4-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE

4-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE

中文名称4-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE
中文同义词4-苄基-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;4-苯甲基-2-甲基-1,2,4-噻二唑烷-3,5-二酮 100MG;4-苄基-2-甲基-1;化合物TDZD8;TDZD-8,GSK-3Β抑制剂;GSK-3Β INHIBITOR I CALBIOCHEM
英文名称4-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE
英文同义词GSK-3InhibitorI,TDZD-8;NP 01139;1,2,4-Thiadiazolidine-3,5-dione,2-Methyl-4-(phenylMethyl)-;TDZD-8/TDZD8;4-Benzyl-2-methyl-[1,2,4]thiadiazolidine-3,5-dione TDZD-8;TDZD-8, >=98%;TDZD-8;TDZD 8;TDZD8;NP 01139;2-Methyl-4-(phenylmethyl)-1,2,4-thiadiazolidine-3,5-dione
CAS号327036-89-5
分子式C10H10N2O2S
分子量222.26
EINECS号
相关类别小分子抑制剂,天然产物;Amines;Aromatics;Sulfur & Selenium Compounds;Other Enzyme Inhibitors and Activators.;Inhibitors;Akt;mTOR;PI3K
Mol文件327036-89-5.mol
结构式4-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE 结构式

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

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。
TargetValue
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.

用途 

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).

安全信息

危险品标志Xi
危险类别码43
安全说明36/37
WGK Germany3
海关编码2934999090

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/01/16B44364-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
327036-89-55mg160元
2024/01/16S29264-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE
TDZD-8
327036-89-55mg1181.41元

4-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE 上下游产品信息

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