Disodium (R)-2-Hydroxyglutarate

Synonyms: D-α-Hydroxyglutaric acid disodium

Disodium (R)-2-Hydroxyglutarate (D-α-Hydroxyglutaric acid disodium) is a competitive inhibitor of α-ketoglutarate-dependent dioxygenases with Ki of 10.87 ± 1.85 mM.

Disodium (R)-2-Hydroxyglutarate Chemical Structure

Disodium (R)-2-Hydroxyglutarate Chemical Structure

CAS: 103404-90-6

Selleck's Disodium (R)-2-Hydroxyglutarate has been cited by 7 publications

Purity & Quality Control

Batch: Purity: 99.74%
99.74

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Biological Activity

Description Disodium (R)-2-Hydroxyglutarate (D-α-Hydroxyglutaric acid disodium) is a competitive inhibitor of α-ketoglutarate-dependent dioxygenases with Ki of 10.87 ± 1.85 mM.
Targets
α-ketoglutarate-dependent dioxygenase [1]
In vitro
In vitro In U-87MG cells, (R)-2-Hydroxyglutarate acts as weak antagonists of α-KG to inhibit α-KG-dependent histone demethylases and increases dimethylation on both H3K9 and H3K79. [1] Besides, (R)-2-Hydroxyglutarate inhibits ATP synthase and mTOR signaling, and thus causes growth arrest and tumor cell killing. [2]
Kinase Assay Enzymatic Assays
To assay human JHDM1A/KDM2A demethylase activity toward H3K36me2, His tagged JHDM1A is first obtained by transforming pET28a-JHDM1A into Escherichia coli BL21 and protein expression is induced by addition of 1 mM IPTG at 30° C when cell density reaches 0.5 OD600 units. Cells are lysed by sonication and Ni-NTA agarose is used to purify His-JHDM1A fusion proteins. Histone demethylase assay is carried out by incubating 2 μg oligonucleosomes, 4 μg purified His-JHDM1A, and/or 10–50 mM L- or D-2-HG in histone demethylation buffer [50 mM HEPES (pH 8.0), 625 μM Fe(NH4)2(SO4)2, 0.1–0.5 mM α-KG, 2 mM ascorbate] at 37° C for 2–3 hr and the reactions are stopped by the addition of SDS loading buffer and subsequently analyzed by western blotting using anti-H3K36me2 antibody. To measure CeKDM7A demethylase activity toward H3K9me2 and H3K27me2, two synthetic dimethylated peptides H3K9me2 [ARTKQTARK (me2)STGGKA] and H3K27me2 [QLATKAARK (me2)SAPAS] are used as substrates. Demethylase assays are carried out in the presence of 10 μg enzyme, 1 μg peptide in 20 μl buffer 20 mM Tris-HCl (pH 7.5), 150 mM NaCl, 50 μM Fe(NH4)2(SO4)22, 100 μM α-KG, 2 mM Vc, 10 mM PMSF for 3 hr. The demethylation reaction mixture is desalted by passing through a C18 ZipTip. To examine the inhibitory effect of 2-HG, various concentrations of 2-HG are incubated with KDM7A briefly before adding other reaction mixtures. The samples are analyzed by a MALDI-TOF/TOF mass spectrometer.
Cell Research Cell lines U87/IDH1(R132H), Octyl α-KG- or octyl 2-HG-treated U87, and HCT 116 IDH1(R132H/+) cells
Concentrations ~800 μM
Incubation Time 4 days
Method

Cells are seeded in 12-well plates and, after overnight incubation, treated with the indicated concentrations of each compound. After harvesting, cells are stained with acridine orange (AO) and 4′,6-diamidino-2-phenylindole (DAPI). Cell number and viability are measured based on AO and DAPI fluorescence as measured by NC3000 following the manufacturer’s instructions.

Chemical Information & Solubility

Molecular Weight 192.08 Formula

C5H6Na2O5

CAS No. 103404-90-6 SDF Download Disodium (R)-2-Hydroxyglutarate SDF
Smiles C(CC(=O)[O-])C(C(=O)[O-])O.[Na+].[Na+]
Storage (From the date of receipt)

In vitro
Batch:

Water : 38 mg/mL

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : Insoluble


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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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