Purmorphamine

製品コードS3042 バッチS304201

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 4 mg/mL warmed with 50ºC water bath (7.68 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 Signaling Antagonist VI), which directly binds and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM in HEK293T cell and also is an inducer of osteoblast differentiation with EC50 of 1 μM. Purmorphamine can reduce both basal and induced autophagy.
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. [1]

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

In contrast to BMP-4, Purmorphamine induces osteogenesis by activating Hedgehog signaling in multipotent mesenchymal progenitor cells. [3]
in vivo

Purmorphamine up-regulates ALP expression in human mesenchymal stem cell-based constructs on rats. [4]

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 Purmorphamine. 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.

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]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Phosphorylation of human glioma-associated oncogene 1 on Ser937 regulates Sonic Hedgehog signaling in medulloblastoma [ Nat Commun, 2024, 15(1):987] PubMed: 38307877
Sonic hedgehog restrains the ubiquitin-dependent degradation of SP1 to inhibit neuronal/glial senescence associated phenotypes in chemotherapy-induced peripheral neuropathy via the TRIM25-CXCL13 axis [ J Adv Res, 2024, S2090-1232(24)00106-1] PubMed: 38479571
The MORC2 p.S87L mutation reduces proliferation of pluripotent stem cells derived from a patient with the spinal muscular atrophy-like phenotype by inhibiting proliferation-related signaling pathways [ Neural Regen Res, 2024, 19(1):205-211] PubMed: 37488868
Host-to-graft propagation of inoculated α-synuclein into transplanted human induced pluripotent stem cell-derived midbrain dopaminergic neurons [ Regen Ther, 2024, 25:229-237] PubMed: 38283940
Human osteoarthritic chondrocytes up-regulate the expression of osteoprotegerin in osteoblasts via the Indian hedgehog signaling pathway [ Chinese Journal of Tissue Engineering Research, 2024, Vol. 28 ›› Issue (26): 4194-4201.] PubMed: none
Transplantation of neural stem progenitor cells from different sources for severe spinal cord injury repair in rat [ Bioact Mater, 2023, 23:300-313] PubMed: 36439085
Selective induction of human renal interstitial progenitor-like cell lineages from iPSCs reveals development of mesangial and EPO-producing cells [ Cell Rep, 2023, S2211-1247(23)01614-5] PubMed: 38237600
Small Molecule Cocktails Promote Fibroblast-to-Leydig-like Cell Conversion for Hypogonadism Therapy [ Pharmaceutics, 2023, 10.3390/pharmaceutics15102456] PubMed: 37896216
An engineered Sox17 induces somatic to neural stem cell fate transitions independently from pluripotency reprogramming [ Sci Adv, 2023, 9(34):eadh2501] PubMed: 37611093
An engineered Sox17 induces somatic to neural stem cell fate transitions independently from pluripotency reprogramming [ Sci Adv, 2023, 9(34):eadh2501] PubMed: 37611093

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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