) HCl in vitro | Phenformin (NSC-756501) HCl cell line | Phenformin (NSC-756501) HCl concentration | Phenformin (NSC-756501) HCl nmr