| 名稱 | Daphnetin |
| 描述 | Daphnetin (7,8-Dihydroxycoumarin), a natural coumarin derivative, is a protein kinase inhibitor with inhibitory for EGFR (IC50: 7.67 μM), PKA (IC50: 9.33 μM), and PKC (IC50: 25.01 μM), also exhibit anti-oxidant and anti-inflammatory activities. |
| 細(xì)胞實驗 | The cytostatic effect of Daphnetin tested on the MCF-7 tumor cells is estimated using the microculture MTT assay. The assay is based on the reduction of soluble tetrazolium salt by mitochondria of viable cells. The reduced product, an insoluble purple-colored formazan, is dissolved in dimethyl sulfoxide and measured spectrophotometrically (570 nm). The amount of formazan formed is proportional to the number of viable cells. Cells (3 × 103) are seeded in each of the 96 microplate wells in a 200 μL medium containing the corresponding concentration of daphnetin. Daphnetin is tested at five concentrations (12.5 μM, 25 μM, 50 μM, 100 μM, 200 μM). After 24-hour, 48-hour, and 72-hour exposure, the percentage of proliferative inhibition of treated cells is estimated against the solvent-treated control cells (PI% = [(T/C) ? 1] × 100). PI = proliferation inhibition; T = treated, C = control. IC50 is calculated from the least square concentration-response regressions.(Only for Reference) |
| 激酶實驗 | Assay of protein kinase C (PKC) and cAMP-dependent protein kinase (PKA) activities.: PKC and PKA activities are detected. Briefly, 5 mL of PKC or PKA is mixed with 5 mL of lipid preparation containing 100 mM phorbol 12-myristate 13-acetate, 2.8 mg/mL phosphatidyl serine, and Triton X-100 mixed micelles for PKC assay or 5 mL of 40 mM cAMP in 50 mM Tris-HCl, pH 7.5, for PKA assay, and 5 mL of daphnetin. The reaction is started by adding 10 mL of PKC substrate solution containing 250 mM acetylated myelin basic protein, 100 mM ATP, 5 mM CaCl2, 10 mM MgCl2, 20 mM Tris-HCl, pH 7.5, or 10 mL of PKA substrate solution containing 200 mM Kemptide, 400 mM ATP, 40 mM MgCl2, 1 mg/mL BSA, 50 mM Tris-HCl, pH 7.5, and 20-25 mCi/mL[g-32P] ATP. After incubation at 25 °C for 5 minutes, 20 mL of each mixture is spotted on a piece of phosphocellulose disc which is immediately put into 1% H3PO4. After free [g-32P] ATP on the discs is removed, the peptide-incorporated 32P on the discs is counted in a scintillation counte |
| 體外活性 | 在水迷宮測試和強(qiáng)迫游泳測試中,Daphnetin（2-8 mg/kg）可增強(qiáng)應(yīng)激小鼠的表現(xiàn). Daphnetin（140 mg/kg）可使子宮重量減少39.5%.Daphnetin可使P. yoelli感染小鼠的存活時間顯著延長. |
| 體內(nèi)活性 | Daphnetin（25-40 μM）對惡性瘧原蟲引起的次黃嘌呤摻入的抑制率可達(dá)50%。Daphnetin（50 μM）可使細(xì)胞周期蛋白D1的水平降低。地塞米松可影響皮質(zhì)神經(jīng)從而降低細(xì)胞活性,Daphnetin可劑量依賴地防止該作用。 Daphnetin能以特殊的方式劑量依賴性地抑制內(nèi)源或重組TaPRK的活性。Daphnetin既對表皮細(xì)胞生長因子受體催化的外源底物酪氨酸磷酸化具有明顯抑制作用,還對PKA和PKC的活性有抑制作用。Daphnetin處理24 h對MCF-7雌激素應(yīng)答的人類癌細(xì)胞系生長有抑制作用（IC50：73 μM）。Daphnetin對ERK1/ERK2促有絲分裂的信號傳導(dǎo)有抑制作用。 |
| 存儲條件 | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 55 mg/mL (308.75 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
|
| 關(guān)鍵字 | Autophagy | PARP | PKA | A2780 cells | mTOR | Protein kinase A | Inhibitor | Caspase | poly ADP ribose polymerase | PKB | inflammation | schizontocidal | Epidermal growth factor receptor | Protein kinase C | Reactive Oxygen Species | HER1 | Bcl-2 Family | Parasite | Protein kinase B | Akt | Mammalian target of Rapamycin | AMPK | Apoptosis | protein kinase | ErbB-1 | Daphnetin | inhibit | AMP-activated protein kinase | PKC | EGFR |
| 相關(guān)產(chǎn)品 | Guanidine hydrochloride | Naringin | Valproic Acid | Taurine | Gefitinib | Aceglutamide | Doxycycline | Hydroxychloroquine | Stavudine | Paeonol | Sodium 4-phenylbutyrate | Kojic acid |
| 相關(guān)庫 | 神經(jīng)保護(hù)化合物庫 | 抑制劑庫 | 激酶抑制劑庫 | 抗衰老化合物庫 | 膜蛋白靶向化合物庫 | 酪氨酸激酶分子庫 | 抗寄生蟲天然產(chǎn)物庫 | 藥物功能重定位化合物庫 | 高通量篩選天然產(chǎn)物庫 | 抗癌藥物庫 |