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

Cat. No.: HY-100542 Purity: >98.0%
Handling Instructions

D-alpha-Hydroxyglutaric acid disodium salt is a weak competitive α-Ketoglutarate(α-KG)-dependent dioxygenase inhibitor with Ki of 10.87±1.85 mM. Ki for L-Hydroxyglutaric acid (L-2-HG) is 0.628±0.036 mM.

For research use only. We do not sell to patients.

D-alpha-Hydroxyglutaric acid disodium salt Chemical Structure

D-alpha-Hydroxyglutaric acid disodium salt Chemical Structure

CAS No. : 103404-90-6

Size Price Stock Quantity
10 mM * 1 mL in Water USD 66 In-stock
Estimated Time of Arrival: December 31
10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
25 mg USD 84 In-stock
Estimated Time of Arrival: December 31
50 mg USD 144 In-stock
Estimated Time of Arrival: December 31
100 mg USD 240 In-stock
Estimated Time of Arrival: December 31
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

D-alpha-Hydroxyglutaric acid disodium salt is a weak competitive α-Ketoglutarate(α-KG)-dependent dioxygenase inhibitor with Ki of 10.87±1.85 mM. Ki for L-Hydroxyglutaric acid (L-2-HG) is 0.628±0.036 mM.

IC50 & Target

Ki: 10.87±1.85 mM (α-KG)[1]

In Vitro

Addition of 50 mM and 100 mM of D-alpha-Hydroxyglutaric acid (D-2-HG) results in partial and nearly complete inhibition of CeKDM7A, respectively. To further examine the mode of interaction between α-KG and D-2-HG, CeKDM7A are incubated with a fixed concentration (50 mM) of D-2-HG and increasing amount of α-KG. A partial inhibition of KDM7A toward both H3K9me2 and H3K27me2 peptides is observed in the presence of 50 mM D-2-HG and 100 μM α-KG. Addition of 300 μM α-KG is capable of reversing the inhibition of CeKDM7A by 50 mM D-2-HG, indicating that D-2-HG is a weak competitive inhibitor against α-KG toward the CeKDM7A demethylase. D-2-HG with Ki of 10.87±1.85 mM for inhibiting KDM5B/JARID1B/PLU-1[1]. D-alpha-Hydroxyglutaric acid (R-2HG) increases the lifespan of C. elegans. (R)-2HG interacts distinctly with the α-KG dependent dioxygenases. The intracellular (R)-2HG levels are 20-100 fold higher in U87 and HCT 116 cells expressing IDH1(R132H) than in control cells. The elevated (R)-2HG levels are comparable to those found in cells treated with octyl (R)-2HG, and levels reported for IDH1-mutant tumor samples[2].

Solvent & Solubility
In Vitro: 

H2O : ≥ 32 mg/mL (166.60 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

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 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 (NH4)2Fe(SO4)2, 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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[2]

U87 cells, HCT 116 IDH1(R132H/+) cells, and HEK 293 cells are seeded in 12-well plates and after overnight incubation are treated with indicated concentrations of each compound (e.g., 400 and 800 μM D-2-HG). After harvesting, cells are stained with Acridine Orange (AO) and DAPI. Cell number and viability are measured based on AO and DAPI fluorescence measured by NC3000[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

192.08

Formula

C₅H₆Na₂O₅

CAS No.

103404-90-6

SMILES

O=C([O-])[[email protected]](O)CCC([O-])=O.[Na+].[Na+]

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: >98.0%

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Product Name:
D-alpha-Hydroxyglutaric acid disodium salt
Cat. No.:
HY-100542
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D-alpha-Hydroxyglutaric acid disodium salt

Cat. No.: HY-100542