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729-46-4

中文名稱 4,4'-(dithiodicarbonothioyl)dimorpholine
英文名稱 4,4'-(dithiodicarbonothioyl)dimorpholine
CAS 729-46-4
分子式 C10H16N2O2S4
分子量 324.51
MOL 文件 729-46-4.mol
更新日期 2025/01/06 14:51:03
729-46-4 結(jié)構(gòu)式 729-46-4 結(jié)構(gòu)式

基本信息

中文別名
化合物JX06
英文別名
JX 06
Bis(morpholinothiocarbonyl) disulfide
Bis(morpholinocarbonothioyl) persulfide
4,4'-(dithiodicarbonothioyl)dimorpholine
Morpholine, 4,4-(dithiodicarbonothioyl)bis-

物理化學(xué)性質(zhì)

熔點(diǎn)136-137 °C
沸點(diǎn)466.3±55.0 °C(Predicted)
密度1.4302 (rough estimate)
折射率1.5650 (estimate)
儲存條件-20°C儲存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)0.58±0.20(Predicted)
形態(tài)固體
顏色White to off-white
4,4'-(dithiodicarbonothioyl)dimorpholine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
2024/11/08HY-195644,4'-(dithiodicarbonothioyl)dimorpholine
JX06
729-46-45mg500元
2024/11/08HY-195644,4'-(dithiodicarbonothioyl)dimorpholine
JX06
729-46-410mM * 1mLin DMSO550元
2024/11/08HY-195644,4'-(dithiodicarbonothioyl)dimorpholine
JX06
729-46-410mg800元

常見問題列表

生物活性
JX06 是一種細(xì)胞中的 PDK1 的選擇性共價(jià)抑制劑。JX06 可劑量依賴性地抑制PDK1、PDK2和PDK3,對應(yīng)的IC50值分別為0.049 μM、0.101 μM 和 0.313 μM。
靶點(diǎn)
TargetValue
PDK1
(Cell-free assay)
0.049 μM
PDK2
(Cell-free assay)
0.101 μM
PDK3
(Cell-free assay)
0.313 μM
體外研究

JX06 barely shows inhibitory activity against PDK4 at a concentration of 10 μM.
JX06 (1-10 μM; 48 hours) induces cell apoptosis in cancer cells with high ECAR/OCR.
JX06 (0-0.6 μM; 72 hours) dose-dependently suppresses the growth of A549 cells.
JX06 (0.1-10 μM; 6-24 hours) inhibits PDHA1 phosphorylation in A549 cells in a time- and dose-dependent manner.
JX06 (1-10 μM) increases glucose uptake and intracellular ATP level and reduces aerobic glycolysis determined by the lactate production in A549 cells.
JX06 (1-10 μM; 24 hours) induces ROS generation in cancer cells with high extracellular acidification rate (ECAR)/ oxygen consumption rate (OCR) .

Apoptosis Analysis

Cell Line: A549, EBC-1, HT-29 and H460 cells
Concentration: 0, 1, 3, 10 μM
Incubation Time: 48 hours
Result: Induces cell apoptosis in A549 and EBC-1 cells.

Cell Viability Assay

Cell Line: A549 cells
Concentration: 0, 0.2, 0.4, 0.6 μM
Incubation Time: 72 hours
Result: Inhibits the viability of A549 cells in a dose dependent manner.

Western Blot Analysis

Cell Line: A549 cells
Concentration: 0, 0.1, 0.3, 1, 3, 10 μM
Incubation Time: 0, 6, 12, 24 hours
Result: Decreased PDHA1 phosphorylation at both serine 293 and serine 232 (S293 and S232) in a time- and dose-dependent manner.
體內(nèi)研究

JX06 (40-80?mg/kg; i.p. for 21 days) inhibits tumor growth in vivo.

Animal Model: A549 subcutaneous xenograft mice
Dosage: 40, 80?mg/kg
Administration: I.p. injections for 21 days
Result: Reduced tumor weights and 67.5% tumor volume at the dose of 80 mg/kg compared with the vehicle control.
Well tolerated at the administration dose.
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