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SAGHh and Smo agonist

SAG

Catalog No. B5837
Size Price Stock Qty
2mg $85.00 In stock
5mg $175.00 In stock
25mg $525.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

SAG

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Chemical Properties

Cas No. 912545-86-9 SDF Download SDF
Chemical Name 3-chloro-N-((1r,4r)-4-(methylamino)cyclohexyl)-N-(3-(pyridin-4-yl)benzyl)benzo[b]thiophene-2-carboxamide
Canonical SMILES CN[C@@]1([H])CC[C@@](N(C(C2=C(Cl)C3=CC=CC=C3S2)=O)CC4=CC(C5=CC=NC=C5)=CC=C4)([H])CC1
Formula C28H28ClN3OS M.Wt 490.06
Solubility Soluble in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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]

References:
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.