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Midkine Inhibitor, iMDK-Calbiochem
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别名
Midkine Inhibitor, iMDK-Calbiochem
3-(2-(4-Fluorobenzyl)imidazo[2,1-b]thiazol-6-yl)-2H-chromen-2-one, 3-(2-(4-Fluorobenzyl)imidazo[2,1-b][1,3]thiazol-6-yl)-2H-chromen-2-one, MDK Expression Inhibitor
基本信息
Empirical Formula【经验(实验)分子式】 | C21H13FN2O2S |
Molecular weight | 376.40 |
General description【一般描述】 | A cell-permeable imidazothiazolyl-chromenone compound that reduces cellular midkine/MDK protein level in H441 lung adenocarcinoma cells in a dose-dependent manner (by >90% in 48 h at 25 nM) via a yet unidentified mechanism. Shown to inhibit the viability of MDK-positive HEK293, H441, and H520 cells (by ≥60% at 500 nM in 48 h), but not MDK-negative NHLF or HEK293 (by <15% at 500 nM in 48 h), via apoptosis induction as a result of PI 3-K/AKT signaling inhibition. Intraperitoneal injection is reported to be efficacious in retarding H441 tumor expansion in mice (9 mg/kg; 3X to 5X per wk) in vivo. A cell-permeable imidazothiazolyl-chromenone compound that reduces cellular midkine/MDK protein level in H441 lung adenocarcinoma cells in a dose-dependent manner (by >90% in 48 h at 25 nM) via a yet unidentified mechanism, while exhibiting little effect toward cellular level of PTN or VEGF. Shown to inhibit the viability of MDK-positive HEK293, H441, and H520 cells (by ≥60% at 500 nM in 48 h), but not MDK-negative NHLF (normal human lung fibroblast) or HEK293 (by <15% at 500 nM in 48 h), via apoptosis induction as a result of PI 3-K/AKT signaling, but not Erk or p38, pathway inhibition. Intraperitoneal injection is reported to be efficacious in retarding H441 tumor expansion in mice (75% vs 400% increase in tumor volume in 10 d with or without treatment; 3 to 5 times 9 mg/kg i.p. dosing per wk) in vivo. |
Biochem/physiol Actions【生化/生理作用】 | Cell permeable: yes Primary Target Midkine Reversible: yes |
Warning【警告】 | Toxicity: Standard Handling (A) |
Reconstitution【重悬】 | Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C. |
Other Notes【其他说明】 | Hao, H., et al. 2013. PLoS ONE8, e71093. |
Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
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性质
Quality Level【质量水平】 | 100 |
Assay【测定】 | ≥98% (HPLC) |
form【形式】 | solid |
manufacturer/tradename | Calbiochem® |
storage condition【储存条件】 | OK to freeze protect from light |
color【颜色】 | off-white |
solubility【溶解性】 | DMSO: 5 mg/mL |
storage temp.【储存温度】 | 2-8℃ |
packaging【包装】 | Packaged under inert gas |
安全信息
Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
WGK | WGK 3 |