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(R)-2-羟基戊二酸 /D-α-Hydroxyglutaric acid {[allProObj[0].p_purity_real_show]}

货号:A496476 同义名: (R)-2-Hydroxyglutarate;(R)-2-Hydroxyglutaric acid

D-α-Hydroxyglutaric acid是神经代谢疾病 D-2-羟基戊二酸尿症的主要代谢产物,能够抑制多种 α-酮戊二酸依赖性双加氧酶,Ki 为 10.87 mM,同时通过增加 ROS 生成抑制 ATP 合酶并抑制 mTOR 信号通路,适用于代谢及神经疾病研究。

D-α-Hydroxyglutaric acid 化学结构 CAS号:13095-47-1
D-α-Hydroxyglutaric acid 化学结构
CAS号:13095-47-1
D-α-Hydroxyglutaric acid 3D分子结构
CAS号:13095-47-1
D-α-Hydroxyglutaric acid 化学结构 CAS号:13095-47-1
D-α-Hydroxyglutaric acid 3D分子结构 CAS号:13095-47-1
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D-α-Hydroxyglutaric acid 纯度/质量文件 产品仅供科研

货号:A496476 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 mTOR mTORC1 mTORC2 其他靶点 纯度
AZD-8055 ++++

mTOR (full length), IC50: 0.8 nM

mTOR (truncated), IC50: 0.13 nM

99%+
Gedatolisib ++++

mTOR, IC50: 1.6 nM

98%
GSK1059615 ++

mTOR, IC50: 12 nM

98%
Vistusertib +++

mTOR, IC50: 2.8 nM

99%+
Torin 1 +++

mTOR, IC50: 4.32 nM

+++

mTORC1, IC50: 2 nM

++

mTORC2, IC50: 10 nM

DNA-PK 99%+
Dactolisib +++

mTOR (p70S6K), IC50: 6 nM

98+%
PI-103 +

mTOR, IC50: 30 nM

99%+
WAY-600 ++

mTOR, IC50: 9 nM

99%
Voxtalisib +

mTOR, IC50: 157 nM

99%+
PF-04691502 ++

mTOR, Ki: 16 nM

98+%
Onatasertib ++

mTOR, IC50: 16 nM

DNA-PK 99%+
Chrysophanol EGFR 98%
Samotolisib DNA-PK 99%+
Torkinib +++

mTOR, IC50: 8 nM

PDGFR,DNA-PK 99%+
Everolimus 99%+
WYE-354 +++

mTOR, IC50: 5 nM

98%
Tacrolimus 98%
PP121 ++

mTOR, IC50: 13 nM

VEGFR,PDGFR 99%+
Torin 2 ++++

mTOR, IC50: 0.25 nM

DNA-PK 99%+
Rapamycin ++++

mTOR, IC50: ~0.1 nM

98%
GDC-0349 +++

mTOR, Ki: 3.8 nM

98%
XL388 ++

mTOR, IC50: 9.9 nM

+++

mTORC1, IC50: 8 nM

+

mTORC2, IC50: 166 nM

99%+
WYE-687 +++

mTOR, IC50: 7 nM

98+%
Apitolisib +

mTOR, Ki app: 17 nM

98%+
WYE-132 ++++

mTOR, IC50: 0.19 nM

99%+
Sapanisertib ++++

mTOR, Ki: 1.4 nM

99%+
BGT226 maleate 99%+
ETP-46464 ++++

mTOR, IC50: 0.6 nM

DNA-PK 98%
PI3K-IN-1 +

mTOR, IC50: 157 nM

98+%
Zotarolimus +++

FKBP-12, IC50: 2.8 nM

99+%
OSI-027 +++

mTOR, IC50: 4 nM

+

mTORC1, IC50: 22 nM

+

mTORC2, IC50: 65 nM

99%+
Ridaforolimus ++++

mTOR, IC50: 0.2 nM

99%+
Temsirolimus +

mTOR, IC50: 1.76 μM

95%
CZ415 ++

mTOR, pIC50: 8.07

99%+
SF2523 +

mTOR, IC50: 280 nM

DNA-PK 99%+
KU-0063794 ++

mTORC1, IC50: ~10 nM

++

mTORC2, IC50: ~10 nM

99%+
Omipalisib ++++

mTORC1, Ki: 0.18 nM

++++

mTORC2, Ki: 0.3 nM

99%+
Palomid 529 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

D-α-Hydroxyglutaric acid 生物活性

