價格 | ¥339 | ¥489 | ¥792 |
包裝 | 1mg | 2mg | 5mg |
最小起訂量 | 1mg |
發(fā)貨地 | 上海 |
更新日期 | 2024-09-29 |
中文名稱:化合物 Smoothened Agonist | 英文名稱:SAG |
CAS:912545-86-9 | 品牌: TargetMol |
產(chǎn)地: 美國 | 保存條件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
純度規(guī)格: 98.88% | 產(chǎn)品類別: 抑制劑 |
貨號: T1779 |
名稱 | SAG |
描述 | SAG (Smoothened Agonist) is a Smo receptor agonist (EC50=3 nM) that is cell-permeable and selective. SAG regulates Smo activity by binding directly to the Smo helix and can activate the Hedgehog signaling pathway. |
激酶實驗 | In vitro Kinase Assays: Kinase assays for CDK1, CDK2 and GSK3-β are all carried out in a radiometric filter binding format. Assays for CDK5 are in DELFIA format and for CDKs 4 and 6 in ELISA format. For CDKs 1 and 2, the relevant CDK and 0.12 μg/mL Histone H1 are incubated in 20 mM MOPS, pH 7.2, 25 mM β-glycerophosphate, 5 mM EDTA, 15 mM MgCl2, 1 mM sodium orthovanadate, 1 mM DTT, 0.1 mg/mL BSA, 45 μM ATP (0.78 Ci/mmol) and different concentrations of AT7519 for 2 or 4 hours respectively. For GSK3-β, the relevant enzyme and 5 μM glycogen synthase peptide 2 along with 10 mM MOPS pH 7.0, 0.1 mg/mL BSA, 0.001% Brij-35, 0.5% glycerol, 0.2 mM EDTA, 10 mM MgCl2, 0.01% β-mercaptoethanol, 15 μM ATP (2.31 Ci/mmol) and different concentrations of AT7519 are incubated for 3 hours. Assay reactions are stopped by adding an excess of orthophosphoric acid and filtered using Millipore MAPH filter plates. The plates are then washed, scintillant added and radioactivity measured by scintillation counting on a Packard TopCount. For CDK5, CDK5/p35 and 1 μM of a biotinylated Histone H1 peptide (Biotin-PKTPKKAKKL) are incubated in 25 mM Tris-HCl, pH 7.5, 2.5 mM MgCl2, 0.025% Brij-35, 0.1 mg/mL BSA, 1 mM DTT, 15 μM ATP and different concentrations of AT7519 for 30 minutes. Assay reactions are stopped using EDTA, transferred to Neutravidin-coated plates and phosphorylated peptide quantified by means of a rabbit phospho-cdk1 substrate polyclonal antibody and DELFIA europium-labelled anti-rabbit IgG secondary antibody using time-resolved fluorescence at λex=335 nM, λem=620 nM. For CDK 4 and 6 assays, plates are coated with GST- pRb769-921 and blocked with Superblock. CDK4 or 6 is incubated with 15 mM MgCl2, 50 mM HEPES, pH 7.4, 1 mM DTT, 1 mM EGTA, pH 8.0, 0.02% Triton X-100, 2.5% DMSO and different concentrations of AT7519; the reaction is initiated by addition of ATP. After 30 minutes, reactions are stopped by the addition of 0.5 M EDTA pH 8.0.Plates are then washed and incubated for one hour with the primary antibody (anti- p-Rb Serine 780) diluted in Superblock followed by secondary antibody (alkaline phosphatase linked anti-rabbit) for a further hour. Plates are developed using the Attophos system and fluorescence read on a Spectramax Gemini plate reader at excitation 450 nm and emission 580 nm. In all cases, IC50 values are calculated from replicate curves, using GraphPad Prism software. |
體外活性 | 方法:胚胎干細(xì)胞 ES 用 SAG (0.5-1.25 μM) 處理 4-6 天,使用 RT-qPCR 基因表達(dá)水平。 結(jié)果:有絲分裂后 V3 標(biāo)志物 Sim1 在所有濃度的 SAG 處理組中的表達(dá)都增加。用 0.5 μM SAG 處理的組表現(xiàn)出顯著更高水平的 Nkx2.2 mRNA 水平。在給定的時間點,Hb9 表達(dá)與 SAG 濃度沒有顯著變化。[1] 方法:非洲綠猴腎臟成纖維細(xì)胞樣細(xì)胞 Cos-1 用 SAG (5-500 nM) 處理,使用 Western Blot 方法檢測靶點蛋白表達(dá)水平。 結(jié)果:SAG 以劑量依賴的方式抑制 Cos-1 細(xì)胞中 ER 定位的和 ER 后形式的 Smo-Myc3 與 125I 標(biāo)記的 PA 環(huán)胺的交聯(lián)。Smo-Myc3 的細(xì)胞水平不受激動劑治療的影響。[2] |
體內(nèi)活性 | 方法:為探索 SHH 信號通路是否通過調(diào)節(jié)線粒體穩(wěn)態(tài)在焦慮中發(fā)揮保護(hù)作用,將 SAG (10 mg/kg) 腹腔注射給高脂飲食的 C57BL/6 小鼠,每三天一次,持續(xù)十二周。 結(jié)果:SHH 信號在肥胖中具有神經(jīng)保護(hù)作用,SAG 通過減少線粒體斷裂來緩解焦慮樣行為。[3] 方法:為研究對發(fā)育中的肢體的影響,將 SAG (15-20 mg/kg in lactated Ringer's solution) 單次腹腔注射給妊娠日 (GD) 9.25 的懷孕的 C57BL/6J 小鼠。 結(jié)果:SAG 最普遍的作用是對軸前多指畸形的劑量依賴性誘導(dǎo);缺陷范圍從拇指寬到拇指軸前側(cè)兩個手指狀指的重復(fù)。[4] |
存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 55 mg/mL (112.23 mM), Heating is recommended. Ethanol : 40 mg/mL (75.97 mM), Heating is recommended. |
關(guān)鍵字 | Smo | SAG | inhibit | Smoothened | Inhibitor |
相關(guān)產(chǎn)品 | ALLO-2 | Tolnaftate | LEQ506 | Halcinonide | Triparanol | MRT-83 | Ellagic acid | Naftifine hydrochloride | GANT 61 | Vismodegib | IHR-1 | Itraconazole |
相關(guān)庫 | 經(jīng)典已知活性庫 | 抗癌化合物庫 | 已知活性化合物庫 | 成骨分子庫 | NO PAINS 化合物庫 | GPCR靶點分子庫 | 膜蛋白靶向化合物庫 | 神經(jīng)元分化化合物庫 | Wnt/Hedgehog/Notch 通路化合物庫 | 抗前列腺癌化合物庫 |
成立日期 | 2013-04-18 (12年) | 注冊資本 | 566.265100萬人民幣 |
員工人數(shù) | 100-500人 | 年營業(yè)額 | ¥ 1億以上 |
主營行業(yè) | 天然產(chǎn)物,生化試劑,分子生物學(xué),分子砌塊,生物技術(shù)服務(wù) | 經(jīng)營模式 | 貿(mào)易,工廠,試劑,定制,服務(wù) |
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