Ezatiostat hydrochloride |
| Catalog No.GC13409 |
Ezatiostat 염산염(TER199; TLK199 염산염)은 글루타티온의 트리펩타이드 유사체이며 선택적이고 경구 활성인 글루타티온 S-트랜스퍼라제 P1-1(GSTP1) 억제제입니다. Ezatiostat 염산염은 GSTP1을 억제하여 JNK 활성화를 유도합니다. Ezatiostat 염산염은 림프구 생성과 골수 전구 세포 증식을 모두 자극합니다. Ezatiostat 염산염은 골수이형성 증후군(MDS) 치료의 가능성이 있습니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 286942-97-0
Sample solution is provided at 25 µL, 10mM.
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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.
| Cell experiment [1]: | |
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Cell lines |
TF-1 erythroleukemia and HL-60 promyelocytic cells |
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Preparation method |
The solubility of this compound in DMSO is >28.3mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
40 μM, 5.5 hours |
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Applications |
Treatment with TLK199 in leukemia cell lines resulted in apoptosis and increase in ROS levels. Treatment with TLK199 resulted in cleavage of PARP protein in a dose- and time-dependent manner. In HL-60 cells, TLK199 (40 μM for 5.5 hours) induced activation of caspase 3 and caspase 9. TLK199 led to loss of cell viability. In TF-1 and HL-60 cell lines, TLK199 treatment resulted in the upregulation of several genes involved in the cellular response to ER stress. TLK199 treatment upregulated genes for AP-1 transcription factors such as c-jun. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Stofega M, Hsu S C, Chew J, et al. Induction of apoptosis by TLK199 in human leukemia cells[J]. 2008. | |
| Cas No. | 286942-97-0 | 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 | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7664 mL | 8.8322 mL | 17.6644 mL |
| 5 mM | 0.3533 mL | 1.7664 mL | 3.5329 mL |
| 10 mM | 0.1766 mL | 0.8832 mL | 1.7664 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 28 reference(s) in Google Scholar.)
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