Art. -Nr.: HY-13634A

Ezatiostat

(Synonyms: TER199free base; TLK199)

8 Cited Publications

Kundenbewertung

Based on 8 publication(s) in Google Scholar

Ezatiostat (TER199 free base; TLK199) is a tripeptide analog of glutathione and is a selective and orally active glutathione S-transferase P1-1 (GSTP1) inhibitor. Ezatiostat leads to JNK activation by inhibiting GSTP1. Ezatiostat stimulates both lymphocyte production and bone marrow progenitor proliferation. Ezatiostat has the potential for myelodysplastic syndrome (MDS) treatment.

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Reinheit: 99.71%
CAS. Nr.: 168682-53-9
Formel: C₂₇H₃₅N₃O₆S
Molecular Weight:529.65

Speicherung:

Sealed storage, away from moisture.

Powder -80°C, 2 years , -20°C, 1 year

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Ezatiostat Chemical Structure

CAS. Nr.: 168682-53-9

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (8)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Glutathione S-transferase P1-1 (GSTP1)^[1]

In Vitro

Ezatiostat causes dissociation of the enzyme from the jun-N-terminal kinase/c-Jun (JNK/JUN) complex, leading to JNK activation by phosphorylation. The therapeutic action of ezatiostat appears to include both proliferation of normal myeloid progenitors as well as apoptosis of the malignant clone^[1].
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 allowes the cells to proliferate under stress conditions that induced high levels of apoptosis in the wild type cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Administration of Ezatiostat (TLK199), stimulates both lymphocyte production and bone marrow progenitor (colony-forming unit-granulocyte macrophage) proliferation, but only in glutathione S-transferase P1-1 (GSTP1^+/+) and not in GSTP1^-/- animals^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 168682-53-9
Appearance Solid
Molecular Weight 529.65
Formel C₂₇H₃₅N₃O₆S
Color White to off-white
Synonyms

TER199free base; TLK199
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Sealed storage, away from moisture

Powder	-80°C	2 years
	-20°C	1 year

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (8)

All Cell Proliferation/Viability AssayBio/Physico-chemical AssayIn Vivo Efficacy StudyWB

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Journal Impact Factor

Cell Res

Tom20 senses iron-activated ROS signaling to promote melanoma cell pyroptosis. [Abstract]

2018 Dec;28(12):1171-1185. PMID: 30287942
Redox Biol

Tryptanthrin targets GSTP1 to induce senescence and increases the susceptibility to apoptosis by senolytics in liver cancer cells. [Abstract]

2024 Aug 20:76:103323. PMID: 39180983

Ezatiostat purchased from MedChemExpress. Usage Cited in: Redox Biol. 2024 Aug 20:76:103323. [Abstract]

Huh7 cells were treated with 0, 5, 10, and 20 μM Ezatiostat (TLK199) for 72 h, followed by FACS analysis to assess ROS production.

Ezatiostat purchased from MedChemExpress. Usage Cited in: Redox Biol. 2024 Aug 20:76:103323. [Abstract]

Protein expression levels of Lamin B1, p21, γ-H2AX and H2AX were detected by western blot upon treatment of Ezatiostat (TLK199, 0-20 μM, 72 h), with β-actin as a loading control.
Redox Biol

GSTP1-mediated S-glutathionylation of Pik3r1 is a redox hub that inhibits osteoclastogenesis through regulating autophagic flux. [Abstract]

2023 May:61:102635. PMID: 36870110
Adv Sci (Weinh)

Targeting GSTP1 as Therapeutic Strategy against Lung Adenocarcinoma Stemness and Resistance to Tyrosine Kinase Inhibitors. [Abstract]

2023 Mar;10(7):e2205262. PMID: 36709476

Ezatiostat purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Mar;10(7):e2205262. [Abstract]

In vitro effects of treatment with the GSTP1 inhibitor Ezatiostat (12.5 μM) on crizotinib sensitivity in LUAD-OG1 evaluated by Cell titer-Glo cell viability assay.

Ezatiostat purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Mar;10(7):e2205262. [Abstract]

Schematic diagram of the treatment regimen with 1% Tween 80/saline (Group 1), crizotinib (10 mg/kg; Group2), ezatiostat (25 mg/kg; Group 3), or the combination of ezatiostat with crizotinib (Group 4) in NOD-SCID mice. n = 4 mice per group. Representative image of LUAD-OG1 xenografts from the four groups at the endpoint are shown.

