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2-Ketoglutaric acid

Name: 2-Ketoglutaric acid
Brand: TargetMol
SKU: T5980
Price: 42 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T5980 Copy Product Info

Purity: 99.92%

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2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM) and exhibits antioxidant activity. As an intermediate in the Krebs cycle, 2-Ketoglutaric acid can generate ATP or GTP. 2-Ketoglutaric acid also serves as the primary carbon skeleton for nitrogen assimilation reactions.

Cas No. 328-50-7

Pack Size	Price	USA Stock	Global Stock	Quantity
1 g	$42	In Stock	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.92%

Appearance:Solid

Color:White

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COA LCMS HNMR

Product Introduction

2-Ketoglutaric acid AI Summary

2-Ketoglutaric acid exhibits diverse bioactivities, including significant enzyme inhibition and antiviral properties. It inhibits the Glutamate racemase enzyme, displaying a low Kcat value of 0.18 s-1 and a strong binding affinity indicated by a Kcat/KM ratio of 3200.0 M-1 s-1. Additionally, it binds to the human PHD2 enzyme with varying Kd values (900.0 to 2200.0 nM) and affects collagen and HIF prolyl hydroxylation involved in hypoxia response. The compound also demonstrates inhibition of ERK signaling and androgen receptor signaling pathways, alongside growth inhibition in various tumor cell lines with GI50 values around 100000.0 nM. In antiviral assays, it shows activity against SARS-CoV-2 induced cytotoxicity in both Caco-2 and VERO-6 cells. Furthermore, 2-Ketoglutaric acid acts as an agonist at PSGR/OR51E2, inhibits uptake processes in various transporter assays, and affects enzymes like KDM5B and HDAC6. It has a Km of 57000.0 nM for Glutamate racemase and exhibits a notable half-life greater than 12.0 hours in TR-FRET assays for PHD2 inhibition..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM) and exhibits antioxidant activity. As an intermediate in the Krebs cycle, 2-Ketoglutaric acid can generate ATP or GTP. 2-Ketoglutaric acid also serves as the primary carbon skeleton for nitrogen assimilation reactions.
Targets & IC50	Tyrosinase:15 mM, HEK293 cells:54 μM (EC50)
In vitro	Methods: Human primary chondrocytes were treated with IL-1β (10 ng/mL) or 2-Ketoglutaric acid (2 mM) or both agents for 24 hours. Cell proliferation was assessed via EdU staining and counted under fluorescence microscopy. Results: IL-1β inhibited cell proliferation, while 2-Ketoglutaric acid significantly reversed this effect. [1] Methods: ESC-1 cells (S/L) were treated with DM-2-Ketoglutaric acid (4 mM). After three passages, global DNA methylation was assessed by ELISA. Results: DM-2-Ketoglutaric acid treatment reduced overall DNA methylation levels. [2] Methods: Neonatal SD rat ventricular myocytes (NRVMs) were co-treated with LPS (0.5 μg/mL) and 2-Ketoglutaric acid (2 mM) for 24 hours. Apoptosis was assessed by TUNEL staining, and Bcl-2 expression was measured by Western Blot. Results: The LPS group exhibited a 7-fold increase in TUNEL-positive cells and significantly reduced Bcl-2 protein levels; 2-Ketoglutaric acid significantly reversed these changes. [3]
In vivo	Methods: To investigate the therapeutic effects of 2-Ketoglutaric acid on osteoarthritis, an osteoarthritis model was established in 8-week-old female Wistar rats via anterior cruciate ligament transection (ACLT) surgery. One week post-surgery, treatment groups received 2-Ketoglutaric acid in drinking water (2% concentration) while the control group received standard drinking water. Treatment lasted for 8 weeks. Results: The surgical group exhibited mitochondrial swelling, vacuolation, and structural disruption, whereas the surgical group treated with 2-Ketoglutaric acid showed normal mitochondrial morphology. PINK1/Parkin expression decreased in the ACLT group; 2-Ketoglutaric acid significantly upregulated its expression. [1] Methods: To investigate the ameliorative effects of 2-Ketoglutaric acid on septic cardiomyopathy, 8-week-old male C57BL/6 mice were intraperitoneally injected with LPS (10 mg/kg) to establish a septic cardiomyopathy model. Prior to LPS injection, mice received 9 weeks of free-drinking water treatment (2-Ketoglutaric acid: 2% drinking water). Ultrasound examinations were performed post-LPS injection. Results: The LPS group exhibited a 33% decrease in LVEF and a 32% decrease in LVFS, along with a 40% increase in LVEDD and a 60% increase in LVESD. 2-Ketoglutaric acid significantly improved these parameters. [3]

Chemical Properties

Molecular Weight	146.10
Formula	C₅H₆O₅
Cas No.	328-50-7
Smiles	OC(=O)CCC(=O)C(O)=O
Relative Density.	1.2821 g/cm3 (Estimated)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 480.00 mg/mL (3285.42 mM), Sonication is recommended.

H2O: 100 mg/mL (684.46 mM), Sonication is recommended.

In Vivo Formulation

PBS: 100.00 mg/mL (684.46 mM)

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5.00 mg/mL (34.22 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

H2O/DMSO

	1mg	5mg	10mg	50mg
1 mM	6.8446 mL	34.2231 mL	68.4463 mL	342.2313 mL
5 mM	1.3689 mL	6.8446 mL	13.6893 mL	68.4463 mL
10 mM	0.6845 mL	3.4223 mL	6.8446 mL	34.2231 mL
20 mM	0.3422 mL	1.7112 mL	3.4223 mL	17.1116 mL
50 mM	0.1369 mL	0.6845 mL	1.3689 mL	6.8446 mL
100 mM	0.0684 mL	0.3422 mL	0.6845 mL	3.4223 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Keywords

TyrosinaseTCAskeletonprecursorintermediateInhibitorinhibitHuman Endogenous MetaboliteEndogenousMetaboliteEndogenous MetabolitecarbonAlpha-Ketoglutaric acid2-Ketoglutaric acid2Ketoglutaric acid2 Ketoglutaric acid

Related Tags: 2-Ketoglutaric acid chemical structure | 2-Ketoglutaric acid in vivo | 2-Ketoglutaric acid in vitro | 2-Ketoglutaric acid formula | 2-Ketoglutaric acid molecular weight