| CAS NO: | 327036-89-5 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 200mg | 电议 |
| 500mg | 电议 |
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 222.26 |
| Cas No. | 327036-89-5 |
| Formula | C10H10N2O2S |
| Solubility | insoluble in H2O; ≥11.1 mg/mL in DMSO; ≥36.45 mg/mL in EtOH with ultrasonic |
| Chemical Name | 4-benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione |
| Canonical SMILES | CN1C(=O)N(C(=O)S1)CC2=CC=CC=C2 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。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。 |
TDZD-8是一种糖原合酶激酶3β(GSK-3β)抑制剂,其IC50值为1.4 μM[1].
TDZD-8是有效的和非ATP竞争性的GSK-3β抑制剂.相对于其它蛋白激酶,包括蛋白激酶A\酪蛋白激酶II和细胞周期蛋白依赖性激酶1(Cdk-1/cyclin B),TDZD-8对GSK-3β具有选择性.然而,TDZD-8也可以抑制蛋白激酶C的PKCβI和PKCδ亚型,相应IC50值为1.4 μM和1.1 μM[1,2].
在细胞实验中,TDZD-8抑制GSK-3β以及PKC,从而降低PDT诱导的神经元坏死和神经胶质细胞凋亡.此外,在多种原代人白血病细胞中,TDZD-8可能由于抑制了PKC和FLT3,从而具有抗白血病活性[3].
参考文献：
[1] Komandirov M A, Knyazeva E A, Fedorenko Y P, et al. On the role of phosphatidylinositol 3-kinase, protein kinase b/Akt, and glycogen synthase kinase-3β in photodynamic injury of crayfish neurons and glial cells. Journal of Molecular Neuroscience, 2011, 45(2): 229-235.
[2] Martinez A, Alonso M, Castro A, et al. First non-ATP competitive glycogen synthase kinase 3 β (GSK-3β) inhibitors: thiadiazolidinones (TDZD) as potential drugs for the treatment of Alzheimer's disease. Journal of medicinal chemistry, 2002, 45(6): 1292-1299.
[3] Guzman M L, Li X, Corbett C A, et al. Rapid and selective death of leukemia stem and progenitor cells induced by the compound 4-benzyl, 2-methyl, 1, 2, 4-thiadiazolidine, 3, 5 dione (TDZD-8). Blood, 2007, 110(13): 4436-4444.
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