Purmorphamine

製品コードS3042 バッチS304202

印刷

化学情報

Chemical Structure Synonyms Shh Signaling Antagonist VI Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C31H32N6O2
分子量 520.62 CAS No. 483367-10-8
Solubility (25°C)* 体外 DMSO 50 mg/mL (96.03 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Purmorphamine (Shhシグナル伝達アンタゴニストVI) は、Smoothenedに直接結合して活性化し、HEK293T細胞においてBODIPY-シクロパミンとSmoの結合をIC50 ~ 1.5 μMで阻害し、また、EC50 1 μMで骨芽細胞分化誘導剤でもあります。Purmorphamineは、基礎および誘導されたオートファジーの両方を減少させることができます。
in vitro

Purmorphamine activates the Hedgehog pathway by directly binds and activates Smoothened with IC50 of ~ 1.5 μM in compete with cyclopamine, a Smo antagonist.

This compound is a potent inducer of osteogenesis in multipotent C3H10T1/2 cells. The EC50 (based on ALP expression) for this chemical is 1 μM in C3H10T1/2 cells. It (1 μM) and BMP-4 (100 ng/mL) together increase ALP activity more than 90-fold in 3T3-L1 cells.

In contrast to BMP-4, this compound induces osteogenesis by activating Hedgehog signaling in multipotent mesenchymal progenitor cells.

in vivo

Purmorphamine up-regulates ALP expression in human mesenchymal stem cell-based constructs on rats.

プロトコル(参考用のみ)

キナーゼアッセイ Binding assay
Smo binding assays are conducted with BODIPY-cyclopamine and Smo-overexpressing cells as previously described4,5, using CMV promoter-based, SV40 origin-containing expression constructs for Smo-Myc3, the deletion mutant SmoCRD (deletion of amino acids 68 to 182), and SmoCT (deletion of amino acids 556 to 793). HEK 293T cells are grown on poly-D-lysine-treated glass coverslips in 12-well plates until 70% confluency and then transfected with the appropriate expression construct (0.5 g/well) using FuGene 6 according the manufacturer
細胞アッセイ 細胞株 C3H10T1/2 cell
濃度 0.5-10 μM
反応時間 4 days
実験の流れ

C3H10T1/2 cells are expanded in T175 flasks; cells at 13th passage are detached by trypsin/EDTA and diluted in the growth media. The resulting cell suspension is then plated into black clear bottom 384-well plates with 2500 cells/well in 100 µL growth medium using a Multi-dropTM liquid delivery system. After overnight incubation, cells attached to the bottom of the wells. A stock solution of each Purmorphamine in DMSO (500 nL) is delivered into corresponding well using a Mini TrakTM multiposition dispenser system to make a final concentration of 5μM of this compound. Cells are then incubated at 37 ℃ with 5% CO2 in air atmosphere. After 4 days, the medium is removed and 10 µL of passive lysis buffer is added into each well. After 5 min, 10 µL of alkaline phosphatase substrate solution is added to each well. After incubating 15 min at room temperature, the plates are read on an Acquest high-throughput plate reader following the manufacturer's protocol.
動物実験 動物モデル Male C57BL/6J mouse pups
投薬量 10 mg/kg
投与方法 i.p.

参考

  • http://www.ncbi.nlm.nih.gov/pubmed?term=16408088
  • https://pubmed.ncbi.nlm.nih.gov/12465946/
  • http://www.ncbi.nlm.nih.gov/pubmed?term=15380183
  • http://www.ncbi.nlm.nih.gov/pubmed?term=23228449
  • https://pubmed.ncbi.nlm.nih.gov/32194421/

カスタマーフィードバック

Data from [Data independently produced by , , J Exp Clin Cancer Res, 2017, 36(1):23]

Data from [Data independently produced by , , Sci Rep, 2017, 7(1):1899]

Data from [Data independently produced by , , Phytother Res, 2017, 31(4):680-688]

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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