Ezatiostat purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Mar;10(7):e2205262. [Abstract]

Ex vivo effects of GSTP1 inhibitor Ezatiostat (12.5 and 25 μM) treatment on crizotinib sensitivity in crizotinib-resistant LUAD-OG1 evaluated by Cell titer-Glo cell viability assay.

Ezatiostat purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Mar;10(7):e2205262. [Abstract]

Schematic diagram of oral gavage of the treatment regimen with 1% Tween 80/saline (Group 1), crizotinib (25 mg kg−1; Group2), ezatiostat (25 mg/kg; Group 3), or the combination of ezatiostat with crizotinib (Group 4) in SCID mice.
Phytomedicine

Galangin alleviated Doxorubicin-induced cardiotoxicity by inhibiting ferroptosis through GSTP1/JNK pathway. [Abstract]

2024 Aug 31:134:155989. PMID: 39217656
Free Radic Biol Med

Mifepristone protects acetaminophen induced liver injury through NRF2/GSH/GST mediated ferroptosis suppression. [Abstract]

2024 Jun 19:S0891-5849(24)00531-8. PMID: 38906233
Arch Biochem Biophys

Subcellular distribution and Nrf2/Keap1-interacting properties of Glutathione S-transferase P in hepatocellular carcinoma. [Abstract]

2024 Jul:757:110043. PMID: 38789086
Cancer Biomark

TUBB3 (βIII-tubulin) drives gastric cancer progression and poor prognosis by regulating cell cycle and invadopodia formation. [Abstract]

2025 Oct;42(10):18758592251390145. PMID: 41129675

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (188.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : ≥ 100 mg/mL (188.80 mM)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8880 mL

9.4402 mL

18.8804 mL

5 mM

0.3776 mL

1.8880 mL

3.7761 mL

10 mM

0.1888 mL

0.9440 mL

1.8880 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.75 mg/mL (5.19 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.75 mg/mL (5.19 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.75 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.75 mg/mL (5.19 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Galili N, et al. Prediction of response to therapy with ezatiostat in lower risk myelodysplastic syndrome. J Hematol Oncol. 2012 May 6;5:20 [Content Brief]

[2]. Ruscoe JE, et al. Pharmacologic or genetic manipulation of glutathione S-transferase P1-1 (GSTpi) influences cell proliferation pathways. J Pharmacol Exp Ther. 2001 Jul;298(1):339-45. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / Ethanol	1 mM	1.8880 mL	9.4402 mL	18.8804 mL	47.2010 mL
	5 mM	0.3776 mL	1.8880 mL	3.7761 mL	9.4402 mL
	10 mM	0.1888 mL	0.9440 mL	1.8880 mL	4.7201 mL
	15 mM	0.1259 mL	0.6293 mL	1.2587 mL	3.1467 mL
	20 mM	0.0944 mL	0.4720 mL	0.9440 mL	2.3600 mL
	25 mM	0.0755 mL	0.3776 mL	0.7552 mL	1.8880 mL
	30 mM	0.0629 mL	0.3147 mL	0.6293 mL	1.5734 mL
	40 mM	0.0472 mL	0.2360 mL	0.4720 mL	1.1800 mL
	50 mM	0.0378 mL	0.1888 mL	0.3776 mL	0.9440 mL
	60 mM	0.0315 mL	0.1573 mL	0.3147 mL	0.7867 mL
	80 mM	0.0236 mL	0.1180 mL	0.2360 mL	0.5900 mL
	100 mM	0.0189 mL	0.0944 mL	0.1888 mL	0.4720 mL

Ezatiostat

8 Cited Publications

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Ezatiostat

Peptidomimetic Library

Peptide Library

MCE Bioactive Compound Library

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) Ezatiostat

Biologische Aktivität

Chemical Information

Publications (8)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Ezatiostat

Peptidomimetic Library

Peptide Library

MCE Bioactive Compound Library

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) Ezatiostat

Biologische Aktivität

Chemical Information

Publications (8)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Ezatiostat Related Classifications

HY-13634A Related Classifications