Ezatiostat

SKU: orb1689912

Description

Ezatiostat (TER199 free base) is a synthetic tripeptide glutathione analog and a selective inhibitor of the GSTP1-1 enzyme. It is utilized in biochemical and cancer research to study glutathione metabolism and drug resistance mechanisms in both cellular and animal models.

Research Area

Cell Biology, Metabolism Research

Key Properties

• CAS Number: 168682-53-9
• MW: 529.65
• Purity: 97.95% (May vary between batches)
• Formula: C₂₇H₃₅N₃O₆S
• SMILES: CCOC(=O)[C@@H](N)CCC(=O)N[C@@H](CSCc1ccccc1)C(=O)N[C@@H](C(=O)OCC)c1ccccc1
• Target: Glutathione Peroxidase,GST,Apoptosis
• Solubility: H2O:Insoluble;10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.78 mM);DMSO:>50 mg/mL (94.4 mM);Ethanol:20 mg/mL (37.76 mM)

Bioactivity

• In Vivo:
  Ezatiostat was administered to 19 patients with non-deletion(5q) myelodysplastic syndrome (MDS) at one of two doses (2000 mg or 2500 mg/day) in combination with 10 mg of lenalidomide on days 1-21 of a 28-day cycle. One of 4 evaluable patients (25%) in the 2500/10 mg dose group experienced an erythroid hematologic improvement (HI-E) response by 2006 MDS International Working Group (IWG) criteria. Four of 10 evaluable patients (40%) in the 2000 mg/10 mg dose group experienced a HI-E response . Systemic inhibition of GSTP1 with Ezatiostat (0-30 mg/kg, i.p.) dose-dependently reduced the reinforcing effects of alcohol as measured by operant self-administration, in the absence of motor effects .

Storage & Handling

• Storage: keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

proliferation, TER199(free base), TLK 199, TLK199, TLK-199, tripeptide, Inhibitor, inhibit, JNK, lymphocyte, ERK1, Ezatiostat, Gutathione S-transferase, GST, GSTs, GSTP1-1, GSTP1, Glutathione Peroxidase, GlutathionePeroxidase, Glutathione transferases, MDS, c-Jun, Apoptosis

Compound Identifiers

PubChem CID

5310939