GSK-690-Hydrochloride - Histone Demethylase 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGSK 690 HydrochlorideCat. No.: HY-117226A分式: CHClNO分量: 405.92作靶点: Histone Demethylase作通路: Epigenetics储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 125 mg/mL (307.94 mM; Need ultrasonic)Ma

2、ss Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.4635 mL 12.3177 mL 24.6354 mL5 mM 0.4927 mL 2.4635 mL 4.9271 mL10 mM 0.2464 mL 1.2318 mL 2.4635 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的

3、百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (5.12 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (5.12 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (5.12 mM); Clear sol

4、ution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 GSK 690 (Hydrochloride)是赖氨酸特异性去甲基化酶1 (LSD1) 的可逆抑制剂，Kd 值为 9 nM，IC50 值为 37nM。IC50 & Target IC50: 37 nM (LSD1), Kd: 8 nM (LSD1) 1.体外研究 GSK690 (1-10 M) acts together with JNJ-26481585 to induce cell death in all four tested RMS

5、 cells lines(RD, RH30, RMS13, and TE381.T cells) 2.GSK690/JNJ-26481585 cotreatment alters the balance between pro- and antiapoptotic proteins with 1MGSK690 for RD cells and 10M GSK690 for RH30 cells 2.GSK690/JNJ-26481585 cotreatment induces caspase-dependent cell death with 1M GSK690 for RD cellsand

6、 10M GSK690 for RH30 cells 2.The addition of GSK690 further enhances the JNJ-26481585-stimulated G2/M arrest 2.REFERENCES1. Mould DP, et al. Development of (4-Cyanophenyl)glycine Derivatives as Reversible Inhibitors of Lysine Specific Demethylase 1. J MedChem. 2017 Oct 12;60(19):7984-7999.2. Haydn T, et al. Concomitant epigenetic targeting of LSD1 and HDAC synergistically induces mitochondrial apoptosis inrhabdomyosarcoma cells. Cell Death Dis. 2017 Jun 15;8(6):e2879.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use onl