SW-100 - HDAC6 抑制劑 - 生命科學(xué)試劑 - 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作靶點: HDAC作通路: Cell Cycle/DNA Damage; Epigenetics儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 125 mg/mL (394.60 mM)* mean

2、s soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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)實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議

3、您現(xiàn)現(xiàn)配，當天使；澄清的儲備液可以根據(jù)儲存條件，適當保存；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 (6.57 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (6.57 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oil1/3 Mast

4、er of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.08 mg/mL (6.57 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 SW-100種有效的組蛋脫酰基酶 6 (HDAC6) 抑制劑，IC50 值為 2.3 nM，相對于其他 HDAC 酶，對HDAC6 的選擇性少 1000倍。SW-100 顯著提了跨越腦屏障的能 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)體外研究 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.體內(nèi)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 您邊的抑制劑師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