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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 2024/12/15 19:35:19
327036-89-5 結(jié)構(gòu)式 327036-89-5 結(jié)構(gòu)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 01139
TDZD-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(xué)性質(zhì)

熔點(diǎn)63-64.4 °C
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

安全數(shù)據(jù)

危險(xiǎn)性符號(GHS)GHS hazard pictograms
GHS08
警示詞危險(xiǎn)
危險(xiǎn)性描述H334
防范說明P261-P342+P311
危險(xiǎn)品標(biāo)志Xi
危險(xiǎn)類別碼43
安全說明36/37
WGK Germany3
WGK Germany3
海關(guān)編碼2934999090

應(yīng)用領(lǐng)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(jià)格(試劑級)
報(bào)價(jià)日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價(jià)格
2024/11/08B44364-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
2024/11/08S29264-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE
TDZD-8
327036-89-55mg1181.41元
2024/11/08B44364-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
327036-89-525mg620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(diǎn)
TargetValue
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(jié)合。在激酶實(shí)驗(yàn)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(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。

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.

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