327036-89-5
中文名称
4-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE
英文名称
4-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE
CAS
327036-89-5
分子式
C10H10N2O2S1
分子量
222.26
MOL 文件
327036-89-5.mol
更新日期
2024/09/09 11:34:01
327036-89-5 结构式
基本信息
中文别名
4-苄基-2-甲基-1,2,4-噻二唑烷-3,5-二酮TDZD-8
TDZD 8
TDZD8
NP 01139
4-苯甲基-2-甲基-1,2,4-噻二唑烷-3,5-二酮
4-苯甲基-2-甲基-1,2,4-噻二唑烷-3,5-二酮 100MG
英文别名
NP 01139TDZD-8/TDZD8
TDZD-8, >=98%
GSK-3InhibitorI,TDZD-8
1,2,4-Thiadiazolidine-3,5-dione,2-Methyl-4-(phenylMethyl)-
4-Benzyl-2-methyl-[1,2,4]thiadiazolidine-3,5-dione TDZD-8
所属类别
生物化工：GSK-3 抑制剂物理化学性质
熔点63-64.4 °C
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
储存条件2-8°C
溶解度DMSO: 18 mg/mL
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needles
颜色white
应用领域
用途1
Glycogen Synthase Kinase-3脽 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-3脽 ( IC50 =2nM). Binds to the active site of GSK-3脽. 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)
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2024/08/19 | B4436 | 4-苯甲基-2-甲基-1,2,4-噻二唑烷-3,5-二酮 4-Benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione | 327036-89-5 | 5mg | 160元 |
| 2024/08/19 | S2926 | 4-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE TDZD-8 | 327036-89-5 | 5mg | 1181.41元 |
| 2024/08/19 | B4436 | 4-苯甲基-2-甲基-1,2,4-噻二唑烷-3,5-二酮 4-Benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione | 327036-89-5 | 25mg | 620元 |
常见问题列表
生物活性
TDZD-8 (NP 01139) 是一种非ATP竞争性GSK-3β抑制剂，IC50为2 μM；对CDK1， casein kinase II， PKA和PKC具有最低限度的抑制效果。靶点
| Target | Value |
| GSK-3β | 2 μM |
体外研究
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。
体内研究
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.