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D-alpha-Hydroxyglutaric acid disodium salt CAS: 103404-90-6

Category: Inhibitors
Product Name: D-alpha-Hydroxyglutaric acid disodium salt
Cat No: I000206
CAS No: 103404-90-6
Synonyms: D-2-HG;D-2-Hydroxyglutaric Acid
Molecular Formula: C5H6O5 • 2Na
Molecular Weight: 192.1
SMILES: [O-]C(CC[C@@H](O)C([O-])=O)=O.[Na+].[Na+]
Solubility: H2O: ≥ 32 mg/mL
Target: 10.87±1.85 mM (α-KG)[1]
Storage: -20°C
CAS 103404-90-6,D-alpha-Hydroxyglutaric acid disodium salt
  • 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.
Ki & Target: 10.87±1.85 mM (α-KG)[1]
InVitro: 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].

  • Spec

Appearance:A crystalline solid

  • References

[1]. Xu W, et al. Oncometabolite 2-hydroxyglutarate is a competitive inhibitor of α-ketoglutarate-dependent dioxygenases. Cancer Cell. 2011 Jan 18;19(1):17-30.
[2]. Fu X, et al. 2-Hydroxyglutarate Inhibits ATP Synthase and mTOR Signaling. Cell Metab. 2015 Sep 1;22(3):508-15.

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