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抑制剂描述:

产品名称:Daphnetin

产品别名:见爱必信官网

英文别名:Daphnetin

靶点:EGFR

CAS:486-35-1

纯度:98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Daphnetin, a natural coumarin derivative, is a protein kinase inhibitor, inhibits EGFR, PKA and PKC with IC50 of 7.67 μM, 9.33 μM and 25.01 μM, respectively, also known to exhibit anti-inflammatory and anti-oxidant activities.

溶解性:DMSO : 33 mg/mL (185.2 mM)

体外研究:

Daphnetin strongly inhibits not only EGF receptor-catalyzed tyrosine phosphorylation of exogenous substrate but also PKA and PKC activities. Daphnetin inhibits MCF-7 estrogen-responsive human carcinoma cell line at 24-hour exposure with IC50 of 73 μM. Daphnetin reduces the level of cyclin D1 even at 50 μM. Daphnetin protects the cortical neurons against dexamethasone-induced reduction of cell viability in a dose-dependent manner. Daphnetin inhibits the activities of endogenous or recombinant TaPRK in a specific and dose-dependent manner. daphnetin causes a 50% inhibition (IC50) of 3H-hypoxanthine incorporation by Plasmodium falciparum at concentrations between 25 μM and 40 μM. Daphnetin inhibits the mitogenic signalling of ERK1/ERK2.

体内研究:Daphnetin at 140 mg/kg significantly decreases uterine weights by 39.5%. Two and 8 mg/kg administration of Daphnetin could improve the performance of stress mice in Morris water maze tests and forced swimming tests. Daphnetin significantly prolongs survival of P. yoelli-infected mice.

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