4-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE
4-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE
4-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE 性质
| 熔点 | 63-64.4 °C |
|---|---|
| 沸点 | 335.5±35.0 °C(Predicted) |
| 密度 | 1.375±0.06 g/cm3(Predicted) |
| 储存条件 | 2-8°C |
| 溶解度 | 二甲基亚砜：18 毫克/毫升 |
| 酸度系数(pKa) | -2.08±0.20(Predicted) |
| 形态 | 针状固体 |
| 颜色 | 白色 |
4-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE 用途与合成方法
| Target | Value |
| GSK-3β | 2 μM |
TDZD-8作为非ATP竞争性抑制剂或与GS-1结合。在激酶实验中，TDZD-8对PKA, PKC, Cdk-1/cyclin B 和 CK-II 没有抑制效果。 TDZD-8特异性诱导原代白血病细胞样本发生细胞死亡。TDZD-8可以除去白血病祖细胞和干细胞。TDZD-8诱导细胞死亡，具有极其迅速的细胞死亡动力学，且细胞膜完全丧失。TDZD-8作用于原代AML细胞样本，抑制PKC和 FLT3。
TDZD-8 (TDZD8, 1 or 2 mg/kg, i.p.) both reduces the induction of p-DARPP32 following chronic L-dopa treatment in parkinsonian animals. TDZD8 treatment of 21 days induces a significant reduction in PKA expression in rats with established dyskinesia. Moreover, TDZD8 reduces FosB mRNA level in the striatum and lowers the expression of PPEB mRNA to similar levels as in 6-OHDA-lesioned rats without treated with L-dopa. The decrease in dyskinesia induced by TDZD8 is overcome by dopamine rceptor-1 agonist.
Glycogen Synthase Kinase-3β is a highly conserved ubiquitously expressed serine/threonine protein kinase involved in signal transduction cascades of multiple cellular processes. TDZD-8 is a thiadiazo lidinone (TDZD) analogue that acts as a highly selective, non-ATP competitive inhibitor of GSK-3β ( IC50 =2nM). Binds to the active site of GSK-3β. Does not significantly affect the activities of Cd k-1/cyclin B, CK-II, PKA, and PKC (IC50 >100nM).
4-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024-01-16 | B4436 | 4-苯甲基-2-甲基-1,2,4-噻二唑烷-3,5-二酮 | 327036-89-5 | 5mg | 160 |
| 2024-01-16 | S2926 | 4-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE | 327036-89-5 | 5mg | 1181.41 |
