L-gamma-Glutamyl-S-(phenylmethyl)-L-cysteinyl-2-phenylglycine diethyl ester monohydrochloride
L-gamma-Glutamyl-S-(phenylmethyl)-L-cysteinyl-2-phenylglycine diethyl ester monohydrochloride Basic information
- Product Name:
- L-gamma-Glutamyl-S-(phenylmethyl)-L-cysteinyl-2-phenylglycine diethyl ester monohydrochloride
- Synonyms:
-
- Ezatiostat hydrochloride
- L-gamma-Glutamyl-S-(phenylmethyl)-L-cysteinyl-2-phenylglycine diethyl ester monohydrochloride
- L-gamma-Glutamyl-S-(phenylmethyl)-L-cysteinyl-D-phenylglycine diethyl ester monohydrochloride
- Ezatiostat (TER199) HCl
- Ezatiostat HCl
- gamma-Glu-S-bzcys-phgly diethyl ester
- Unii-D59N834676
- Glycine,L-g-glutaMyl-S-(phenylMethyl)-L-cysteinyl-2-phenyl-,diethyl ester, Monohydrochloride
- CAS:
- 286942-97-0
- MF:
- C27H35N3O6S.ClH
- MW:
- 566.115
- Mol File:
- 286942-97-0.mol
L-gamma-Glutamyl-S-(phenylmethyl)-L-cysteinyl-2-phenylglycine diethyl ester monohydrochloride Chemical Properties
- solubility
- >28.3mg/mL in DMSO
- form
- Powder
L-gamma-Glutamyl-S-(phenylmethyl)-L-cysteinyl-2-phenylglycine diethyl ester monohydrochloride Usage And Synthesis
Uses
Ezatiostat hydrochloride (TER199; TLK199 hydrochloride) is a tripeptide analog of glutathione and is a selective and orally active glutathione S-transferase P1-1 (GSTP1) inhibitor. Ezatiostat hydrochloride leads to JNK activation by inhibiting GSTP1. Ezatiostat hydrochloride stimulates both lymphocyte production and bone marrow progenitor proliferation. Ezatiostat hydrochloride has the potential for myelodysplastic syndrome (MDS) treatment[1][2].
in vivo
Administration of Ezatiostat (TLK199), stimulates both lymphocyte production and bone marrow progenitor (colony-forming unit-granulocyte macrophage) proliferation, but only in glutathione S-transferase P1-1 (GSTP1+/+) and not in GSTP1-/-animals[2].
References
[1] Galili N, et al. Prediction of response to therapy with ezatiostat in lower risk myelodysplastic syndrome. J Hematol Oncol. 2012 May 6;5:20 DOI:10.1186/1756-8722-5-20
[2] Ruscoe JE, et al. Pharmacologic or genetic manipulation of glutathione S-transferase P1-1 (GSTpi) influences cell proliferation pathways. J Pharmacol Exp Ther. 2001 Jul;298(1):339-45. PMID:11408560
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