Smoothened Agonist (SAG) HCl

For research use only.

Catalog No.S7779

34 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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10mM (1mL in DMSO) USD 447 In stock
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Selleck's Smoothened Agonist (SAG) HCl has been cited by 34 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.
Targets
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 M{jUemZ2dmO2aX;uJIF{e2G7 NETwS2M1QCCqcoO= MoHXRYN1cX[jdHnvckBw\iCVaHigdIF1cHejeTDpckBud3W|ZTDTbIguVGmpaISgTWkh[2WubIOgZZN{\XO|ZXSgZZMhcW6mdXP0bY9vKG:oIHfsbVEh\XiycnXzd4lwdiCjZoTldkA1QCCqcoOgZpkhemWwaXzsZUBtfW2rbnXzZ4Vv[2ViYYPzZZktKEWFNUC9NE4xODh6IN88US=> M4XSTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OUi1PVU5Lz5{Mkm4OVk2QDxxYU6=
HUVEC MnLlR5l1d3SxeHnjbZR6KGG|c3H5 MoTKNlQhcA>? NYSwZpg1S3m2b4TvfIlkcXS7IHHnZYlve3RiSGXWSWMh[W[2ZYKgNlQhcHK|IHL5JHdUXC1zIHHzd4F6NCCLQ{WwQVIzKM7:TR?= MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjl6NUm1PEc,OjJ7OEW5OVg9N2F-
Shh-Light II NVvveGdFTnWwY4Tpc44h[XO|YYm= NXLENG5FPDhiaILz MlXqRYN1cX[jdHnvckBw\iCVaHigdIF1cHejeTDpckBud3W|ZTDTbIguVGmpaISgTWkh[2WubIOgZZN{\XO|ZXSgZZMhcW6mdXP0bY9vKG:oIHfsbVEh\XiycnXzd4lwdiCjZoTldkA1QCCqcoOgZpkhemWwaXzsZUBtfW2rbnXzZ4Vv[2ViYYPzZZktKEWFNUCgQUAxNjB4MUig{txONg>? M4W4OVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OUi1PVU5Lz5{Mkm4OVk2QDxxYU6=
NIH/3T3 MVHGeY5kfGmxbjDhd5NigQ>? NHvpWoFC\2:waYP0JIFkfGm4aYT5JIF1KFOvbzDpckBud3W|ZTDOTWgwO1R|IHPlcIx{KHS{YX7z[oVkfGWmIIfpeIghT2yrLXTldIVv\GWwdDDmbZJm\my7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKgZZN{\XO|ZXSgZZMhe3SrbYXsZZRqd25ib3[gS4xqKHS{YX7zZ5JqeHSrb36g[oFkfG:{LDDFR|UxKD1iMD6wN{DPxE1w NWOwdGJ[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke0NlkzPTVpPkK3OFI6OjV3PD;hQi=>
C3H10T1/2 MoKySpVv[3Srb36gZZN{[Xl? NGrnd2c3KGSjeYO= NH[0dYJC\2:waYP0JIFkfGm4aYT5JIF1KFOvbzDpckBud3W|ZTDDN2gyOFRzL{KgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5lfWO2aX;uJI9nKGOnbHyg[Iln\mW{ZX70bYF1cW:wIHnueI8hd3O2ZX;icIF{fCCrbnP1ZoF1\WRiZn;yJFYh\GG7czDifUBidGujbHnu[UBxcG:|cHjheIF{\SCjc4PhfUwhTUN3MDC9JFAvOTNizszNMi=> NFPlfms9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{SyPVI2PSd-Mke0NlkzPTV:L3G+
A673 MlTkdWhVWyCjc4PhfS=> M4jVTJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCDNkezJINmdGy| MmrRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Saos-2 NVTOTVlyeUiWUzDhd5NigQ>? NYXLb2dUeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPhc5MuOiClZXzsdy=> MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
BT-37 Mor1dWhVWyCjc4PhfS=> MX\xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSlRvM{egZ4VtdHN? M2PoXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
RD MoPvdWhVWyCjc4PhfS=> MY\xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWkRiY3XscJM> NVjVVmc3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-SH MlzudWhVWyCjc4PhfS=> NXrJZlB2eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uW0hiY3XscJM> M2\F[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
BT-12 MnvXdWhVWyCjc4PhfS=> M{nMV5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2xNkBk\Wyucx?= MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
MG 63 (6-TG R) MmfudWhVWyCjc4PhfS=> MnnWdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE2JIE[zJEg3NVSJIGKpJINmdGy| M1HIUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB1643 MYDxTHRUKGG|c3H5 NIrHNIFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKxOlQ{KGOnbHzz NVzsXIRkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
OHS-50 MXvxTHRUKGG|c3H5 MlzqdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE:KUz21NEBk\Wyucx?= MmL6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SJ-GBM2 NUfU[pdzeUiWUzDhd5NigQ>? MnTpdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO= MlPaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC MkjpdWhVWyCjc4PhfS=> NV[3ZZhoeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM> M17FcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB-EBc1 MU\xTHRUKGG|c3H5 Ml20dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6ELVXCZ|Eh[2WubIO= MkHTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh18 NXXxN|N4eUiWUzDhd5NigQ>? MX;xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmhzODDj[Yxtew>? M4TmN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=

... Click to View More Cell Line Experimental Data

Assay
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.

23504944
Immunofluorescence
Smo; 

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]

Protocol

Animal Research:[3]
- Collapse
  • 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):
water
For best results, use promptly after mixing.
100mg/mL

* 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
Formula

C28H29Cl2N3OS

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
NCT02044068 Completed -- Vertical Disease Transmission|HBV Hopital Lariboisière October 2014 --
NCT02058134 Terminated Device: cardioPAT cell saver Coronary Artery Disease|Aortic Stenosis|Aortic Insufficiency|Mitral Insufficiency|Aortic Aneurysm Rigshospitalet Denmark December 2013 Not Applicable
NCT01264094 Terminated Drug: Clevudine Chronic Hepatitis B Bukwang Pharmaceutical November 2009 Phase 4

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Hedgehog/Smoothened Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID