SGC-GAK-1 - GAK 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESGC-GAK-1Cat. No.: HY-122186CAS No.: 2226517-76-4分式: CHBrNO分量: 389.24作靶點(diǎn): Others作通路: Others儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 125 mg/mL (321.14 mM)* means soluble, but saturati

2、on unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.5691 mL 12.8455 mL 25.6911 mL5 mM 0.5138 mL 2.5691 mL 5.1382 mL10 mM 0.2569 mL 1.2846 mL 2.5691 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請根據(jù)您的實(shí)驗(yàn)動物和給藥式選擇適當(dāng)?shù)娜芙獍福渲魄罢埾扰渲瞥吻宓膬湟?，再依次添加助溶?為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲備液可以根據(jù)儲存條

3、件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (5.34 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (5.34 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 SGC-GAK

4、-1種有效的選擇性細(xì)胞周 期蛋 G 相關(guān)激酶 (GAK) 抑制劑，Ki 為 3.1 nM。SGC-GAK-1是GAK的化學(xué)探針 1。IC50 & Target Ki: 3.1 nM (GAK) 1體外研究 SGC-GAK-1 potently binds cyclin G-associated kinase (GAK), adaptor protein 2-associated kinase (AAK1),serine/threonine kinase 16 (STK16) with Kis of 3.1 nM, 53 M, 51 M, respectively 1.SGC-GAK-1 pot

5、ently binds cyclin G-associated kinase (GAK), receptor-interacting protein kinase 2 (RIPK2),AarF domain containing kinase 3 (ADCK3), and nemo-like kinase (NLK) with KDs of 1.9 nM, 110 nM, 190nM, and 520 nM, respectively 1.SGCGAK-1 (0.1, 1, and 10 M, 48 hours or 72 hours) shows strong growth inhibiti

6、on in LNCaP, VCaP, and22Rv1 cells at 10 M, but minimal effect in PC3 and DU145 cells 1.Cell Viability Assay 1Cell Line: Prostate cancer cells (22Rv1, LNCaP, VCaP, PC3, DU145)Concentration: 0.1, 1, and 10 MIncubation Time: 48 hours or 72 hoursResult: Showed potent antiproliferative activity in LNCaP and 22Rv1 cells with IC50s of0.050.15 M and 0.170.65 M, respectively.REFERENCES1. Asquith CRM, et al. SGC-GAK-1: A Chemical Probe for Cyclin G Associated Kinase (GAK). J Med Chem. 2019 Feb 26.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use on