Product Introduction
Bioactivity


英文名: Sulforaphane

描述: Sulforaphane 是存在于多種蔬菜中的一種天然異硫氰酸酯。它可以激活Nrf2，并通過 AMPK 依賴性信號傳導抑制高糖誘導的胰腺癌。它增加腫瘤抑制蛋白的轉(zhuǎn)錄并抑制組蛋白脫乙酰酶的活性，具有抗癌和抗炎活性。

細胞實驗: HT29 cells are seeded at low density (5×10^4 cells/mL) in 35- or 120-mm diameter Primaria dishes in standard medium containing 5% FCS. One day after seeding, the medium is changed, and HT29 cells are treated with sulforaphane (0-30 μM). An equivalent amount of the solvent (ethanol) is added to control cells (0.2% final concentration). The drug effect on cellular viability is evaluated using the MTT assay [1].

動物實驗: At age 47, 48, 49, 50, and 51 days, each animal receives by gavage either 0.5 mL of Emulphor EL-620 alone or the specified doses (75, 100, or 150 μM daily) of sulforaphane or compound 2, 3, or 4 in 0.5 mL of Emulphor EL-620. On day 50, 3 hr after administration of the vehicle or protector, all rats also receive an intragastric instillation of 8.0 mg of DMBA dissolved in 1.0 mL of sesame oil. This dose of DMBA is selected to produce a substantial tumor incidence, but not one so high as to overwhelm a potential chemoprotective effect. The animals are examined once weekly for the appearance and location of palpable tumors. At age 202 days, i.e., 152 days after carcinogen administration, all animals are euthanized with ether and weighed. The tumors are separated from the fat and connective tissue by dissection weighed and fixed in buffered 10% formalin. All tumors are identified microscopically by examination of stained sections [3].

體外活性: Sulforaphane以劑量依賴的方式引起細胞周期阻滯，隨后導致細胞死亡。這種由sulforaphane引起的細胞周期阻滯與cyclins A和B1表達增加有關。Sulforaphane通過凋亡過程誘導細胞死亡，并抑制HT29靜息結腸癌細胞的生長重啟及降低細胞活性，對分化的CaCo2細胞毒性較低[1]。H9c2大鼠心肌細胞預處理sulforaphane可減少凋亡細胞數(shù)和凋亡蛋白表達，并降低多柔比星引起的線粒體膜電位增加。此外，sulforaphane增加血紅素加氧酶-1的mRNA和蛋白表達，從而降低多柔比星引起的線粒體反應性氧種類水平[2]。

體內(nèi)活性: 給予sulforaphane能夠降低單劑量DMBA誘發(fā)的雌性SD大鼠乳腺腫瘤的發(fā)生率、數(shù)量、體重，并延緩其發(fā)展[3]。

存儲條件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 55 mg/mL (310.23 mM)


關鍵字: Keap1-Nrf2 | inhibit | Inhibitor | HDAC | Histone deacetylases | Apoptosis | Sulforaphane

相關產(chǎn)品: BG45 | GSK1904529A | LCH-7749944 | COTI-2 | Omaveloxolone | ML141 | Voreloxin hydrochloride | Coenzyme Q9 | Larotrectinib sulfate | Nocodazole

相關庫: Drug Repurposing Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Ferroptosis Compound Library | Anti-Cancer Clinical Compound Library | Epigenetics Compound Library | Anti-Cancer Active Compound Library | DNA Damage & Repair Compound Library | Natural Product Library | Chromatin Modification Compound Library

TargetMol（陶術）作為一家全球性的生物醫(yī)藥領域高科技企業(yè)，我們致力于為高校、研究所、醫(yī)院、企業(yè)等各類生物醫(yī)藥研發(fā)機構提供優(yōu)質(zhì)的產(chǎn)品和服務，為全球醫(yī)藥科學家更高效地完成科研工作助力�？商峁�20,000+種 抑制劑和激動劑 、800+種 化合物庫 、19,000+種 天然產(chǎn)物 ，以及9,000+種 重組蛋白 、多種 多肽 、抗體 和 生命科學試劑盒 等。此外，在上海，TargetMol研發(fā)中心配備了 CADD & AIDD研究中心、藥理實驗室和藥物化學合成 平臺三大技術中心，可提供虛擬篩選、化合物活性測試、分子間結合力檢測和化合物結構優(yōu)化等技術服務，多方位滿足用戶的研發(fā)需求。