1. Membrane Transporter/Ion Channel
  2. Monocarboxylate Transporter
  3. α-Cyano-4-hydroxycinnamic acid

α-Cyano-4-hydroxycinnamic acid  (Synonyms: α-Cyano-4-hydroxycinnamate)

Cat. No.: HY-107641 Purity: 99.92%
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α-Cyano-4-hydroxycinnamic acid (α-Cyano-4-hydroxycinnamate) is a potent and non-competitive inhibitor of monocarboxylate transporters (MCTs). α-Cyano-4-hydroxycinnamic acid inhibits mitochondrial pyruvate transporter with a Ki of 6.3 μM. α-Cyano-4-hydroxycinnamic acid is used as a matrix to facilitate peptide ionization in matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) mass spectrometry applications.

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

CAS No. : 28166-41-8

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Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of α-Cyano-4-hydroxycinnamic acid:

Top Publications Citing Use of Products

    α-Cyano-4-hydroxycinnamic acid purchased from MedChemExpress. Usage Cited in: Cell Host Microbe. 2026 Feb 11;34(2):245-262.e8.  [Abstract]

    RAW 264.7 macrophages were infected with the WT E. faecalis and incubated in cell culture media in the presence or absence of α-Cyano-4-hydroxycinnamic acid (CHC; 5 mM) for 6 h prior to measurement of NF-kB-driven SEAP reporter activity.

    α-Cyano-4-hydroxycinnamic acid purchased from MedChemExpress. Usage Cited in: Theranostics. 2024 Jul 8;14(11):4297-4317.  [Abstract]

    α-cyano-4-hydroxycinnamate (4-CIN; 36 mM; 3.6 μL; ICV) showed little influence on lactate production in C57BL/6 male mice. Lactate levels in the ischemic brain at 6 h after cerebral ischemia were measured.

    α-Cyano-4-hydroxycinnamic acid purchased from MedChemExpress. Usage Cited in: Theranostics. 2024 Jul 8;14(11):4297-4317.  [Abstract]

    α-cyano-4-hydroxycinnamate (4-CIN; 36 mM; 3.6 μL; ICV) markedly reduce the protein lactylation levels of ischemic brain tissues at 6 h after cerebral ischemia in C57BL/6 male mice.

    α-Cyano-4-hydroxycinnamic acid purchased from MedChemExpress. Usage Cited in: Autophagy. 2024 Apr;20(4):752-768.  [Abstract]

    Preincubation of RTH-149 cells with 100 µM α-Cyano-4-hydroxycinnamic acid (CHC) blocked the HG-induced accumulation of oxidized proteins.

    α-Cyano-4-hydroxycinnamic acid purchased from MedChemExpress. Usage Cited in: Autophagy. 2024 Apr;20(4):752-768.  [Abstract]

    α-Cyano-4-hydroxycinnamic acid (CHC) prevented the formation of KFERQ-PA-mCherry1 puncta after 16 h exposure to high-glucose.

    View All Monocarboxylate Transporter Isoform Specific Products:

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    α-Cyano-4-hydroxycinnamic acid (α-Cyano-4-hydroxycinnamate) is a potent and non-competitive inhibitor of monocarboxylate transporters (MCTs). α-Cyano-4-hydroxycinnamic acid inhibits mitochondrial pyruvate transporter with a Ki of 6.3 μM. α-Cyano-4-hydroxycinnamic acid is used as a matrix to facilitate peptide ionization in matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) mass spectrometry applications[1][2].

    Cellular Effect
    Cell Line Type Value Description References
    A-431 IC50
    2 x 102 μM
    Compound: 116
    Inhibition of EGFR in human A431 cells
    Inhibition of EGFR in human A431 cells
    [PMID: 1479375]
    A549 GI50
    52.7 μM
    Compound: 8; CHC
    Antiproliferative activity against human A549 cells expressing MCT1 assessed as growth inhibition incubated for 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells expressing MCT1 assessed as growth inhibition incubated for 72 hrs by MTT assay
    [PMID: 36584238]
    HCT-116 IC50
    1650 μM
    Compound: CHC
    Cytotoxicity against human HCT-116 cells overexpressing MCT-1 assessed as reduction in cell viability measured after 72 hrs by MTT assay
    Cytotoxicity against human HCT-116 cells overexpressing MCT-1 assessed as reduction in cell viability measured after 72 hrs by MTT assay
    [PMID: 33221062]
    HT-29 EC50
    9.8 μM
    Compound: CHCA
    Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay
    Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay
    [PMID: 24900447]
    HT-29 IC50
    30.4 μM
    Compound: CHCA
    Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins
    Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins
    [PMID: 24900447]
    HeLa IC50
    2140 μM
    Compound: CHC
    Cytotoxicity against human HeLa cells overexpressing MCT-1 assessed as reduction in cell viability measured after 72 hrs by MTT assay
    Cytotoxicity against human HeLa cells overexpressing MCT-1 assessed as reduction in cell viability measured after 72 hrs by MTT assay
    [PMID: 33221062]
    MCF7 GI50
    108 μM
    Compound: 8; CHC
    Antiproliferative activity against human MCF7 cells expressing MCT1 assessed as growth inhibition incubated for 72 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells expressing MCT1 assessed as growth inhibition incubated for 72 hrs by MTT assay
    [PMID: 36584238]
    Oocyte IC50
    24 μM
    Compound: 4-CIN
    TP_TRANSPORTER: inhibition of lactate uptake in Xenopus laevis oocytes
    TP_TRANSPORTER: inhibition of lactate uptake in Xenopus laevis oocytes
    [PMID: 10417314]
    Oocyte IC50
    425 μM
    Compound: 4-CIN
    TP_TRANSPORTER: inhibition of lactate uptake in Xenopus laevis oocytes
    TP_TRANSPORTER: inhibition of lactate uptake in Xenopus laevis oocytes
    [PMID: 10417314]
    Oocyte IC50
    991 μM
    Compound: alpha-Cyano-4-hydroxycinnamate
    TP_TRANSPORTER: inhibition of L-Lactate uptake (L-Lactate:30mM) in Xenopus laevis oocytes
    TP_TRANSPORTER: inhibition of L-Lactate uptake (L-Lactate:30mM) in Xenopus laevis oocytes
    [PMID: 11101640]
    SiHa EC50
    10.7 μM
    Compound: CHC
    Cytotoxicity against human SiHa cells in lactate-containing medium after 72 hrs by MTT assay
    Cytotoxicity against human SiHa cells in lactate-containing medium after 72 hrs by MTT assay
    [PMID: 24095010]
    SiHa IC50
    10.7 μM
    Compound: CHC
    Inhibition of MCT4-mediated [14C]-lactate uptake in human SiHa cells in lactate-containing medium assessed as remaining lactate concentration in culture medium after 12 mins by liquid scintillation counting
    Inhibition of MCT4-mediated [14C]-lactate uptake in human SiHa cells in lactate-containing medium assessed as remaining lactate concentration in culture medium after 12 mins by liquid scintillation counting
    [PMID: 24095010]
    SiHa IC50
    43.5 μM
    Compound: CHC
    Inhibition of MCT4-mediated [14C]-lactate uptake in human SiHa cells in lactate-containing medium assessed as remaining lactate concentration in culture medium after 24 hrs by liquid scintillation counting
    Inhibition of MCT4-mediated [14C]-lactate uptake in human SiHa cells in lactate-containing medium assessed as remaining lactate concentration in culture medium after 24 hrs by liquid scintillation counting
    [PMID: 24095010]
    U2OS EC50
    70.7 μM
    Compound: CHCA
    Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay
    Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay
    [PMID: 24900447]
    In Vitro

    α-Cyano-4-hydroxycinnamic acid (α-Cyano-4-hydroxycinnamate) inhibits monocarboxylates transport such as lactate and pyruvate[2].
    α-Cyano-4-hydroxycinnamic acid (CHC; 0.5 mM and 1 mM) of 1 mM has a significant inhibitory effect on branching morphogenesis and decreases the epithelial perimeter and area of lung explants in a dose dependent way[2].
    At 100 μM concentration, α-Cyano-4-hydroxycinnamic acid rapidly and almost totally inhibits O2 uptake by rat heart mitochondria oxidizing pyruvate. Inhibition can be detected at concentrations of inhibitor as low as 1 μM although inhibition took time to develop at this concentration[1].

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

    Molecular Weight

    189.17

    Formula

    C10H7NO3

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(O)/C(C#N)=C/C1=CC=C(O)C=C1

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 200 mg/mL (1057.25 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 5.2863 mL 26.4313 mL 52.8625 mL
    5 mM 1.0573 mL 5.2863 mL 10.5725 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    C2

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (11.00 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (11.00 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    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).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.92%

    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 5.2863 mL 26.4313 mL 52.8625 mL 132.1563 mL
    5 mM 1.0573 mL 5.2863 mL 10.5725 mL 26.4313 mL
    10 mM 0.5286 mL 2.6431 mL 5.2863 mL 13.2156 mL
    15 mM 0.3524 mL 1.7621 mL 3.5242 mL 8.8104 mL
    20 mM 0.2643 mL 1.3216 mL 2.6431 mL 6.6078 mL
    25 mM 0.2115 mL 1.0573 mL 2.1145 mL 5.2863 mL
    30 mM 0.1762 mL 0.8810 mL 1.7621 mL 4.4052 mL
    40 mM 0.1322 mL 0.6608 mL 1.3216 mL 3.3039 mL
    50 mM 0.1057 mL 0.5286 mL 1.0573 mL 2.6431 mL
    60 mM 0.0881 mL 0.4405 mL 0.8810 mL 2.2026 mL
    80 mM 0.0661 mL 0.3304 mL 0.6608 mL 1.6520 mL
    100 mM 0.0529 mL 0.2643 mL 0.5286 mL 1.3216 mL
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      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.

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    Product Name:
    α-Cyano-4-hydroxycinnamic acid
    Cat. No.:
    HY-107641
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