الصفحة الرئيسية>>Signaling Pathways>> Stem Cell>> Smoothened>>Purmorphamine

Purmorphamine

رقم الكتالوجGC15064

Purmorphamine is the first small molecule agonist developed for Smoothened protein.

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Purmorphamine التركيب الكيميائي

Cas No.: 483367-10-8

الحجم السعر المخزون الكميّة
5mg
69٫00
متوفر
10mM (in 1mL DMSO)
84٫00
متوفر
25mg
230٫00
متوفر
125mg
1648٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 1 publications

Description of Purmorphamine

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 of Purmorphamine

Kinase experiment[1]:

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.

Reaction Conditions

0, 1.5, or 5μM Purmorphamine

Applications

Purmorphamine directly binds and activates Smoothened, blocking BODIPY-cyclopamine binding to Smo, with an IC50 of about 1.5 μM in HEK293T cells.

Cell experiment [2]:

Cell lines

C3H10T1/2 cells

Preparation method

Cells were treated with 2 μM of purmorphamine or 0.5% DMSO control for 4 days.

Reaction Conditions

2 μM purmorphamine;4 days

Applications

Purmorphamine induces osteogenesis in pluripotent mesenchymal progenitor cells.

Animal experiment [3]:

Animal models

Male C57BL/6J mouse ( HI injury)

Dosage form

10 mg/kg purmorphamine, i.p.

Applications

Purmorphamine prevents Hypoxic-Ischemic(HI)-induced brain injury.

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.

Chemical Properties of Purmorphamine

Cas No. 483367-10-8 SDF
Chemical Name 9-cyclohexyl-N-(4-morpholin-4-ylphenyl)-2-naphthalen-1-yloxypurin-6-amine
Canonical SMILES C1CCC(CC1)N2C=NC3=C2N=C(N=C3NC4=CC=C(C=C4)N5CCOCC5)OC6=CC=CC7=CC=CC=C76
Formula C31H32N6O2 M.Wt 520.62
الذوبان ≥ 8.7mg/mL in DMSO, ≥ 1.82 mg/mL in EtOH with ultrasonic Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Purmorphamine

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.9208 mL 9.6039 mL 19.2079 mL
5 mM 0.3842 mL 1.9208 mL 3.8416 mL
10 mM 0.1921 mL 0.9604 mL 1.9208 mL
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Product Documents

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Quality Control

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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