| 货号 | 16248-1mg |
| 描述 | Glutathione S-transferases (GSTs) are ubiquitous multifunctional enzymes that play key roles in cellular detoxification and signal transduction by conjugating target substrates to glutathione. GSTP1-1, the most prevalent GST isozyme in nonhepatic tissues, binds to and inhibits the stress-activated c-Jun N-terminal kinase (JNK), an important regulator of cell proliferation, differentiation, and apoptosis.1 GSTP1-1 is overexpressed in many cancers and has been linked to drug resistance.2 Ezatiostat is a tripeptide analog of glutathione that can selectively inhibit GSTP1-1 catalytic activity (Ki = 400 nM) with minimal effect on the related GSTα and -µ families (Kis range from 20-75 µM).1 After intracellular de-esterification, the active form of ezatiostat, TLK117, binds to and inhibits GSTP1-1, restoring JNK-mediated cellular proliferation and differentiation signaling pathways.2,3,4 Ezatiostat has been shown to stimulate the proliferation of myeloid precursors in preclinical models and is under clinical examination for its potential prevention of myelosuppression in myelodysplastic syndrome.3,4 |
| 别名 | Terrapin 199;TLK199; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Ruscoe, J.E.,Rosario, L.A.,Wang, T., et al. Pharmacologic or genetic manipulation of glutathione S-transferase P1-1 (GSTπ) influences cell proliferation pathways. Journal of Pharmacology and Experimental Therapeutics 298(1), 339-345 (2001). 2.OBrien, M.L.,Vulevic, B.,Freer, S., et al. Glutathione peptidomimetic drug modulator of multidrug resistance-associated protein. Journal of Pharmacology and Experimental Therapeutics 291(3), 1348-1355 (1999). 3.Raza, A.,Galili, N.,Smith, S., et al. Phase 1 multicenter dose-escalation study of ezatiostat hydrochloride (TLK199 tablets), a novel glutathione analog prodrug, in patients with myelodysplastic syndrome. Blood 113(26), 6533-6540 (2009). 4.Raza, A.,Galili, N.,Callander, N., et al. Phase 1-2a multicenter dose-escalation study of ezatiostat hydrochloride liposomes for injection (Telintra(R), TLK199), a novel glutathione analog prodrug in patients with myelodysplastic syndrome. J.Hematol.Oncol. 2, 1-12 (2009). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 529.7 |
| 分子式 | C27H35N3O6S |
| CAS号 | 168682-53-9 |
| 稳定性 | ≥ 2 years |
| 本官网所有报价均为常温或者蓝冰运输价格，如有产品需要干冰运输，需另外加收干冰运输费。 |