Ezatiostat | GSTP1 inhibitor

CAS:
 168682-53-9
Catalog Number:
 10-4711

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Ezatiostat (168682-53-9) is a peptidomimetic inhibitor of glutathione S-transferase P1-1 (GSTP1).1,2  It showed significant hematopoietic stimulatory activity possibly via JNK activation through disruption of the GSPT/JNK interaction.3 Ezatiostat displayed efficacy in treating myelodysplastic syndrome.4,5 Combined treatment with ezatiostat and a PRDX6 inhibitor displayed synergistic effects in the treatment of neuroblastoma in vitro and in vivo.6

References/Citations:

  1. Ciaccio et al. (1995) Modulation of detoxification gene expression in human colon HT29 cells by glutathione-S-transferase inhibitors; Mol. Pharmacol, 48 639
  2. Ruscoe et al. (2001) Pharmacologic or genetic manipulation of glutathione S-transferase P1-1 (GSTpi) influences cell proliferation pathways; J. Pharmacol. Exp. Ther., 298 339
  3. Adler et al. (1999) Regulation of JNK signaling by GSTp; EMBO J., 18 1321
  4. Galli et al. (2012) Prediction of response to therapy with ezatiostat in lower risk myelodysplastic syndrome; J. Hematol. Oncol., 5 20
  5. Raza et al. (2012) A phase 2 randomized multicenter study of 2 extended dosing schedules of oral ezatiostat in low to intermediate-1 risk myelodysplastic syndrome; Cancer, 118 2138
  6. Liano-Pons et al. (2025) Combined targeting of PRDX6 and GSTP1 as a potential differentiation strategy for neuroblastoma treatment; Proc. Natl. Acad. Sci. USA, 122 e2427211122
168682-53-9, Ezatiostat, Ezatiostat supplier, GSTP1 inhibitor, TLK 199, TLK199
CAS:
168682-53-9
Catalog Number:
10-4711
Activity:
GSTP1 inhibitor
Chemical Names:
Ethyl (2S)-2-amino-5-[[(2R)-3-benzylsulfanyl-1-[[(1R)-2-ethoxy-2-oxo-1-phenylethyl]amino]-1-oxopropan-2-yl]amino]-5-oxopentanoate
Alternate Name:
TLK199
Molecular Weight:
529.65
Molecular Formula:

C27H35N3O6S

Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
White solid
Purity:

98% HPLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Safety Data Sheet:

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Product Data Sheet:

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Ezatiostat (168682-53-9) is a peptidomimetic inhibitor of glutathione S-transferase P1-1 (GSTP1).1,2  It showed significant hematopoietic stimulatory activity possibly via JNK activation through disruption of the GSPT/JNK interaction.3 Ezatiostat displayed efficacy in treating myelodysplastic syndrome.4,5 Combined treatment with ezatiostat and a PRDX6 inhibitor displayed synergistic effects in the treatment of neuroblastoma in vitro and in vivo.6

References/Citations:

  1. Ciaccio et al. (1995) Modulation of detoxification gene expression in human colon HT29 cells by glutathione-S-transferase inhibitors; Mol. Pharmacol, 48 639
  2. Ruscoe et al. (2001) Pharmacologic or genetic manipulation of glutathione S-transferase P1-1 (GSTpi) influences cell proliferation pathways; J. Pharmacol. Exp. Ther., 298 339
  3. Adler et al. (1999) Regulation of JNK signaling by GSTp; EMBO J., 18 1321
  4. Galli et al. (2012) Prediction of response to therapy with ezatiostat in lower risk myelodysplastic syndrome; J. Hematol. Oncol., 5 20
  5. Raza et al. (2012) A phase 2 randomized multicenter study of 2 extended dosing schedules of oral ezatiostat in low to intermediate-1 risk myelodysplastic syndrome; Cancer, 118 2138
  6. Liano-Pons et al. (2025) Combined targeting of PRDX6 and GSTP1 as a potential differentiation strategy for neuroblastoma treatment; Proc. Natl. Acad. Sci. USA, 122 e2427211122

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