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SAG (Smoothened Agonist) HCl

Name: SAG (Smoothened Agonist) HCl
Brand: Selleck Chemicals
SKU: S7779
Rating: 5 (68 reviews)

Catalog No.S7779 Purity:99.98%

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

CAS No. 2095432-58-7

Purity & Quality Control

Batch: Purity: 99.98%

99.98

SAG (Smoothened Agonist) HCl Related Products

Related Targets	Hedgehog Smoothened GLI	Click to Expand
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Related Compound Libraries	Kinase Inhibitor Library FDA-approved Drug Library Stem Cell Signaling Compound Library GPCR Compound Library Stem Cell Differentiation Compound Library	Click to Expand

Signaling Pathway

Hedgehog/Smoothened Signaling Pathway

Cell Data

Cell Lines	Assay Type	Incubation Time	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
Kinase Assay	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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
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	--

References

[4] Heine VM, et al. Sci Transl Med. 2011, 3(105), 105ra104.

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Chemical Information & 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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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