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D-α-Hydroxyglutaric acid disodium

Catalog No. T6820 CAS 103404-90-6

Synonyms: D-alpha-Hydroxyglutaric acid disodium salt, Disodium (R)-2-Hydroxyglutarate

D-α-Hydroxyglutaric acid disodium (Disodium (R)-2-Hydroxyglutarate) is a competitive inhibitor of α-ketoglutarate-dependent dioxygenases with Ki of 0.628 mM.

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D-α-Hydroxyglutaric acid disodium Chemical Structure

D-α-Hydroxyglutaric acid disodium, CAS 103404-90-6

Pack Size	Availability	Price/USD
5 mg	In stock	$ 30.00
10 mg	In stock	$ 47.00
25 mg	In stock	$ 67.00
50 mg	In stock	$ 112.00
100 mg	In stock	$ 197.00
200 mg	In stock	$ 293.00
500 mg	In stock	$ 490.00

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Purity: 98%

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Description	D-α-Hydroxyglutaric acid disodium (Disodium (R)-2-Hydroxyglutarate) is a competitive inhibitor of α-ketoglutarate-dependent dioxygenases with Ki of 0.628 mM.
Targets&IC50	α-ketoglutarate-dependent dioxygenase:0.628 mM(Ki)
In vitro	In U-87 mg 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	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.(Only for Reference)

Synonyms	D-alpha-Hydroxyglutaric acid disodium salt, Disodium (R)-2-Hydroxyglutarate
Molecular Weight	192.08
Formula	C5H6Na2O5
CAS No.	103404-90-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 2.5 mM

References and Literature

1. Xu W, et al. Cancer Cell. 2011, 19(1), 17-30. 2. Kim SY, et al. Cardiovasc Res. 2011, 92(2), 307-316.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Kinase Inhibitor Library Membrane Protein-targeted Compound Library Anti-Obesity Compound Library Anti-Colorectal Cancer Compound Library PI3K-AKT-mTOR Compound Library NO PAINS Compound Library Anti-Fibrosis Compound Library Reprogramming Compound Library Oxidation-Reduction Compound Library

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