Powder: -20°C for 3 years | In solvent: -80°C for 1 year
D-α-Hydroxyglutaric acid disodium (Disodium (R)-2-Hydroxyglutarate) 是神经代谢疾病 D-2-羟基戊二酸尿症中积累的主要代谢产物,可增加活性氧的产生。它是 α-酮戊二酸 (α-KG) 的弱竞争拮抗剂,可抑制多种α-KG 依赖性双加氧酶,Ki 为 10.87 mM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 233 | 现货 | ||
10 mg | ¥ 323 | 现货 | ||
25 mg | ¥ 578 | 现货 | ||
50 mg | ¥ 933 | 现货 | ||
100 mg | ¥ 1,660 | 现货 | ||
200 mg | ¥ 2,470 | 现货 | ||
500 mg | ¥ 3,970 | 现货 |
产品描述 | D-α-Hydroxyglutaric acid disodium (Disodium (R)-2-Hydroxyglutarate) is a competitive inhibitor of α-ketoglutarate-dependent dioxygenases with Ki of 0.628 mM. |
靶点活性 | α-ketoglutarate-dependent dioxygenase:0.628 mM(Ki) |
体外活性 | 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] |
激酶实验 | 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. |
细胞实验 | 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) |
别名 | D-alpha-Hydroxyglutaric acid disodium salt, (R)-2-羟基戊二酸二钠盐, Disodium (R)-2-Hydroxyglutarate |
分子量 | 192.08 |
分子式 | C5H6Na2O5 |
CAS No. | 103404-90-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 2.5 mM
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 5.2062 mL | 26.0308 mL | 52.0616 mL | 130.1541 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
D-α-Hydroxyglutaric acid disodium 103404-90-6 Immunology/Inflammation Membrane transporter/Ion channel Metabolism NF-Κb Others PI3K/Akt/mTOR signaling ATPase Reactive Oxygen Species Endogenous Metabolite mTOR DαHydroxyglutaric acid disodium ATP Synthase excitotoxic Mammalian target of Rapamycin D-a-Hydroxyglutaric acid disodium 5-methlycytosine H3K9me2 H3K27me2 inhibit Inhibitor IDH2 neurotoxic IDH1 α-ketoglutarate competitor D-alpha-Hydroxyglutaric acid D-alpha-Hydroxyglutaric acid disodium salt D-α-Hydroxyglutaric acid D-alpha-Hydroxyglutaric acid disodium Disodium 2-Hydroxyglutarate CeKDM7A (R)-2-羟基戊二酸二钠盐 D α Hydroxyglutaric acid disodium D-a-Hydroxyglutaric acid Disodium (R)-2-Hydroxyglutarate inhibitor