Ezatiostat

Catalog No.S9698 Batch:S969801

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Technical Data

Formula

C29H36F3N3O8S
Molecular Weight 643.67 CAS No. 168682-53-9
Solubility (25°C)* In vitro DMSO 100 mg/mL (155.35 mM)
Ethanol 15 mg/mL (23.3 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO Corn oil
6.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 120 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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]
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]

Protocol (from reference)

Cell Assay:

[1]
  • 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.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.