2. Metabolic Enzyme/Protease PI3K/Akt/mTOR Epigenetics Apoptosis Autophagy
  3. Mitochondrial Metabolism AMPK Apoptosis Autophagy mTOR
  4. Phenformin

Phenformin  (Synonyms: Phenethylbiguanide)

Cat. No.: HY-16397 Purity: 98.02%
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Phenformin (Phenethylbiguanide) is an orally active biguanide hypoglycemic agent. Phenformin inhibits mitochondrial respiratory chain complex I, leading to an increased AMP/ATP ratio, activation of AMPK, and subsequent inhibition of the mTOR pathway, thereby suppressing cell proliferation, inducing apoptosis and autophagy. Phenformin inhibits cancer stem cells (CSCs) and possesses potent antitumor potential.

For research use only. We do not sell to patients.

CAS No. : 114-86-3

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10 mM * 1 mL in Water
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Based on 10 publication(s) in Google Scholar

Other Forms of Phenformin:

Phenformin Related Antibodies

Top Publications Citing Use of Products

    Phenformin purchased from MedChemExpress. Usage Cited in: NPJ Precis Oncol. 2026 Mar 6;10(1):156.

    Dose-response curves showing the effect of phenformin (4-10 mM; 48 h) on cell viability in MG63 cells with high (sh-NC) and low PDHA1 expression (sh-PDHA1).

    Phenformin purchased from MedChemExpress. Usage Cited in: Pharmaceuticals (Basel). 2024 Sep 19;17(9):1234.  [Abstract]

    Representative recordings illustrating the NMDA receptors inhibition by Phenformin hydrochloride (Phen) (3-30 μM).

    Phenformin purchased from MedChemExpress. Usage Cited in: Mol Syst Biol. 2023 Jul 11;19(7):e11267.  [Abstract]

    Phenformin hydrochloride (1-20 μM) increased cell survival of U2-OS cells treated with etoposide.

    Phenformin purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2022 Nov 15;3(11):100802.  [Abstract]

    Phenformin hydrochloride (370 µM) strongly potentiated the induction of apoptosis of 298B cells in response to CR.

    Phenformin purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Jul 1;10(1):2901.   [Abstract]

    Phenformin hydrochloride (Phen) (100 µM; 24 h) markedly reduced Ezh2 and Suz12 protein expression in NIC cells.

    View All AMPK Isoform Specific Products:

    View All Isoforms
    NUAK1 NUAK2 AMPK AMPK α1β1γ1 AMPK α2β1γ1 AMPK α1β2γ1 AMPK α2β2γ1 BRSK1 BRSK2 HUNK AMPKα

    View All mTOR Isoform Specific Products:

    View All Isoforms
    mTOR mTORC1 mTORC2

    • Biological Activity

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    Description

    Phenformin (Phenethylbiguanide) is an orally active biguanide hypoglycemic agent. Phenformin inhibits mitochondrial respiratory chain complex I, leading to an increased AMP/ATP ratio, activation of AMPK, and subsequent inhibition of the mTOR pathway, thereby suppressing cell proliferation, inducing apoptosis and autophagy. Phenformin inhibits cancer stem cells (CSCs) and possesses potent antitumor potential[1][2][3][4].

    Cellular Effect
    Cell Line Type Value Description References
    Oocyte IC50
    10 μM
    Compound: Phenformin
    TP_TRANSPORTER: inhibition of Cimetidine uptake (Cimetidine: 1 uM) in Xenopus laevis oocytes
    TP_TRANSPORTER: inhibition of Cimetidine uptake (Cimetidine: 1 uM) in Xenopus laevis oocytes
    		[PMID: 12240953]
    Oocyte IC50
    65 μM
    Compound: Phenformin
    TP_TRANSPORTER: inhibition of Cimetidine uptake (Cimetidine: 1 uM) in Xenopus laevis oocytes
    TP_TRANSPORTER: inhibition of Cimetidine uptake (Cimetidine: 1 uM) in Xenopus laevis oocytes
    		[PMID: 12240953]
    UMUC3 IC50
    0.25 mM
    Compound: 12
    Antiproliferative activity in human UMUC3 cells assessed as cell growth inhibition
    Antiproliferative activity in human UMUC3 cells assessed as cell growth inhibition
    		[PMID: 36205714]
    In Vitro

    Phenformin induces G0/G1 cell cycle arrest, reduces the proportion of S phase in a dose-dependent manner, inhibits CDK4 and D glycine, and activates p21 protein in SKOV3, IGROV-1 and Hey ovarian cancer cell lines[1].
    Phenformin acts synergistically with SCH772984 (HY-50846) to inhibit proliferation, induce apoptosis, and completely suppress the mTOR signaling pathway in NF1-mutant melanoma cells[1].
    Combination treatment with Phenformin and Temozolomide (HY-17364) exerts a synergistic effect on the death of glioblastoma stem cells, thereby enhancing the anti-tumor activity of Phenformin and reducing its required administration concentration[1].
    Phenformin (0.5-5 mM; 24-72 h) reduces the viability and promotes apoptosis of SET2 JAK2V617F cells, with corresponding IC50 values of 2 mM, 1.79 mM and 0.79 mM at 24 h, 48 h and 72 h, respectively[2].
    Phenformin (2 mM; 12-48 h) inhibits the proliferation of human cholangiocarcinoma cell lines RBE and Huh28 in a time-dependent manner, with significant effects observed at 12, 24 and 48 h[3].
    Phenformin (2 mM; 10 days) inhibits the colony-forming ability of human cholangiocarcinoma cell lines RBE and Huh28[3].
    Phenformin (2 mM; 24 h) induces apoptosis in human cholangiocarcinoma cell lines RBE and Huh28 after 24 h of treatment[3].
    Phenformin (2 mM; 24 h) upregulates the mRNA expression of autophagy-related genes (BECN1, ATG5, ATG7) in human cholangiocarcinoma cell lines RBE and Huh28 after 24 hours of treatment[3].
    Phenformin (2 mM; 12-48 h) exerts a significantly stronger inhibitory effect on the viability of LKB1-knockdown RBE and Huh28 human cholangiocarcinoma cell lines than on cells transfected with negative control siRNA at 12, 24, and 48 h[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Phenformin Related Antibodies

