Reagenti e strumenti per immunologia, biologia cellulare e biologia molecolare

α-Cyano-4-hydroxycinnamic acid [28166-41-8]

Stampa

Cat# HY-107641-50mg

Size : 50mg

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Marca : MedChemExpress

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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 K_i 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
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]
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]
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]
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]
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	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	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.

Solvant et solubilité

In Vitro:

DMSO : 250 mg/mL (1321.56 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
10 mM	0.5286 mL	2.6431 mL	5.2863 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.

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (11.00 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Pureté et documentation

Purity: 99.98%

Fiche technique (274 KB) SDS (393 KB)

COA (246 KB) HNMR (271 KB) RP-HPLC (245 KB)

Instruction de manipulation (2659 KB)

Références

[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]

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α-Cyano-4-hydroxycinnamic acid [28166-41-8]

Cat# HY-107641-50mg

Contatta il distributore locale :

Marca : MedChemExpress

Contatta il distributore locale :

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