产品说明
生化/生理作用
ETaKG is a cell-permeable, aqueous stable, bioavailable, non-toxic α-ketoglutarate/2-oxoglutarate (α-KG/2-OG) diester derivative that readily undergoes hydrolysis by cytosolic esterases to α-KG. The monoester analog, TaKG is also membrane permeant. ETaKG elevates intracellular [α-KG] by ~15-fold in a prologned fashion, destabilizes HIF-1α/2α and reactivates prolyl hydroxylases (PHDs) in hypoxic HCT116, A431 and RPE cells at 2 mM. Further, shown to selectively trigger PHD-dependent cell death in hypoxic cells and decreases cellular [ATP] and glucose uptake. ETaKG has shown to reduce glucose metabolism, elevate [α-KG] levels and suppress A375 xenograft tumor growth (750 mg/kg of mice, p.o., q.d., 14 days). Also, induces mTORC1 lysosomal translocation and stimulates mTORC1 activity in the absence of glutaminolysis in U2OS cells.
基本信息
经验(实验)分子式 | C15H15F3O5 |
分子量 | 332.27 |
PubChem化学物质编号 | 329826049 |
NACRES | NA.77 |
产品性质
质量水平 | 100 |
测定 | ≥95% (HPLC) |
形式 | oil |
颜色 | colorless to light yellow |
储存温度 | 2-8℃ |
SMILES string | O=C(C(CCC(OCC)=O)=O)OCC1=CC=CC(C(F)(F)F)=C1 |
安全信息
储存分类代码 | 13 - Non Combustible Solids |
WGK | WGK 3 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |
Sigma-Aldrich