    Cell Viability Assay[3]

    Cell Line: RBE, Huh28 human cholangiocarcinoma (CCA) cell lines
    Concentration: 2 mM
    Incubation Time: 12 h, 24 h, 48 h
    Result: Significantly inhibited proliferation of RBE and Huh28 cells compared to 0 mM controls at 12, 24, and 48 hours, with increasing inhibition over time.

    Apoptosis Analysis[3]

    Cell Line: RBE, Huh28 human cholangiocarcinoma (CCA) cell lines
    Concentration: 2 mM
    Incubation Time: 24 h
    Result: Significantly increased the apoptosis rate of RBE and Huh28 cells compared to 0 mM controls.

    Real Time qPCR[3]

    Cell Line: RBE, Huh28 human cholangiocarcinoma (CCA) cell lines
    Concentration: 2 mM
    Incubation Time: 24 h
    Result: Significantly elevated the mRNA expression levels of BECN1, ATG5, and ATG7 in RBE and Huh28 cells compared to 0 mM controls.

    Cell Viability Assay[3]

    Cell Line: LKB1-knockdown RBE, Huh28 human cholangiocarcinoma (CCA) cell lines
    Concentration: 2 mM
    Incubation Time: 12 h, 24 h, 48 h
    Result: Further reduced the viability of RBE and Huh28 cells treated with phenformin compared to negative control siRNA-transfected cells.
    In Vivo

    Phenformin (40 mg/kg; i.p.; daily; 45 days) increases the percentages of LSK, myeloid progenitor, and multipotent progenitor populations but does not reduce disease burden in Jak2V617F-knockin MPN mice[2].
    Phenformin (2 mM; intratumoral; every 4 days; 30 days) significantly inhibits RBE tumor volume in a subcutaneous cholangiocarcinoma xenograft mouse model[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: C57BL/6 Pepboy (female, lethally irradiated, transplanted with bone marrow cells from conditional vavCre knockin Jak2V617F mice)[2]
    Dosage: 40 mg/kg
    Administration: i.p.; daily; 45 days
    Result: Increased frequencies of LSK (Lin⁻Sca-1⁺c-Kit⁺), myeloid progenitors (Lin⁻Sca-1⁺c-Kitʰⁱᵍʰ), and multipotent progenitors (MPP: Lin⁻Sca-1⁺c-Kit⁺CD150⁻CD48⁺) in the bone marrow; showed no effects on peripheral blood counts, spleen weight, megakaryocyte count, erythroid precursors frequency, or ex vivo clonogenic capacity.
    Animal Model: BALB/c (nu/nu) (male, 5 weeks old, mean weight 15 g, subcutaneous RBE cell xenograft)[3]
    Dosage: 2 mM
    Administration: intratumoral; every 4 days; 30 days
    Result: Exhibited significantly smaller RBE tumor volume compared with the control group after 28 days.
    Molecular Weight

    205.26

    Formula

    C10H15N5
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    NC(NC(NCCC1=CC=CC=C1)=N)=N
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    RT, protect from light

    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    H2O : 350 mg/mL (1705.15 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 4.8719 mL 24.3594 mL 48.7187 mL
    5 mM 0.9744 mL 4.8719 mL 9.7437 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    Purity & Documentation
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O 1 mM 4.8719 mL 24.3593 mL 48.7187 mL 121.7967 mL
    5 mM 0.9744 mL 4.8719 mL 9.7437 mL 24.3593 mL
    10 mM 0.4872 mL 2.4359 mL 4.8719 mL 12.1797 mL
    15 mM 0.3248 mL 1.6240 mL 3.2479 mL 8.1198 mL
    20 mM 0.2436 mL 1.2180 mL 2.4359 mL 6.0898 mL
    25 mM 0.1949 mL 0.9744 mL 1.9487 mL 4.8719 mL
    30 mM 0.1624 mL 0.8120 mL 1.6240 mL 4.0599 mL
    40 mM 0.1218 mL 0.6090 mL 1.2180 mL 3.0449 mL
    50 mM 0.0974 mL 0.4872 mL 0.9744 mL 2.4359 mL
    60 mM 0.0812 mL 0.4060 mL 0.8120 mL 2.0299 mL
    80 mM 0.0609 mL 0.3045 mL 0.6090 mL 1.5225 mL
    100 mM 0.0487 mL 0.2436 mL 0.4872 mL 1.2180 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Phenformin Related Classifications

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Phenformin114-86-3PhenethylbiguanideMitochondrial MetabolismAMPKApoptosisAutophagymTORAMP-activated protein kinaseMammalian target of Rapamycinglioblastoma stem cellsSKOV3 cellsmitochondrial respiratory chain complex IHey ovarian cancer cell linesapoptosismTOR regulatory complexIGROV-1 cellsautophagytype 2 diabetes mellitusInhibitorinhibitorinhibit

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