Home Metabolism Transferase inhibitor - JNK activator - ERK activator - Apoptosis related activator Ezatiostat For research use only.

Ezatiostat

Synonyms: TER199, TLK199

Ezatiostat, a tripeptide analog of glutathione, is a peptidomimetic inhibitor of Glutathione S-transferase P1-1 (GSTP1-1). Ezatiostat activates c-Jun NH2 terminal kinase (JNK1) and ERK1/ERK2 and induces apoptosis.

Ezatiostat Chemical Structure

Ezatiostat Chemical Structure

CAS No. 168682-53-9

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Ezatiostat Related Products

Signaling Pathway

Transferase Signaling Pathways

Transferase Signaling Pathway

Biological Activity

Description Ezatiostat, a tripeptide analog of glutathione, is a peptidomimetic inhibitor of Glutathione S-transferase P1-1 (GSTP1-1). Ezatiostat activates c-Jun NH2 terminal kinase (JNK1) and ERK1/ERK2 and induces apoptosis.
Targets
GSTP1-1 [1] JNK1 [1] ERK1/ERK2 [1]
In vitro
In vitro

Selection of a resistant clone of an HL60 tumor cell line through chronic exposure to Ezatiostat (TLK199) results in cells with elevated activities of c-Jun NH2 terminal kinase (JNK1) and ERK1/ERK2, and allows the cells to proliferate under stress conditions that induced high levels of apoptosis in the wild type cells.[1]
Cell Research Cell lines Human myeloid leukemic cells (HL60)
Concentrations 2.5 μM - 50 μM
Incubation Time 8 h, 24 h
Method

Human myeloid leukemic cells (HL60) are chronically exposed to TLK199, and drug-resistant cells are selected by passage. Cells are initially exposed to 2.5 μM (1/10th IC50), and the drug concentration is increased in increments of 5 μM after 3 to 4 passages. Cells resistant to 50 μM TLK199 are cloned from single cells and selected for investigation.
In Vivo
In vivo

Ezatiostat (TLK199) stimulates both lymphocyte production and bone marrow progenitor (colony-forming unitgranulocyte macrophage) proliferation, but only in GSTπ+/+ and not in GSTπ-/- animals.[1]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01459159 Terminated
Myelodysplastic Syndrome (MDS)
Telik
 October 2011 Phase 2
NCT01422486 Terminated
Myelodysplastic Syndrome (MDS)
Telik
 October 2011 Phase 2

Chemical Information & Solubility

Molecular Weight 643.67 Formula

C29H36F3N3O8S
CAS No. 168682-53-9 SDF --
Smiles CCOC(=O)C(N)CCC(=O)NC(CSCC1=CC=CC=C1)C(=O)NC(C(=O)OCC)C2=CC=CC=C2.OC(=O)C(F)(F)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (155.35 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 15 mg/mL

Water : Insoluble


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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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