Home Stem Cells & Wnt Hedgehog/Smoothened agonist SAG (Smoothened Agonist) HCl For research use only.

SAG (Smoothened Agonist) HCl

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

SAG (Smoothened Agonist) HCl Chemical Structure

SAG (Smoothened Agonist) HCl Chemical Structure

CAS: 2095432-58-7

Selleck's SAG (Smoothened Agonist) HCl has been cited by 65 publications

Purity & Quality Control

Batch: Purity: 99.98%
99.98

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
mouse Shh-Light II cell Function assay 48 hrs Activation of Shh pathway in mouse Shh-Light II cells assessed as induction of gli1 expression after 48 hrs by renilla luminescence assay, EC50=0.0088 μM 22985958
HUVEC Cytotoxicity assay 24 h Cytotoxicity against HUVEC after 24 hrs by WST-1 assay, IC50=22 μM 22985958
Shh-Light II Function assay 48 hrs Activation of Shh pathway in mouse Shh-Light II cells assessed as induction of gli1 expression after 48 hrs by renilla luminescence assay, EC50 = 0.0618 μM. 22985958
NIH/3T3 Function assay Agonist activity at Smo in mouse NIH/3T3 cells transfected with Gli-dependent firefly luciferase reporter assessed as stimulation of Gli transcription factor, EC50 = 0.03 μM. 27429255
C3H10T1/2 Function assay 6 days Agonist activity at Smo in mouse C3H10T1/2 cells assessed as induction of cell differentiation into osteoblast incubated for 6 days by alkaline phosphatase assay, EC50 = 0.13 μM. 27429255
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
Click to View More Cell Line Experimental Data

Biological Activity

Description SAG (Smoothened Agonist) 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
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]
Kinase Assay Cell-Based Assays for Hh Pathway Activation
Assays for Hh pathway activation in Shh-LIGHT2 cells, a clonal NIH 3T3 cell line stably incorporating Gli-dependent firefly luciferase and constitutive Renilla luciferase reporters, are conducted. For studies of SAG (a chlorobenzothiophene-containing Hh pathway agonist) and PA-SAG, Shh-LIGHT2 cells are cultured to confluency in 96-well plates and then treated with various concentrations of these compounds in DMEM containing 0.5% (vol/vol) bovine calf serum.
Cell Research Cell lines Shh-LIGHT2 cells
Concentrations 3 nM
Incubation Time 30 h
Method

Cells were treated with various concentrations of SAG in DMEM containing 0.5% (vol/vol) bovine calf serum.
Experimental Result Images Methods Biomarkers Images PMID
Western blot LC3I / LC3II 23504944
Immunofluorescence Smo acetylated alpha tubulin 25636740
In Vivo
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 Animal Models Rat
Dosages 2.5 nM
Administration Intracerebroventricular administration
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05937178 Recruiting Hepatitis B Chronic Huashan Hospital|The First Affiliated Hospital of Anhui Medical University|Anhui Provincial Hospital|Beijing YouAn Hospital|Peking University People''s Hospital|Peking University First Hospital|Xiamen Hospital of Traditional Chinese Medicine|First Affiliated Hospital of Fujian Medical University|LanZhou University|Third Affiliated Hospital Sun Yat-Sen University|First Affiliated Hospital of Guangxi Medical University|The Affiliated Hospital Of Guizhou Medical University|Hainan General Hospital|Hebei Medical University Third Hospital|The First Affiliated Hospital of Henan University of Traditional Chinese Medicine|Henan Provincial People''s Hospital|The Second Affiliated Hospital of Harbin Medical University|Tongji Hospital|Wuhan Union Hospital China|Renmin Hospital of Wuhan University|Central South University|Xiangya Hospital of Central South University|The First Hospital of Jilin University|the Second Hospital of Nangjing|The Affiliated Nanjing Drum Tower Hospital of Nanjing University Medical School|The First Affiliated Hospital with Nanjing Medical University|The Affiliated Hospital of Xuzhou Medical University|The First Affiliated Hospital of Nanchang University|Shengjing Hospital|Qingdao Sixth People''s Hospital|Shandong Provincial Hospital|The Second Hospital of Shandong University|The First Affiliated Hospital of Shanxi Medical University|Tang-Du Hospital|First Affiliated Hospital Xi''an Jiaotong University|Ruijin Hospital|West China Hospital|Tianjin Second People''s Hospital|First Affiliated Hospital of Xinjiang Medical University|The First People''s Hospital of Yunnan|Shulan (Hangzhou) Hospital|Zhejiang University|Southwest Hospital China|The Second Affiliated Hospital of Chongqing Medical University|Sichuan Provincial People''s Hospital January 31 2023 --
NCT05701592 Recruiting Posterior Cruciate Ligament Tear Konrad Malinowski MD|Artromedical Konrad Malinowski Clinic December 20 2022 --
NCT03645044 Active not 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 --

Chemical lnformation & Solubility

Molecular Weight 526.52 Formula

C28H29Cl2N3OS
CAS No. 2095432-58-7 SDF Download SAG (Smoothened Agonist) HCl SDF
Smiles CNC1CCC(CC1)N(CC2=CC(=CC=C2)C3=CC=NC=C3)C(=O)C4=C(C5=CC=CC=C5S4)Cl.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 82 mg/mL ( (155.73 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 50 mg/mL

Ethanol : 27 mg/mL


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In vivo
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Tech Support

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