| CAS NO: | 876150-14-0 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| Cas No. | 876150-14-0 |
| 别名 | α-KG octyl ester |
| 化学名 | 2-oxo-pentanedioic acid, 1-octyl ester |
| Canonical SMILES | OC(CCC(C(OCCCCCCCC)=O)=O)=O |
| 分子式 | C13H22O5 |
| 分子量 | 258.3 |
| 溶解度 | ≤20mg/ml in ethanol;10mg/ml in DMSO;10mg/ml in dimethyl formamide |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Octyl-α-ketoglutarate is a stable, cell-permeable form of α-ketoglutarate, a substrate of prolyl hydroxylases (PHD) [1][2]. The high turnover of HIFα is initiated by prolyl hydroxylases (PHD), which hydroxylate proline residues on the oxygen-dependent degradation (ODD) domain of HIFα, facilitating ubiquitination and degradation. To catalyze proline hydroxylation, PHDs convert molecular oxygen and α-ketoglutarate to carbon dioxide and succinate [2]. Loss of IDH1 activity would reduce cellular levels of α-KG [3]. Octyl-α-ketoglutarate is a cell-permeating α-ketoglutarate derivative, which built up rapidly and preferentially in cells with a dysfunctional TCA cycle. Octyl-α-ketoglutarate increased intracellular levels of freeα-ketoglutaric acid by approximately fourfold. In HEK293-derived cell lines expressing both a GFP-ODD fusion protein and HA-tagged pVHL, Octyl-α-ketoglutarate reactivated PHD activity inhibited by succinate or fumarate. Octyl-α-ketoglutarate restored hydroxylation and targeted HIF1 for ubiquitylation and proteasomally mediated degradation [2]. Octyl-α-ketoglutarate inhibited the HIF-1α induction caused by IDH1 knockdown in HeLa cells or overexpression of IDH1R132H mutant in U-87MG cells, suggesting a reduction in IDH1 activity caused a reduction in α-KG levels that in turn led to stabilization of HIF-1α [3]. References: |
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