327036-89-5
中文名稱
4-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE
英文名稱
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
2025/03/21 11:17:12
327036-89-5 結構式
基本信息
中文別名
4-芐基-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
英文別名
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
所屬類別
生物化工：GSK-3 抑制劑物理化學性質(zhì)
熔點63-64.4 °C
熔點63-64.4 °C
沸點335.5±35.0 °C(Predicted)
密度1.375±0.06 g/cm3(Predicted)
儲存條件2-8°C
儲存條件2-8°C
溶解度DMSO: 18 mg/mL
溶解度二甲基亞砜：18 毫克/毫升
酸度系數(shù)(pKa)-2.08±0.20(Predicted)
形態(tài)needles
顏色white
應用領域
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-苯甲基-2-甲基-1,2,4-噻二唑烷-3,5-二酮價格(試劑級)
| 報價日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
| 2025/02/05 | 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 |
| 2025/02/05 | S2926 | 4-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE TDZD-8 | 327036-89-5 | 5mg | 1181.41元 |
| 2025/02/05 | 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 |
常見問題列表
生物活性
TDZD-8 (NP 01139) 是一種非ATP競爭性GSK-3β抑制劑，IC50為2 μM；對CDK1， casein kinase II， PKA和PKC具有最低限度的抑制效果。靶點
| Target | Value |
| GSK-3β | 2 μM |
體外研究
TDZD-8作為非ATP競爭性抑制劑或與GS-1結合。在激酶實驗中，TDZD-8對PKA, PKC, Cdk-1/cyclin B 和 CK-II 沒有抑制效果。 TDZD-8特異性誘導原代白血病細胞樣本發(fā)生細胞死亡。TDZD-8可以除去白血病祖細胞和干細胞。TDZD-8誘導細胞死亡，具有極其迅速的細胞死亡動力學，且細胞膜完全喪失。TDZD-8作用于原代AML細胞樣本，抑制PKC和 FLT3。
體內(nèi)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.