Ezatiostat hydrochloride

Catalogue Number: B1250-APE

Manufacturer:	Apexbio
Molecular Formula:	C27H36ClN3O6S
Type:	Enzyme Inhibitors
Shipping Condition:	Blue Ice
Unit(s):	10 mg, 10 mM (in 1mL DMSO), 100 mg, 25 mg, 5 mg, 50 mg

Overview
Datasheets

Description

Description: Ezatiostat hydrochloride(TLK199) is an effective inhibitor of glutathione S-transferase (GST) [1].Ezatiostat hydrochloride (TLK199) is a novel glutathione analog and the potential treatment of cytopenias. In addition, Ezatiostat hydrochloride has been revealed to selectively bind to and thus inhibit GST P1-1. Because GST P1-1 can bind to and inhibit JNK, Ezatiostat hydrochloride has also been exhibited to inhibit GST P1-1, activate JNK, and promote the growth and maturation of hematopoietic progenitors in preclinical models. Moreover, Ezatiostat hydrochloride has been reported to stimulate the proliferation of myeloid precursors. Ezatiostat hydrochloride has been elucidated to induce growth inhibition and cellular apoptosis in human leukemia cells (HL-60) with a CC50 value of 6-17µM. Apart from these, Ezatiostat hydrochloride has shown the stimulation of multilineage differentiation in mature monocytes, granulocytes and erythrocytes [1,2].References:[1] Tew KD1, Dutta S, Schultz M.Inhibitors of glutathione S-transferases as therapeutic agents. Adv Drug Deliv Rev. 1997 Jul 7;26(2-3):91-104.[2] Raza A1, Galili N, Callander N, Ochoa L, Piro L, Emanuel P, Williams S, Burris H 3rd, Faderl S, Estrov Z, Curtin P, Larson RA, Keck JG, Jones M, Meng L, Brown GL. Phase 1-2a multicenter dose-escalation study of ezatiostat hydrochloride liposomes for injection (Telintra, TLK199), a novel glutathione analog prodrug in patients with myelodysplastic syndrome. J Hematol Oncol. 2009 May 13;2:20.

Additional Text

Storage Note

Store at -20°C

Short Description

GST inhibitor

Reagent:Smile String

CCOC(=O)C(CCC(=O)NC(CSCC1=CC=CC=C1)C(=O)NC(C2=CC=CC=C2)C(=O)OCC)N.Cl

Solubility

≥28.3 mg/mL in DMSO; ≥3.32 mg/mL in H2O with ultrasonic; ≥3.4 mg/mL in EtOH with ultrasonic

B1250 Datasheet

B1250 CofA

B1250 MSDS

Price

£131.00

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