Smoothened Agonist (SAG) HCl

For research use only.

Catalog No.S7779

22 publications

Smoothened Agonist (SAG) HCl Chemical Structure

CAS No. 2095432-58-7

Smoothened Agonist (SAG) HCl is a cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells.

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Selleck's Smoothened Agonist (SAG) HCl has been cited by 22 publications

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Biological Activity

Description Smoothened Agonist (SAG) HCl is a cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells.
Smoothened [1]
(mouse cultured cell assay)
3 nM(EC50)
In vitro

SAG regulates Smo activity by binding directly to the Smo heptahelical bundle. [1] SAG induces Smo-dependent signaling through Gli in a GRK2-dependent way. [2] SAG also (1 nM) induces proliferation of neuronal and glial precursors without affecting the differentiation pattern of newly produced cells. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
mouse Shh-Light II cell MVXGeY5kfGmxbjDhd5NigQ>? Ml7mOFghcHK| M{TWXWFkfGm4YYTpc44hd2ZiU3joJJBifGi5YYmgbY4hdW:3c3WgV4hpNUyrZ3j0JGlKKGOnbHzzJIF{e2W|c3XkJIF{KGmwZIXjeIlwdiCxZjDncIkyKGW6cILld5Nqd25iYX\0[ZIhPDhiaILzJIJ6KHKnbnnscIEhdHWvaX7ld4NmdmOnIHHzd4F6NCCHQ{WwQVAvODB6ODFOwG0> NIXZc2kzOjl6NUm1PC=>

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
LC3I / LC3II; 

PubMed: 23504944     

Western blotting for LC3I/II. Huh7, Hep3B and HepG2 cells were incubated with vehicle control, SAG (0.5 µM), Pur (10 µM), Shh (0.4 µg/ml), GANT61 (20 µM) or GDC0449 (20 µM) for 48 hours.


PubMed: 25636740     

In the absence of SAG, Smo is not detected at the cilium. MRT-92 alone does not induce Smo trafficking to the primary cilium. Cell exposure to SAG induces Smo trafficking to the cilium, which is abolished by MRT-92.

acetylated alpha tubulin; 

PubMed: 25992706     

TM3 cells were cultured in the presence of the SMO agonist (SAG) to monitor response to HH activation. A) In control cells (a-c; 0 h), primary cilia marked by Ac-T (red; arrows) only displayed occasional, speckled appearance of SMO (green). After 1 h in the presence of 100 nM SAG (d-f), a stronger and more frequent localization of SMO to the primary cilia was observed, now also at the ciliary base (f; insert; arrow), and this was even more apparent after 4 h of SAG-stimulation (g-i). Nuceli were stained with DAPI. Scale bar = 10 μm. 

25636740 25992706
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. [3] In mice, SAG (20 μg/g, i.p.) effectively prevents GC-induced neonatal cerebellar developmental abnormalities. [4]


Animal Research:[3]
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  • Animal Models: Rat
  • Dosages: 2.5 nM
  • Administration: Intracerebroventricular administration
    (Only for Reference)

Solubility (25°C)

In vitro Water 100 mg/mL (189.92 mM)
DMSO 71 mg/mL warmed (134.84 mM)
Ethanol 40 mg/mL warmed (75.97 mM)
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
For best results, use promptly after mixing.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 526.52


CAS No. 2095432-58-7
Storage powder
in solvent
Synonyms N/A
Smiles CNC1CCC(CC1)N(CC2=CC(=CC=C2)C3=CC=NC=C3)C(=O)C4=C(C5=CC=CC=C5S4)Cl.Cl

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03645044 Recruiting -- Hiv|HBV Coinfection University of Melbourne|National Health and Medical Research Council Australia|The University of Western Australia|University of Adelaide|The HIV Netherlands Australia Thailand Research Collaboration|University of Malaya|YR Gaitonde Centre for AIDS Research and Education|Melbourne Health May 24 2018 --
NCT03180619 Active not recruiting Drug: TAF Chronic Hepatitis B Gilead Sciences June 29 2017 Phase 2
NCT02195518 Completed Drug: Tenofovir disoproxil fumarate Hepatitis B Chronic GlaxoSmithKline March 18 2015 Phase 4
NCT02364336 Completed Drug: Peginterferon alfa-2a Chronic Hepatitis B National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|National Institutes of Health Clinical Center (CC) February 14 2015 Phase 2

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Hedgehog/Smoothened Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID