α-Cyano-4-hydroxycinnamic acid
Based on 13 publication(s) in Google Scholar
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.
- Purity: 99.92%
- CAS No.: 28166-41-8
- Formula: C10H7NO3
- Molecular Weight:189.17
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) α-Cyano-4-hydroxycinnamic acid
More- Cell Host Microbe. 2026 Feb 11;34(2):245-262.e8. [Abstract]
- Autophagy. 2024 Apr;20(4):752-768. [Abstract]
- Neuron. 2026 Mar 16:S0896-6273(26)00137-6. [Abstract]
- Theranostics. 2024 Jul 8;14(11):4297-4317. [Abstract]
- Adv Sci (Weinh). 2026 Jan 9:e18180. [Abstract]
- Acta Biomater. 2025 Apr:196:399-409. [Abstract]
- Int J Biol Macromol. 2025 Oct 9;330(Pt 3):148223. [Abstract]
- Pharmaceutics. 2025 Nov 20;17(11):1503. [Abstract]
- CNS Neurosci Ther. 2026 Jan;32(1):e70753. [Abstract]
- Compr Physiol. 2026 Jun;16(3):e70184. [Abstract]
- Exp Neurol. 2026 Feb:396:115553. [Abstract]
- bioRxiv. 2026 Jun 18.
- SSRN. 2023 Jun 15.
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
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WB
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WB
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Cell Imaging/Staining
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | GI50 |
52.7 μM
Compound: 8; CHC
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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
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[PMID: 36584238] |
| HCT-116 | IC50 |
1650 μM
Compound: CHC
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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
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[PMID: 33221062] |
| HeLa | IC50 |
2140 μM
Compound: CHC
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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
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[PMID: 33221062] |
| HT-29 | EC50 |
9.8 μM
Compound: CHCA
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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
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[PMID: 24900447] |
| HT-29 | IC50 |
30.4 μM
Compound: CHCA
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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
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[PMID: 24900447] |
| MCF7 | GI50 |
108 μM
Compound: 8; CHC
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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
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[PMID: 36584238] |
| Oocyte | IC50 |
991 μM
Compound: alpha-Cyano-4-hydroxycinnamate
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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
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[PMID: 11101640] |
| SiHa | EC50 |
10.7 μM
Compound: CHC
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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
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[PMID: 24095010] |
| SiHa | IC50 |
10.7 μM
Compound: CHC
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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
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[PMID: 24095010] |
| SiHa | IC50 |
43.5 μM
Compound: CHC
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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
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[PMID: 24095010] |
| U2OS | EC50 |
70.7 μM
Compound: CHCA
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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
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[PMID: 24900447] |
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.
Chemical Information
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CAS No. 28166-41-8
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Appearance Solid
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Molecular Weight 189.17
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Formula C10H7NO3
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Color Light yellow to yellow
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SMILES
O=C(O)/C(C#N)=C/C1=CC=C(O)C=C1
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Synonyms
α-Cyano-4-hydroxycinnamate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (13)
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Journal Impact Factor
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Most Recent
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Cell Host Microbe
Enterococcus faecalis-derived lactic acid suppresses macrophage activation to facilitate persistent and polymicrobial wound infections. [Abstract]2026 Feb 11;34(2):245-262.e8. PMID: 41605216
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.
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Autophagy
2024 Apr;20(4):752-768. PMID: 37798944
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.
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Neuron
Oligodendrocyte-encoded lactate dehydrogenase A couples glycolysis to remyelination via protein lactylation. [Abstract]2026 Mar 16:S0896-6273(26)00137-6. PMID: 41844160 -
Theranostics
Astrocyte-derived lactate aggravates brain injury of ischemic stroke in mice by promoting the formation of protein lactylation. [Abstract]2024 Jul 8;14(11):4297-4317. PMID: 39113798
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.
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Adv Sci (Weinh)
Hepatocyte BPGM Induces RET Lactylation and Macrophage Reprogramming to Promote Tumorigenesis in Hepatocellular Carcinoma. [Abstract]2026 Jan 9:e18180. PMID: 41514495 -
Acta Biomater
Oral delivery of ultra-small zwitterionic nanoparticles to overcome mucus and epithelial barriers for macrophage modulation and colitis therapy. [Abstract]2025 Apr:196:399-409. PMID: 39983856 -
Int J Biol Macromol
The role of solute carrier family 16 member 3 protein in hepatocellular carcinoma and sorafenib resistance. [Abstract]2025 Oct 9;330(Pt 3):148223. PMID: 41075888 -
Pharmaceutics
Functional pH-Responsive Nanoparticles for Immune Reprogramming in MSS Colorectal Cancer via ER Stress-Induced Proteostasis Disruption, PD-L1-Targeting miRNA, and TLR7 Activation. [Abstract]2025 Nov 20;17(11):1503. PMID: 41304839 -
CNS Neurosci Ther
Tregs Promote Astrocyte-Neuron Lactate Shuttle via Inhibiting STING Pathway to Improve Neurological Recovery After Ischemic Stroke. [Abstract]2026 Jan;32(1):e70753. PMID: 41552852 -
Compr Physiol
SLC16A9-Mediated Carnitine Uptake Enhances Radiotherapy Resistance in Colorectal Cancer via Lipid Metabolic Reprogramming. [Abstract]2026 Jun;16(3):e70184. PMID: 42271166 -
Exp Neurol
2026 Feb:396:115553. PMID: 41238154 -
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Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. A P Halestrap, et al. The mitochondrial pyruvate carrier. Kinetics and specificity for substrates and inhibitors. Biochem J. 1975 Apr; 148(1): 85-96. [Content Brief]
[2]. Sara Granja, et al. The Monocarboxylate Transporter Inhibitor α-cyano-4-hydroxycinnamic Acid Disrupts Rat Lung Branching. Cell Physiol Biochem. 2013;32(6):1845-56. [Content Brief]
[3]. Makoto Watanabe, et al. Improvement of Mass Spectrometry Analysis of Glycoproteins by MALDI-MS Using 3-aminoquinoline/α-cyano-4-hydroxycinnamic Acid. Anal Bioanal Chem. 2013 May;405(12):4289-93. [Content Brief]
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 |