4-苯甲基-2-甲基-1,2,4-噻二唑烷-3,5-二酮
| 中文名稱 | 4-苯甲基-2-甲基-1,2,4-噻二唑烷-3,5-二酮 |
|---|---|
| 中文同義詞 | 4-芐基-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-芐基-2-甲基-1;化合物TDZD8;TDZD-8,GSK-3Β抑制劑;GSK-3Β INHIBITOR I CALBIOCHEM;化合物TDZD8,10 MM DMSO 溶液 |
| 英文名稱 | 4-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE |
| 英文同義詞 | 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號(hào) | 327036-89-5 |
| 分子式 | C10H10N2O2S |
| 分子量 | 222.26 |
| EINECS號(hào) | |
| 相關(guān)類別 | 小分子抑制劑，天然產(chǎn)物;Amines;Aromatics;Sulfur & Selenium Compounds;Other Enzyme Inhibitors and Activators.;Inhibitors;Akt;mTOR;PI3K |
| Mol文件 | 327036-89-5.mol |
| 結(jié)構(gòu)式 |  |
4-苯甲基-2-甲基-1,2,4-噻二唑烷-3,5-二酮 性質(zhì)
| 熔點(diǎn) | 63-64.4 °C |
|---|---|
| 沸點(diǎn) | 335.5±35.0 °C(Predicted) |
| 密度 | 1.375±0.06 g/cm3(Predicted) |
| 儲(chǔ)存條件 | 2-8°C |
| 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) | 針狀固體 |
| 顏色 | 白色 |
| InChI | InChI=1S/C10H10N2O2S/c1-11-9(13)12(10(14)15-11)7-8-5-3-2-4-6-8/h2-6H,7H2,1H3 |
| InChIKey | JDSJDASOXWCHPN-UHFFFAOYSA-N |
| SMILES | S1C(=O)N(CC2=CC=CC=C2)C(=O)N1C |
| Target | Value |
| GSK-3β | 2 μM |
TDZD-8作為非ATP競(jìng)爭(zhēng)性抑制劑或與GS-1結(jié)合。在激酶實(shí)驗(yàn)中，TDZD-8對(duì)PKA, PKC, Cdk-1/cyclin B 和 CK-II 沒有抑制效果。 TDZD-8特異性誘導(dǎo)原代白血病細(xì)胞樣本發(fā)生細(xì)胞死亡。TDZD-8可以除去白血病祖細(xì)胞和干細(xì)胞。TDZD-8誘導(dǎo)細(xì)胞死亡，具有極其迅速的細(xì)胞死亡動(dòng)力學(xué)，且細(xì)胞膜完全喪失。TDZD-8作用于原代AML細(xì)胞樣本，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).
| 更新日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS號(hào) | 包裝 | 價(jià)格 |
|---|---|---|---|---|---|
| 2026/07/06 | S2926 | 4-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE TDZD-8 | 327036-89-5 | 5mg | 1181.41元 |
| 2026/07/06 | S2926 | 4-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE TDZD-8 | 327036-89-5 | 25mg | 3013.59元 |