| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
L-2-Hydroxyglutaric acid disodium targets histone demethylases and mitochondrial creatine kinase (Mi-CK). As an epigenetic modifier， it inhibits histone demethylases, enzymes that remove methyl groups from histone proteins. This inhibition promotes histone methylation, which can alter gene expression patterns and contribute to oncogenesis. The compound also inhibits mitochondrial creatine kinase (Mi-CK), an enzyme involved in cellular energy metabolism, with Km and Ki values of 2.52 mM and 11.13 mM, respectively. L-2-Hydroxyglutaric acid is a putative oncometabolite in renal cancer and is involved in various biochemical pathways including energy production and amino acid metabolism.
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| ln Vitro |
Eleven-eleven translocation (TET) enzymes and other 2-oxoglutarate (2-OG)-dependent dioxygenases (2OGD) are efficiently inhibited by L-2-hydroxyglutarate [1].
In vitro, L-2-Hydroxyglutaric acid disodium inhibits histone demethylases, thereby promoting histone methylation. The compound also inhibits mitochondrial creatine kinase (Mi-CK) activity with Km and Ki values of 2.52 mM and 11.13 mM, respectively. As an epigenetic modifier， it alters gene expression patterns and can contribute to oncogenesis. The compound is a putative oncometabolite in renal cancer and is involved in various biochemical pathways including energy production and amino acid metabolism. Its in vitro activities are concentration-dependent, with efficacy observed at millimolar concentrations. L-2-Hydroxyglutaric acid disodium is used in renal cancer-related research. |
| ln Vivo |
In vivo, L-2-Hydroxyglutaric acid disodium is a putative oncometabolite in renal cancer and an epigenetic modifier. The compound inhibits histone demethylases and mitochondrial creatine kinase. As an oncometabolite, it accumulates in certain cancers and contributes to tumorigenesis through epigenetic alterations and metabolic dysregulation. The compound is involved in various biochemical pathways including energy production and amino acid metabolism. It is used in renal cancer-related research to study the role of oncometabolites in cancer development and progression. However, detailed in vivo pharmacokinetic and toxicological data require further investigation.
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| Enzyme Assay |
In vitro enzyme/receptor binding (non-cellular) assays for L-2-Hydroxyglutaric acid disodium involve measuring inhibition of histone demethylase and mitochondrial creatine kinase (Mi-CK) activities. For histone demethylase assays, purified enzyme is incubated with methylated histone substrates and varying concentrations of the compound. Demethylation is measured by detecting the release of formaldehyde or by using antibody-based detection of methylated histones. For Mi-CK assays, the enzyme is incubated with creatine, ATP, and varying concentrations of the compound. Enzyme activity is measured by detecting ATP production or by coupled enzyme assays. Km and Ki values of 2.52 mM and 11.13 mM, respectively, have been reported. These assays help characterize the compound's mechanism of action as an oncometabolite and epigenetic modifier.
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| Cell Assay |
In vitro cellular experiments with L-2-Hydroxyglutaric acid disodium are performed using renal cancer cell lines or other cell types to study its effects on histone methylation, gene expression, and cell proliferation. Cells are cultured in appropriate media (e.g., DMEM with 10% FBS) and treated with varying concentrations of L-2-Hydroxyglutaric acid disodium (typically 0.1-10 mM) for 24-72 hours. Histone methylation is assessed by Western blot analysis using methylation-specific antibodies. Gene expression changes are measured by RT-qPCR or RNA-seq. Cell viability and proliferation are assessed using MTT or CellTiter-Glo assays. Mitochondrial function may be assessed by measuring ATP levels or oxygen consumption rates. Cells are maintained at 37°C in 5% CO₂ with appropriate media supplements.
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| Animal Protocol |
In vivo animal studies with L-2-Hydroxyglutaric acid disodium are performed in renal cancer models to study the role of oncometabolites in tumorigenesis. Mice bearing renal cancer xenografts or genetically engineered mouse models of renal cancer may be used. Animals are treated with L-2-Hydroxyglutaric acid disodium via oral, intraperitoneal, or intravenous administration at various doses. Efficacy is assessed by measuring tumor growth, survival, and histopathological examination. Histone methylation and gene expression changes in tumor tissues are assessed by Western blot, immunohistochemistry, or RNA-seq. Mitochondrial function in tumor tissues may be assessed by measuring ATP levels or enzyme activities. Further studies are needed to establish in vivo efficacy and safety.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of L-2-Hydroxyglutaric acid disodium are not extensively characterized. The compound has molecular formula C₅H₆O₅Na₂ and is the disodium salt of L-2-hydroxyglutaric acid. It is an important metabolite involved in various biochemical pathways. The compound is also known as (S)-2-Hydroxyglutaric acid disodium and s-2-羟基戊二酸二钠. Storage: follow manufacturer's guidelines. As a small polar molecule, it is expected to have limited membrane permeability and may be transported by specific transporters. Detailed pharmacokinetic parameters including half-life, clearance, and bioavailability require further investigation.
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| Toxicity/Toxicokinetics |
Toxicological information for L-2-Hydroxyglutaric acid disodium is not extensively detailed in the available literature. As a research compound with oncometabolite activity, it should be handled with appropriate safety precautions. Standard safety guidelines for handling research chemicals apply, including use of personal protective equipment (gloves, safety goggles, lab coat) and working in a well-ventilated area. The compound is intended for research use only and is not approved for human therapeutic use. Cytotoxicity studies in cell-based assays help establish the therapeutic window and selectivity index of the compound.
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| References | |
| Additional Infomation |
Sodium (S)-2-hydroxypentanedioate is an organic molecular entity that plays a metabolic role in animals.
L-2-Hydroxyglutaric acid disodium (CAS 63512-50-5) is an epigenetic modifier and putative oncometabolite in renal cancer. The compound has molecular formula C₅H₆O₅Na₂. L-2-Hydroxyglutaric acid disodium inhibits histone demethylases, thereby promoting histone methylation. It also inhibits mitochondrial creatine kinase (Mi-CK) activity with Km and Ki values of 2.52 mM and 11.13 mM, respectively. The compound is involved in various biochemical pathways including energy production and amino acid metabolism. Also known as (S)-2-Hydroxyglutaric acid disodium and s-2-羟基戊二酸二钠. |
| Molecular Formula |
C5H6O5-2.2[NA+]
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| Molecular Weight |
192.07774
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| Exact Mass |
192.001
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| CAS # |
63512-50-5
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| Related CAS # |
L-2-Hydroxyglutaric acid;13095-48-2
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| PubChem CID |
56845267
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| Appearance |
White to off-white solid powder
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| Melting Point |
>300ºC
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
12
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| Complexity |
130
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C(CC(=O)[O-])[C@@H](C(=O)[O-])O.[Na+].[Na+]
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| InChi Key |
DZHFTEDSQFPDPP-QTNFYWBSSA-L
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| InChi Code |
InChI=1S/C5H8O5.2Na/c6-3(5(9)10)1-2-4(7)8;;/h3,6H,1-2H2,(H,7,8)(H,9,10);;/q;2*+1/p-2/t3-;;/m0../s1
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| Chemical Name |
disodium;(2S)-2-hydroxypentanedioate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~83.33 mg/mL (~433.83 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 25 mg/mL (130.15 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with heating and sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.2062 mL | 26.0308 mL | 52.0616 mL | |
| 5 mM | 1.0412 mL | 5.2062 mL | 10.4123 mL | |
| 10 mM | 0.5206 mL | 2.6031 mL | 5.2062 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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