Purmorphamine
Products are for research use only. Not for human use. We do not sell to patients.
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $86.00 | In Stock | 1 | |
| 5mg | $70.00 | In Stock | 1 | |
| 25mg | $230.00 | In Stock | 1 | |
| 125mg | $1,648.00 | In Stock | 1 |
Citations
1 publicationsPublications from researchers using this productDescription
Purmorphamine is the first small molecule agonist developed for Smoothened protein. Purmorphamine directly binds and activates Smoothened, blocking the binding of BODIPY-cyclopamine to Smo. Purmorphamine activates the Hedgehog(Hh) signaling pathway, resulting in up-regulation and down-regulation of its downstream target genes, including Gli1 and Patched Purmorphamine can be used to treat bone-related diseases and neurodegenerative diseases[1-2].
Purmorphamine(2 µM;4 days) induces osteogenesis in pluripotent mesenchymal progenitor cells[3]. Purmorphamine enhances osteogenic activity of human osteoblasts derived from bone marrow mesenchymal cells, Purmorphamine(1, 2 or 3 µM;21days) did not affect cell proliferation or viability, but increased ALP activity and bone-like nodule formation[4]. Purmorphamine(2 µM ) had a promotive effect on adhesion, proliferation and osteogenic differentiation of human dental pulp stem cells (hDPSCs) cultured on β-TCP[5]. Purmorphamine substantially suppressed proliferation, enhanced and accelerated alkaline phosphatase activity and calcium sedimentation and increased the expression of osteopontin and osteocalcin in rat mesenchymal stem cells[6].
Purmorphamine(10 mg/kg; i.p.) prevents Hypoxic-Ischemic(HI)-induced brain injury. Purmorphamine exerted long-term protective effects upon tissue loss and improved neurobehavioral outcomes as determined at 14 and 28 days post-HI insult[7].Purmorphamine(1mg/kg; i.p.) activated Sonic hedgehog (SHH) signal to attenuate LPS-induced inflammatory response in mice[8].
Protocol
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Kinase experiment[1]: |
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Preparation method |
Smo binding experiments were performed using BODIPY-Cyclopamine and cells overexpressing Smo. Two days after transfection of HEK 293T cells, the cells were incubated at 37 ℃for 1 hour with DMEM medium containing BODIPY-Cyclopamine and varying concentrations of Purmorphamine (0, 1.5, or 5μM) (1 mL per well). The overexpressed Smo cells were then washed with 1xPBS buffer (1 mL per well), placed in a medium containing DAPI, observed using fluorescence microscopy, and binding detection was performed using fixed cells. Smo-overexpressing HEK293T cells were fixed at room temperature with 3% paraformaldehyde dissolved in 1 xPBS buffer (1 mL per well) for 10 minutes, then treated with 1 xPBS buffer (1 mL per well) containing 10 mm of glycerine and 0.2% sodium azide for 5 minutes with 1 xPBS buffer (1 ml per well). Cells were washed and then treated with a medium containing Purmorphamine at room temperature for 4 hours. |
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Reaction Conditions |
0, 1.5, or 5μM Purmorphamine |
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Applications |
Purmorphamine directly binds and activates Smoothened, blocking BODIPY-cyclopamine binding to Smo, with an IC50 of about 1.5 μM in HEK293T cells. |
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Cell experiment [2]: |
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Cell lines |
C3H10T1/2 cells |
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Preparation method |
Cells were treated with 2 μM of purmorphamine or 0.5% DMSO control for 4 days. |
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Reaction Conditions |
2 μM purmorphamine;4 days |
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Applications |
Purmorphamine induces osteogenesis in pluripotent mesenchymal progenitor cells. |
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Animal experiment [3]: |
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Animal models |
Male C57BL/6J mouse ( HI injury) |
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Dosage form |
10 mg/kg purmorphamine, i.p. |
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Applications |
Purmorphamine prevents Hypoxic-Ischemic(HI)-induced brain injury. |
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References: [1]. Sinha S, Chen JK. Purmorphamine activates the Hedgehog pathway by targeting Smoothened. Nat Chem Biol. 2006 Jan;2(1):29-30. doi: 10.1038/nchembio753. Epub 2005 Nov 20. PMID: 16408088. [2].Wu X, Walker J,et,al. Purmorphamine induces osteogenesis by activation of the hedgehog signaling pathway. Chem Biol. 2004 Sep;11(9):1229-38. doi: 10.1016/j.chembiol.2004.06.010. PMID: 15380183. [3]. Liu D, Bai X, et,al. Purmorphamine Attenuates Neuro-Inflammation and Synaptic Impairments After Hypoxic-Ischemic Injury in Neonatal Mice via Shh Signaling. Front Pharmacol. 2020 Mar 4;11:204. doi: 10.3389/fphar.2020.00204. PMID: 32194421; PMCID: PMC7064623. |
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Product Documents
Biological Data
Chemical Properties
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
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