CAS NO: | 103404-90-6 |
包装 | 价格(元) |
10mM (in 1mL H2O) | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 192.08 |
Cas No. | 103404-90-6 |
Formula | C5H6Na2O5 |
Solubility | insoluble in EtOH; insoluble in DMSO; ≥9.1 mg/mL in H2O |
Chemical Name | sodium (R)-2-hydroxypentanedioate |
Canonical SMILES | O[C@](C([O-])=O)([H])CCC([O-])=O.[Na+].[Na+] |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
这里使用(R)-2-hydroxyglutarate ((R)-2HG)代替Disodium (R)-2-Hydroxyglutarate。(R)-2HG抑制腺苷三磷酸(ATP)合成酶[1]。IC50值没有测定结果。
ATP合酶含有旋转马达,参与生物能量转换。它促使无机磷酸盐和腺苷二磷酸(ADP)产生ATP。它主要是从呼吸作用或光合作用产生的跨膜质子原动力的能量来产生作用[2]。
数据表明,(R)-2HG在携带突变异柠檬酸脱氢酶(IDH)1和2的基因的人类癌症中累积。在IDH1突变的细胞中,(R)-2HG抑制ATP合酶。这表明(R)-2HG具有生长抑制功能。在胶质母细胞瘤细胞中,(R)-2HG对ATP合酶的抑制足以杀死肿瘤细胞,并在葡萄糖限制条件下停滞生长,例如,当酮体替代葡萄糖提供能量。在细胞中,(R)-2HG降低了ATP合酶相关的耗氧速率[1]。
(R)-2HG的正常细胞的浓度为200 mM。在该浓度下,(R)-2HG不太可能显著地抑制ATP合酶。在IDH突变的神经胶质瘤患者中,(R)-2HG累积到正常水平的10-100倍,可能抑制 ATP合酶。(R)-2HG用α-KG相似的方式延长了线虫的寿命。数据表明,2-HG增加依赖性ATP合成酶的寿命[1]。
参考文献:
[1]. Fu X, Chin RM, Vergnes L, et al. 2-Hydroxyglutarate inhibits ATP synthase and mTOR signaling. Cell metabolism, 2015, 22(3): 508-515.
[2]. Stock D, Leslie AGW and Walker JE. Molecular architecture of the rotary motor in ATP synthase. Science, 1999, 286(5445): 1700-1705.
Cell experiment:[1] | |
Cell lines | TF-1 cells |
Reaction Conditions | 100 ~ 500 μM (R)-2HG for 0 ~ 12 d incubation |
Applications | TF-1 cells passaged in the presence of the cell membrane-permeable version of (R)-2HG became growth factor-independent and no longer differentiated in response to erythropoietin (EPO). Promotion of growth factor-independence and loss of EPO-responsiveness by (R)-2HG was dose-dependent and passage-dependent. (R)-2HG was sufficient to promote leukemogenesis and its effects were reversible. |
Note | The technical data provided above is for reference only. |
References: 1. Losman JA, Looper RE, Koivunen P, et al. (R)-2-hydroxyglutarate is sufficient to promote leukemogenesis and its effects are reversible. Science, 2013, 339(6127): 1621-1625. |