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SML1743 Sigma-Aldrich

ETaKG

≥95% (HPLC)

Synonym: 2-Oxo-pentanedioic acid 5-ethyl ester 1-(3-trifluoromethyl-benzyl) ester, 5-Ethyl 1-(3-(trifluoromethyl)benzyl) 2-oxopentanedioate

  • Empirical Formula (Hill Notation) C15H15F3O5

  • Molecular Weight 332.27

  •  PubChem Substance ID 329826049

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Properties

Related Categories Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience, Cell Stress,
assay   ≥95% (HPLC)
form   oil
color   colorless to light yellow
storage temp.   2-8°C

Description

Biochem/physiol Actions

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.

Safety & Documentation

Safety Information

RIDADR 
NONH for all modes of transport

Documents

Certificate of Analysis

Protocols & Articles
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