Sulforaphane _HDAC 抑制剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESulforaphaneCat. No.: HY-13755CAS No.: 4478-93-7分式: CHNOS分量: 177.29作靶点: HDAC作通路: Cell Cycle/DNA Damage; Epigenetics储存式: -20C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性数据体外实验 DMSO : 62.

2、5 mg/mL (352.53 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液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

3、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: 2.5 mg/mL (14.10 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (14.10 mM); Clear solution3. 请依序添加每种溶剂： 10

4、% DMSO 90% corn oilSolubility: 2.5 mg/mL (14.10 mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 Sulforaphane存在于多种蔬菜中的天然异硫氰酸酯；具有抗癌和保护脏的活性。IC50 & Target HDAC体外研究 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.体内研究 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.户使本产品发表的科研献2/3 Master of Small Molecules 您边的抑制剂师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