Ezatiostat hydrochloride
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Ezatiostat hydrochloride(TLK199)是一种高效的谷胱甘肽S-转移酶(GST)抑制剂[1]。
Ezatiostat hydrochloride(TLK199)是一种新的谷胱甘肽类似物,也是一种潜在的血细胞减少疗法。此外,ezatiostat hydrochloride可以选择性地结合并抑制GST P1-1。由于GST P1-1可以结合并抑制JNK,ezatiostat hydrochloride也可在临床前模型中抑制GST P1-1,激活JNK,并能促进定向造血干细胞的生长和成熟。此外,ezatiostat hydrochloride已被报道可以刺激骨髓前体细胞的增殖。Ezatiostat hydrochloride已被阐明可在人类白血病细胞(HL-60)中引起生长抑制和细胞凋亡,其CC50值为6-17 μM。除此之外,ezatiostat hydrochloride也显示出刺激成熟细胞、粒细胞和红细胞多向分化的能力[1,2]。
参考文献:
[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.
- 1. Zhao S, Wang B, et al. "Contributions of enzymes and gut microbes to biotransformation of perfluorooctane sulfonamide in earthworms (Eisenia fetida)." Chemosphere. 2019 Aug 19;238:124619. PMID:31450114
- 2. Liberti, Eileen. "An In-vitro Investigation of Glutathione Transferases in Idiopathic Pulmonary Fibrosis." George Mason University.2018.
- 3. Faccidomo S, Swaim KS, et al. "Mining the nucleus accumbens proteome for novel targets of alcohol self-administration in male C57BL/6J mice."Psychopharmacology (Berl).2018 Mar 3. PMID:29502276
- 4. 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
Storage | Store at -20°C |
M.Wt | 566.11 |
Cas No. | 286942-97-0 |
Formula | C27H36ClN3O6S |
Solubility | ≥28.3 mg/mL in DMSO; ≥3.32 mg/mL in H2O with ultrasonic; ≥3.4 mg/mL in EtOH with ultrasonic |
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 |
SDF | Download SDF |
Canonical SMILES | CCOC(=O)C(CCC(=O)NC(CSCC1=CC=CC=C1)C(=O)NC(C2=CC=CC=C2)C(=O)OCC)N.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
TF-1红白血病和HL-60早幼粒细胞 |
溶解方法 |
该化合物在DMSO中的溶解度大于28.3 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。 |
反应条件 |
40 μM,5.5小时 |
应用 |
在白血病细胞系中,TLK199引发凋亡和ROS水平升高。TLK199以剂量和时间依赖的方式裂解PARP蛋白。在HL-60细胞中,TLK199(40 μM,5.5小时)最大程度诱导caspase 3和caspase 9的活化。TLK199导致细胞活力丧失。在TF-1和HL-60细胞系中,TLK199引起参与ER应激的基因上调。TLK199上调AP-1转录因子如c-jun的基因表达。 |
注意事项 |
由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。 |
References: [1]. Stofega M, Hsu S C, Chew J, et al. Induction of apoptosis by TLK199 in human leukemia cells[J]. 2008. |
质量控制和MSDS
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