Name: SAG
Price: 426.00 USD

- Overview
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    Background
    
    SAG is a synthetic chlorobenzothiophene-containing Hh pathway agonist that regulates smo activity. It is a SMO agonist at EC50 of 3 nM and but inhibits hedgehog signaling at >1 μM. [1]
    Smoothened (SMO) is a GPCR-like receptor that mediates hedgehog signaling with Patched to regulate gene expression through the Gli transcription factors. It is plays an important role for embryogenesis and adults tissue homeostasis
    In a mouse cultured cell assay (Shh-LIGHT2), SAG induces pathway activation (EC50 ≈3 nM). It differs in that pathway activity decreases dramatically as SAG concentration surpasses 1 μM. [1] SAG binds directly to the SMO heptahelical bundle. SAG dose dependently blocks this association and produces apparent dissociation constant (KD) of 59 nM for the SAG/SMO complex. [2]
    SAG also antagonizes GC’s antiproliferative effects in CGNP P4 wild-type mice primary cultures. At 15-240 nM, SAG prevents the neurotoxic effects of glucocorticoids without interfering with the beneficial effects of glucocorticoids on lung maturation. [2]
    
    1. Chen JK, Taipale J, Young KE et al. Small molecule modulation of Smoothened activity. Proc Natl Acad Sci U S A. 2002 Oct 29;99(22):14071-6.
    2. Heine VM, Griveau A, Chapin C et al. A small-molecule smoothened agonist prevents glucocorticoid-induced neonatal cerebellar injury. Sci Transl Med. 2011 Oct 19;3(105):105ra104.
- Properties
  - Categories
    
    Hh and Smo agonist
    
    Alternative Name
    
    3-chloro-N-((1r,4r)-4-(methylamino)cyclohexyl)-N-(3-(pyridin-4-yl)benzyl)benzo[b]thiophene-2-carboxamide
    
    CAS Number
    
    912545-86-9
    
    Molecular Formula
    
    C28H28ClN3OS
    
    Molecular Weight
    
    490.06
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥24.5 mg/mL in DMSO; ≥16.33 mg/mL in H2O with gentle warming and ultrasonic; ≥2.61 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    CN[[email protected]@]1([H])CC[[email protected]@](N(C(C2=C(Cl)C3=CC=CC=C3S2)=O)CC4=CC(C5=CC=NC=C5)=CC=C4)([H])CC1
    
    * For Research Use Only

Documents

COA (Certificate Of Analysis)

MSDS (Material Safety Data Sheet)

Datasheet

SAG

SAG

Background

Documents

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