300833-95-8 Usage
Description
Smoothened (SMO) is a cell surface receptor that, with Patched, mediates hedgehog signaling to regulate gene expression through the Gli transcription factors. GSA 10 is a quinolinecarboxamide derivative that acts as an agonist of SMO. By acting at SMO, GSA 10 has been shown to promote the differentiation of multipotent mesenchymal progenitor cells into osteoblasts (EC50 = 1.2 μM). Most notably, GSA 10 does not recognize the classic cyclopamine binding site as do other SMO agonists and as such has been used to characterize a novel SMO active site.
Uses
GSA 10 is a novel small-molecule positive modulator of smoothened. GSA 10 may have therapeutic interests in regenerative medicine.
Check Digit Verification of cas no
The CAS Registry Mumber 300833-95-8 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 3,0,0,8,3 and 3 respectively; the second part has 2 digits, 9 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 300833-95:
(8*3)+(7*0)+(6*0)+(5*8)+(4*3)+(3*3)+(2*9)+(1*5)=108
108 % 10 = 8
So 300833-95-8 is a valid CAS Registry Number.
300833-95-8Relevant articles and documents
Design, synthesis and biological characterization of a new class of osteogenic (1H)-quinolone derivatives
Manetti, Fabrizio,Petricci, Elena,Gabrielli, Annalisa,Mann, Andrè,Faure, Hélène,Gorojankina, Tatiana,Brasseur, Laurent,Hoch, Lucile,Ruat, Martial,Taddei, Maurizio
, p. 747 - 757 (2016/07/21)
Smoothened (Smo) is the signal transducer of the Hedgehog (Hh) pathway and its stimulation is considered a potential powerful tool in regenerative medicine to treat severe tissue injuries. Starting from GSA-10, a recently reported Hh activator acting on Smo, we have designed and synthesized a new class of quinolone-based compounds. Modification and decoration of three different portions of the original scaffold led to compounds able to induce differentiation of multipotent mesenchymal cells into osteoblasts. The submicromolar activity of several of these new quinolones (0.4–0.9?μM) is comparable to or better than that of SAG and purmorphamine, two reference Smo agonists. Structure-activity relationships allow identification of several molecular determinants important for the activity of these compounds.
