SAG (Smoothened Agonist) HCl

SAG (Smoothened Agonist) HClは1種の細胞浸透性Smoothened (Smo)の作動剤で、Shh-LIGHT2細胞の中でEC50 値は3 nMです。

SAG (Smoothened Agonist) HCl化学構造

CAS No. 2095432-58-7

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 44500 国内在庫なし(納期7~10日)
JPY 22000 国内在庫あり
JPY 37000 国内在庫あり
JPY 112000 国内在庫あり
JPY 145500 国内在庫あり
JPY 595500 国内在庫なし(納期7~10日)

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SAG (Smoothened Agonist) HCl関連製品

Hedgehog/Smoothened阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
HUVEC Cytotoxicity assay 24 h Cytotoxicity against HUVEC after 24 hrs by WST-1 assay, IC50=22 μM 22985958
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
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
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
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
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
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生物活性

製品説明 SAG (Smoothened Agonist) HClは1種の細胞浸透性Smoothened (Smo)の作動剤で、Shh-LIGHT2細胞の中でEC50 値は3 nMです。
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.
細胞実験 細胞株 Shh-LIGHT2 cells
濃度 3 nM
反応時間 30 h
実験の流れ

Cells were treated with various concentrations of SAG in DMEM containing 0.5% (vol/vol) bovine calf serum.

実験結果図 Methods Biomarkers 結果図 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]

動物実験 動物モデル Rat
投与量 2.5 nM
投与経路 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 --

化学情報

分子量 526.52 化学式

C28H29Cl2N3OS

CAS No. 2095432-58-7 SDF Download SAG (Smoothened Agonist) HCl SDFをダウンロードする
Smiles CNC1CCC(CC1)N(CC2=CC(=CC=C2)C3=CC=NC=C3)C(=O)C4=C(C5=CC=CC=C5S4)Cl.Cl
保管

In vitro
Batch:

DMSO : 82 mg/mL ( (155.73 mM); Warmed with 50℃ water bath; 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : 50 mg/mL

Ethanol : 27 mg/mL

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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Handling Instructions

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