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Ezatiostat hydrochlorideGST inhibitor

Ezatiostat hydrochloride

Catalog No. B1250
Size Price Stock Qty
10mM (in 1mL DMSO) $140.00 In stock
5mg $76.00 In stock
10mg $128.00 In stock
25mg $209.00 In stock
50mg $380.00 In stock
100mg $646.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Liu X, et al. "Human glutathione S-transferase P1-1 functions as an estrogen receptor α signaling modulator." Biochem Biophys Res Commun. 2014 Sep 16. pii: S0006-291X(14)01625-8. PMID: 25218501

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Chemical structure

Ezatiostat hydrochloride

Related Biological Data

Ezatiostat hydrochloride

Ezatiostat hydrochloride Dilution Calculator

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Chemical Properties

Cas No. 286942-97-0 SDF Download SDF
Chemical Name ethyl (2S)-2-amino-5-[[(2R)-3-benzylsulfanyl-1-[[(1R)-2-ethoxy-2-oxo-1-phenylethyl]amino]-1-oxopropan-2-yl]amino]-5-oxopentanoate;hydrochloride
Canonical SMILES CCOC(=O)C(CCC(=O)NC(CSCC1=CC=CC=C1)C(=O)NC(C2=CC=CC=C2)C(=O)OCC)N.Cl
Formula C27H36ClN3O6S M.Wt 566.11
Solubility >28.3mg/mL in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

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.