Sulforaphane _HDAC 抑制劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESulforaphaneCat. No.: HY-13755CAS No.: 4478-93-7分式: CHNOS分量: 177.29作靶點: HDAC作通路: Cell Cycle/DNA Damage; Epigenetics儲存式: -20C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性數據體外實驗 DMSO : 62.

2、5 mg/mL (352.53 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 5.6405 mL 28.2024 mL 56.4048 mL5 mM 1.1281 mL 5.6405 mL 11.2810 mL10 mM 0.5640 mL 2.8202 mL 5.6405 mL請根據產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。體內實驗 請根據您的實驗動物和給藥式選擇適當的溶解案，配制前請先配制澄清的儲備液，再依次添

3、加助溶劑(為保證實驗結果的可靠性，體內實驗的作液，建議您現現配，當天使；澄清的儲備液可以根據儲存條件，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: 2.5 mg/mL (14.10 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (14.10 mM); Clear solution3. 請依序添加每種溶劑： 10

4、% DMSO 90% corn oilSolubility: 2.5 mg/mL (14.10 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Sulforaphane存在于多種蔬菜中的天然異硫氰酸酯；具有抗癌和保護臟的活性。IC50 & Target HDAC體外研究 Sulforaphane induces a cell cycle arrest in a dose-dependent manner, followed by cell death. This

5、sulforaphane-induced cell cycle arrest was correlated with an increased expression of cyclins A and B1.Sulforaphane induces cell death via an apoptotic process. Sulforaphane inhibits the reinitiation of growth anddiminishes cellular viability in quiescent colon carcinoma cells (HT29) and has a lower

6、 toxicity ondifferentiated CaCo2 cells 1. Pre-treatment of H9c2 rat myoblasts with sulforaphane decreases theapoptotic cell number and the expression of pro-apoptotic proteins (Bax, caspase-3 and cytochrome c), aswell as the doxorubicin-induced increase in mitochondrial membrane potential. Furthermo

7、re, sulforaphaneincreases the mRNA and protein expression of heme oxygenase-1, which consequently reduces the levels ofreactive oxygen species (ROS, measured using MitoSOX Red reagent) in the mitochondria which areinduced by doxorubicin 2.體內研究 Sulforaphane can block the formation of ammary tumors in

8、 Sprague-Dawley rats treated with single doses of9,10-dimethyl-1,2-benzanthracene. Administration of sulforaphane reduces the incidence, multiplicity, andweights and delays the development of the mammary tumors evoked by a single dose of DMBA in femaleSprague-Dawley rats 3.PROTOCOLCell Assay 1 HT29

9、cells are seeded at low density (5104 cells/mL) in 35- or 120-mm diameter Primaria dishes instandard medium containing 5% FCS. One day after seeding, medium is changed, and HT29 cells aretreated with sulforaphane (0-30 M). An equivalent amount of the solvent (ethanol) is added to control cells(0.2%

10、final concentration). Drug effect on cellular viability is evaluated using the MTT assay 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Rats: At age 47, 48, 49, 50, and 51 days, each animal receives by gavage either 0.5 mL of Emulphor EL-620Ad

11、ministration 3 alone or the specified doses (75, 100, or 150 M daily) of sulforaphane or compound 2, 3, or 4 in 0.5 mL ofEmulphor EL-620. On day 50, 3 hr after administration of the vehicle or protector, all rats also receive anintragastric instillation of 8.0 mg of DMBA dissolved in 1.0 mL of sesam

12、e oil. This dose of DMBA is selectedto produce a substantial tumor incidence, but not one so high as to overwhelm a potential chemoprotectiveeffect. The animals are examined once weekly for the appearance and location of palpable tumors. At age202 days, i.e., 152 days after carcinogen administration

13、, all animals are euthanized with ether and weighed.The tumors are separated from fat and connective tissue by dissection, weighed, and fixed in buffered 10%formalin. All tumors are identified microscopically by examination of stained sections 3.MCE has not independently confirmed the accuracy of th

14、ese methods. They are for reference only.戶使本產品發(fā)表的科研獻2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE J Cancer Res Clin Oncol. 2019 Apr;145(4):861-872. Vascul Pharmacol. 2018 Oct;109:56-71.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Gamet-Payrastre L, et al. Sulforaphane, a

15、 naturally occurring isothiocyanate, induces cell cycle arrest and apoptosis in HT29 humancolon cancer cells. Cancer Res. 2000 Mar 1;60(5):1426-33.2. Li B, et al. Sulforaphane prevents doxorubicin-induced oxidative stress and cell death in rat H9c2 cells. Int J Mol Med. 2015 Jul;36(1):53-64.3. Zhang Y, et al. Anticarcinogenic activities of sulforaphane and structurally related synthetic norbornylisothiocyanates. Proc Natl Acad SciU