Purmorphamine
Catalog No.S3042
Molecular Weight(MW): 520.62
Purmorphamine, 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.
5 Customer Reviews
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a-d) LoVo cells were separately or simultaneously treated with 1 μM purmorphamine and 1 μM thiostrepton for the indicated time. a The Gli1, FoxM1, and CCNB1 protein expression levels were examined by immunoblotting after drug treatment for 48 h. b Cell viability was detected after 6 days using an MTT assay. c LoVo cells treated with indicated drugs were cultured for 2 weeks, and outgrowth colonies were stained with crystal violet. d The matched colony count of (c). Error bars represent the mean and S.D. of three independent experiments. **, p < 0.01.
J Exp Clin Cancer Res, 2017, 36(1):23. Purmorphamine purchased from Selleck.
Immunoblotting analysis illustrating that SMO agonist Purmorphamine (PUR) activated SMO expression in A549 and H1299 cells
Sci Rep, 2017, 7(1):1899. Purmorphamine purchased from Selleck.
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Western blot analysis of lung CSC markers. Data are expressed as mean ± SD of three independent experiments. * P < 0.05, ** P < 0.01 compared with control group. # P < 0.05 compared with 20-μM curcumin group.
Phytother Res, 2017, 31(4):680-688. Purmorphamine purchased from Selleck.
In the thalamus, the expression of NR2B was significantly decreased after PUR administration, which the lowest level was detected on day 14. Moreover, the expression of GABAA‐α1 was significantly increased after PUR administration, which the highest level was detected on day 1 (*P < 0.05, **P < 0.01 vs. CCI + V rats).
IUBMB Life, 2018, 70(2):143-152. Purmorphamine purchased from Selleck.
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(C) mRNA levels of Nek2A in purmorphamine treated H4 cells. Total mRNA was extracted and quantified by real-time PCR. Error bars represent the standard deviation of three independent experiments. **P<0.01 compared with the control groups.
Int J Oncol, 2016, doi: 10.3892/ijo.2016.3819. . Purmorphamine purchased from Selleck.
Purity & Quality Control
Choose Selective Hedgehog/Smoothened Inhibitors
Biological Activity
| Description | Purmorphamine, 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. | ||||||||||||||||||||||||||||||
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| 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] |
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| Cell Data |
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| In vivo | Purmorphamine up-regulates ALP expression in human mesenchymal stem cell-based constructs on rats. [4] |
Protocol
| Kinase Assay:[1] |
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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 SmoCRD (deletion of amino acids 68 to 182), and SmoCT (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's protocols. Two days after transfection, the HEK 293T cells are incubated with DMEM containing 0.5% bovine calf serum, 5 nM BODIPY-cyclopamine, and varying concentrations of Purmorphamine (0, 1.5, or 5 M) (1 mL/well) for 1 h at 37 ℃. The Smo-overexpressing cells are then washed with 1 × PBS buffer (1 mL/well), mounted with DAPI-containing medium, and visualized using a Leica DM4500B fluorescence microscope. For binding assays using fixed cells, the Smo-overexpressing HEK 293T cells are fixed with 3% paraformaldehyde in 1 × PBS buffer for 10 min at room temperature (1 mL/well), treated with 1 × PBS containing 10 mM glycine and 0.2% sodium azide for 5 min (1 mL/well), washed with 1 × PBS buffer (1 mL/well), and treated with the Purmorphamine-containing media described above for 4 h at room temperature. |
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| Cell Research:[2] |
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Solubility (25°C)
| In vitro | DMSO | 4 mg/mL warmed (7.68 mM) |
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| Water | Insoluble | |
| Ethanol | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 2% DMSO+30% PEG 300+5% Tween 80+ddH2O For best results, use promptly after mixing. |
1mg/mL |
* 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.
Chemical Information
| Molecular Weight | 520.62 |
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| Formula | C31H32N6O2 |
| CAS No. | 483367-10-8 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
Bio Calculators
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