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Cat. No.: HY-13634

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Ezatiostat hydrochloride

Name: Ezatiostat hydrochloride
Brand: MedChemExpress
SKU: HY-13634
Availability: PreOrder

(Synonyms: TER199; TLK199 hydrochloride)

8 Cited Publications

고객리뷰

Based on 8 publication(s) in Google Scholar

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

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No.: 286942-97-0
화학식: C₂₇H₃₆ClN₃O₆S
분자량:566.11

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

Ezatiostat hydrochloride Chemical Structure

CAS No.: 286942-97-0

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (8)
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 286942-97-0
분자량 566.11
화학식 C₂₇H₃₆ClN₃O₆S
Synonyms

TER199; TLK199 hydrochloride
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

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 Oct:76:103323. PMID: 39180983

Ezatiostat hydrochloride purchased from MedChemExpress. Usage Cited in: Redox Biol. 2024 Oct: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 hydrochloride purchased from MedChemExpress. Usage Cited in: Redox Biol. 2024 Oct: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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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 Nov:134:155989. PMID: 39217656
Free Radic Biol Med

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

2024 Sep:222:229-243. 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

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 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)

References

[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]

Calculators

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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.

Bioz

Ezatiostat hydrochloride

8 Cited Publications

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Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (8)
순도&문서
References

1/16
1/16

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

Customer Validation
Huh7 cells were treated with 0, 5, 10, and 20 μM Ezatiostat (TLK199) for 72 h, followed by FACS analysis to assess ROS production.
1/16

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

Customer Validation
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.
1/16

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

Customer Validation
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.
1/16

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

Customer Validation
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.
1/16

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

Customer Validation
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.
1/16

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

Customer Validation
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.

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Ezatiostat hydrochloride

Ezatiostat

GSTO1-IN-1

TLK117

GSTO-IN-2

LAS17

Seneciphylline

Seneciphylline (Standard)

Publications Citing Use of MedChemExpress (MCE) Ezatiostat hydrochloride

Biological Activity

Chemical Information

Publications (8)

순도&문서

References

Calculators

Help & FAQs

Bioz

Ezatiostat hydrochloride

Ezatiostat

GSTO1-IN-1

TLK117

GSTO-IN-2

LAS17

Seneciphylline

Seneciphylline (Standard)

Publications Citing Use of MedChemExpress (MCE) Ezatiostat hydrochloride

Biological Activity

Chemical Information

Publications (8)

순도&문서

References

Calculators

Help & FAQs

Ezatiostat hydrochloride Related Classifications

HY-13634 Related Classifications

Bioz