Cat. No. Name Size Price Add Cart
KI3740Purmorphamine5 mg$250
Purmorphamine25 mg$800

Chemical Characteristic

Product NamePurmorphamine
CAS No.483367-10-8
Molecular Weight 520.62
FormulaC31H32N6O2
Chemical Name9-Cyclohexyl-N-[4-(4-morpholinyl)phenyl]-2-(1-naphthalenyloxy)-9H-purin-6-amine
Smilesn1cn(c2nc(nc(c12)Nc1ccc(cc1)N1CCOCC1)Oc1cccc2ccccc12)C1CCCCC1
Chemical Structure

Biological activities

Purmorphamine, which directly binds to and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 ?M. It also is an inducer of osteoblast differentiation with EC50 of 1 ?M [1]. It is a Hedgehog agonist. Purmorphamine directly binds to and activates the 7-transmembrane Smo receptor of the Hedgehog signaling pathway. Hedgehog agonist Purmorphamine most significantly increased the neuronal differentiation of a human striatal NSC line (STROC05). Purmorphamine up-regulated gene expression of the mediators of Hh pathway, SMO, PTCH1, GLI1, and GLI2. The activation of Hh pathway by Purmorphamine increased the expression of several genes. Purmorphamine triggers Hh signaling pathway in hMSCs, inducing an increase in the expression of a set of genes involved in the osteoblast differentiation program [2]. In vitro, it can be used by 1 ?M in 3T3-L1 cells [3].

References

[1] F. Faghihia, M. Baghaban Eslaminejada, A. Nekookara, et al. The effect of purmorphamine and sirolimus on osteogenic differentiation of human bone marrow-derived mesenchymal stem cells. Biomedicine & Pharmacotherapy. 2013, 67(1): 31-38.
[2] Gran?li C, Karlsson C, Lindahl A, et al. Virtual ligand-based screening reveals purmorphamine analogs with the capacity to induce the osteogenic differentiation of human mesenchymal stem cells. Cells Tissues Organs. 2013,197(2):89-102.
[3] Gu D, Fan Q, Zhang X, et al. A role for transcription factor STAT3 signaling in oncogene smoothened-driven carcinogenesis. J Biol Chem. 2012,287(45):38356-38366.

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