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Datasheet of Ezatiostat
Description: Ezatiostat(TER199; TLK199) is a glutathione analog inhibitor of glutathione S-transferase (GST) P1-1. Ezatiostat hydrochloride (TLK199, Telintra) is the first glutathione S-transferase P1-1 (GST P1-1) inhibitor prodrug to demonstrate a clinically significant improvement in the cytopenias affecting patients with myelodysplastic syndrome (MDS), thereby validating this enzyme as a candidate target for pharmacologic intervention. Structurally, ezatiostat is a tripeptide glutathione analog diethyl ester that is metabolized in vivo to the diacid, which is a potent and selective inhibitor of GST P1-1, an enzyme overexpressed in many human hematologic cancers. This inhibition induces a dissociation of GST P1-1 from its complex with c-jun N-terminal kinase (JNK)/c-Jun and activates signaling pathways that lead to cell proliferation and differentiation of normal hematopoietic cells and apoptosis of malignant cells.
Chemical Information Catalog
DC7204
Purity of current batch:
>98%
Molecular Weight (MW)
376.41
Molecular Formula
C21H20N4O3
CAS No.
168682-53-9
Solubility (25째C)
DMSO
Storage
Store at -20째C (desiccating conditions).
Handling: Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months. Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20째C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.