Ezatiostat

Catalog No.S9698 Batch:S969802

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	25 mg/mL (38.83 mM)
		Water	Insoluble
* <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.)

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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 GST_π^+/+ and not in GST_π^-/- 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.

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.

References

[1] J E Ruscoe, et al. J Pharmacol Exp Ther. 2001 Jul;298(1):339-45.

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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.

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