描述 D-α-Hydroxyglutaric acid is the major cumulative metabolite of the neurometabolic disease D-2-hydroxyglutaric aciduria. D-α-Hydroxyglutaric acid is a weak competitive antagonist of α-ketoglutarate (α-KG) and inhibits a number of α-KG-dependent dioxygenases, with a Ki value of 10.87 mM. D-α Hydroxyglutaric acid increases reactive oxygen species (ROS) production. D-α-Hydroxyglutaric acid binds and inhibits ATP synthase and inhibits mTOR signalling[1][2][3][4][5].In the presence of 50 mM D-2-HG and 100 μM α-ketoglutarate (α-KG), KDM7A partially inhibited both H3K9me2 and H3K27me2 peptides. Addition of 300 μM α-KG was able to reverse the inhibitory effect of 50 mM D-2-HG on Cryptosporidium hidradii KDM7A (CeKDM7A), suggesting that D-2-HG is a weakly competitive inhibitor of α-KG on CeKDM7A demethylases[1].D-α-Hydroxyglutaric acid is a weak inhibitor of TET hydroxylase. In the presence of 0.1 mM α-KG, the addition of 10 mM D-α-Hydroxyglutaric acid resulted in partial inhibition of TET2 (33%), whereas the addition of 50 mM D-α-Hydroxyglutaric acid resulted in greater inhibition of TET2 (83%). D-α Hydroxyglutaric acid inhibited TET1 less significantly[1].

D-α-Hydroxyglutaric acid 动物研究

Animal study D-α-Hydroxyglutaric acid strongly inhibits glucose utilisation, carbon dioxide production and the respiratory chain in rat cerebral cortex and human skeletal muscle as well as in submembranous cartilage granules of bovine heart, suggesting that aerobic metabolism is impaired. D-α-Hydroxyglutaric acid has also been suggested to be an endogenous excitatory organic acid because it inhibits TET1 through stimulation of specific NMDA glutamate receptors and significantly reduced cell viability in chicken embryo telencephalon and neonatal rat hippocampal neuronal cultures[5].

D-α-Hydroxyglutaric acid 参考文献

[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.

[3]Martijn Kranendijk, et al. Progress in understanding 2-hydroxyglutaric acidurias. J Inherit Metab Dis. 2012 Jul;35(4):571-87.

[4]Martin Böttcher, et al. D-2-hydroxyglutarate interferes with HIF-1α stability skewing T-cell metabolism towards oxidative phosphorylation and impairing Th17 polarization. Oncoimmunology. 2018 Mar 26;7(7):e1445454.

[5]Alexandra Latini , et al. D-2-hydroxyglutaric acid induces oxidative stress in cerebral cortex of young rats. Eur J Neurosci. 2003 May;17(10):2017-22.

D-α-Hydroxyglutaric acid 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

6.75mL

1.35mL

0.68mL

33.76mL

6.75mL

3.38mL

67.52mL

13.50mL

6.75mL

D-α-Hydroxyglutaric acid 技术信息

CAS号13095-47-1
分子式C5H8O5
分子量 148.114
别名 (R)-2-Hydroxyglutarate;(R)-2-Hydroxyglutaric acid;D-2-Hydroxyglutaric Acid;D-2-HG;(R)-2-Hydroxypentanedioic acid
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

溶解度

H2O: 200 mg/mL(1350.31 mM),配合低频超声助溶

动物实验配方
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