product name Smoothened Agonist (SAG)
Description: Smoothened Agonist (SAG) is a potent cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells. SAG potently activates the Hedgehog signaling pathway in Shh-light 2 cells (EC50 ~ 3 nM). SAG induces pathway activation independently of Ptch proteins. The Smoothened receptor (SMO) mediates signal transduction in the hedgehog pathway, which is implicated in normal development and carcinogenesis. SMO antagonists can suppress the growth of some tumors.
References: Proc Natl Acad Sci U S A. 2002 Oct 29;99(22):14071-6; Neurosci Lett. 2010 Sep 27;482(2):81-5.
490.06
Formula
C28H28ClN3OS
CAS No.
912545-86-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 71 mg/mL (134.8 mM)
Water:
Ethanol: 40 mg/mL (75.9 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19426195
| In Vitro |
In vitro activity: SAG regulates Smo activity by binding directly to the Smo heptahelical bundle. SAG induces Smo-dependent signaling through Gli in a GRK2-dependent way. SAG also (1 nM) induces proliferation of neuronal and glial precursors without affecting the differentiation pattern of newly produced cells. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | In the adult rat hippocampus, the intracerebroventricular administration of SAG (2.5 nM) significantly increases the number of newly generated cells and extends survival of hippocampal cells. In mice, SAG (20 μg/g, i.p.) effectively prevents GC-induced neonatal cerebellar developmental abnormalities. |
| Animal model | |
| Formulation & Dosage | |
| References | Proc Natl Acad Sci U S A. 2002 Oct 29;99(22):14071-6; Neurosci Lett. 2010 Sep 27;482(2):81-5. |
