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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.
Midkine Inhibitor, iMDK - CAS 881970-80-5 - Calbiochem 分析证书
标题
批号
508052
参考
参考信息概述
Hao, H., et al. 2013. PLoS ONE8, e71093.
数据表
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
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.
Form
Off-white solid
Intert gas (Yes/No)
Packaged under inert gas
CAS number
881970-80-5
Chemical formula
C₂₁H₁₃FN₂O₂S
Structure formula
Purity
≥98% by HPLC
Solubility
DMSO (5 mg/ml)
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
