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- Potent Smoothened (Smo) receptor agonist
- Binds directly to Smo and antagonizes Cyclopamine
- Enhancer of neuronal differentiation of iPSCs into dopaminergic neurons
Smoothened (Smo) is a transmembrane receptor that relays the Hedgehog (Hh) signal and plays an essential role during embryonic development and tumorigenesis. SAG is a potent cell-permeable benzothiophene compound that modulates the coupling of Smo with its downstream effector by interacting with the Smo heptahelical domain (KD = 59 nM). SAG was shown to induce Hedgehog pathway activation independently of the Hh binding receptor Patched (Ptch) (EC50= ~3 nM in NIH 3T3-derived Shh-LIGHT2 cells) and counteract inhibition of Smo by Cyclopamine (Prod. No. BML-GR334). Smo is reported to act as an activator at low concentrations and as an inhibitor at very high concentrations.
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| Regulatory Status |
RUO – Research Use Only |
|---|
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