SW-100 - HDAC6 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESW-100Cat. No.: HY-115475CAS No.: 2126744-35-0分式: CHClNO分量: 316.78作靶点: HDAC作通路: Cell Cycle/DNA Damage; 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 (394.60 mM)* mean

2、s soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.1568 mL 15.7838 mL 31.5676 mL5 mM 0.6314 mL 3.1568 mL 6.3135 mL10 mM 0.3157 mL 1.5784 mL 3.1568 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

3、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 (6.57 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 (6.57 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/3 Mast

4、er of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.08 mg/mL (6.57 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 SW-100种有效的组蛋脱酰基酶 6 (HDAC6) 抑制剂，IC50 值为 2.3 nM，相对于其他 HDAC 酶，对HDAC6 的选择性少 1000倍。SW-100 显著提了跨越脑屏障的能 1。IC50 & Target HDAC1 HDAC2 HDAC3 HDAC45.23 M (IC50) 32.8 M (IC50) 29.5 M (IC50) 10.9 M (IC

5、50)HDAC5 HDAC6 HDAC7 HDAC84.07 M (IC50) 2.3 nM (IC50) 4.55 M (IC50) 3.72 M (IC50)HDAC9 HDAC10 HDAC113.46 M (IC50) 26.2 M (IC50) 5.72 M (IC50)体外研究 SW-100 (0.01-10 M; 48 hours) shows obvious increase in the acetylated -tubulin levels in a dose-dependent manner 1.Western Blot Analysis 1Cell Line: HEK29

6、3 cellsConcentration: 0.01, 0.1, 1, 10 MIncubation Time: 48 hoursResult: Showed obvious increase in the acetylated -tubulin levels in a dose-dependent manner.体内研究 SW-100 (20 mg/kg; i.p.; twice a day for two days) ameliorates several memory and learning impairmentsincluding novel object recognition,

7、temporal ordering, and coordinate and categorical spatial processing inmouse model of Fragile X syndrome 1.Animal Model: 8-10 weeks old C57BL/6 mice (Fmr1-/- mice) 1Dosage: 20 mg/kgAdministration: Intraperitoneal injection; twice a day for two daysResult: Ameliorated several memory and learning impa

8、irments including novel objectrecognition, temporal ordering, and coordinate and categorical spatial processing inFmr1-/- mice。REFERENCES2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE1. Kozikowski AP, et al. Brain Penetrable Histone Deacetylase 6 Inhibitor SW-100 Ameliorates Memory and LearningImpairments in aMouse Model of Fragile X Syndrome. ACS Chem Neurosci. 2019 Mar 20;10(3):1679-1695.McePdfHeightCaution: Product has not been fully validated for medical applica