Ezatiostat hydrochloride |
| Katalog-Nr.GC13409 |
Ezatiostat-Hydrochlorid (TER199; TLK199-Hydrochlorid) ist ein Tripeptid-Analogon von Glutathion und ein selektiver und oral aktiver Glutathion-S-Transferase-P1-1 (GSTP1)-Inhibitor. Ezatiostathydrochlorid fÜhrt zu einer JNK-Aktivierung durch Hemmung von GSTP1. Ezatiostathydrochlorid stimuliert sowohl die Lymphozytenproduktion als auch die Proliferation von KnochenmarksvorlÄuferzellen. Ezatiostathydrochlorid hat das Potenzial zur Behandlung des myelodysplastischen Syndroms (MDS).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 286942-97-0
Sample solution is provided at 25 µL, 10mM.
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Ezatiostat hydrochloride(TLK199) is an effective inhibitor of glutathione S-transferase （GST）[1].
Ezatiostat hydrochloride (TLK199) is a novel glutathione analog and the potential treatment of cytopenias. In addition, Ezatiostat hydrochloride has been revealed to selectively bind to and thus inhibit GST P1-1. Because GST P1-1 can bind to and inhibit JNK, Ezatiostat hydrochloride has also been exhibited to inhibit GST P1-1, activate JNK, and promote the growth and maturation of hematopoietic progenitors in preclinical models. Moreover, Ezatiostat hydrochloride has been reported to stimulate the proliferation of myeloid precursors. Ezatiostat hydrochloride has been elucidated to induce growth inhibition and cellular apoptosis in human leukemia cells (HL-60) with a CC50 value of 6-17μM. Apart from these, Ezatiostat hydrochloride has shown the stimulation of multilineage differentiation in mature monocytes, granulocytes and erythrocytes [1,2].
References:
[1] Tew KD1, Dutta S, Schultz M.Inhibitors of glutathione S-transferases as therapeutic agents. Adv Drug Deliv Rev. 1997 Jul 7;26(2-3):91-104.
[2] Raza A1, Galili N, Callander N, Ochoa L, Piro L, Emanuel P, Williams S, Burris H 3rd, Faderl S, Estrov Z, Curtin P, Larson RA, Keck JG, Jones M, Meng L, Brown GL. Phase 1-2a multicenter dose-escalation study of ezatiostat hydrochloride liposomes for injection (Telintra, TLK199), a novel glutathione analog prodrug in patients with myelodysplastic syndrome. J Hematol Oncol. 2009 May 13;2:20.
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