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CAS No.: 486-35-1

瑞香素 Catalog No. CSN10745

Synonyms: 7,8-Dihydroxycoumarin;NSC 633563;瑞香素

Daphnetin is an inhibitor of EGFR, PKA and PKC with IC50 of 7.67 μM, 9.33 μM and 25.01 μM respectively. It derives from plants of the genus Daphne.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 EGFR

IC50:7.67μM PKA

IC50:9.33μM PKC

IC50:25.01μM
描述Daphnetin (7,8-dihydroxycoumarin, DAP) is a 7, 8 dihydroxy coumarin isolated from different medicinal plants of the Thymelaeaceae family and exhibits copious pharmacological activities including neuroprotection, anti-cancer, anti-malarial, anti-inflammatory, anti-parasitic and anti-arthritic activity, The inhibition of EGF receptor tyrosine kinase by daphnetin was competitive to ATP and non-competitive to the peptide substrate^[3]. DAP markedly decreased cell viability and induced the apoptosis of CIA-FLS along with typical morphological and ultrastructural changes; moreover, DAP increased FasL, cytochrome c (Cyt-c), Bax, caspase-3, caspase-8, and caspase-9 mRNA expression and Bax, caspase-3, caspase-8, and caspase-9 protein expression^[4]. Daphnetin attenuated H2O2-induced apoptosis in a concentration-dependent manner, reduced the cleavage of poly ADP ribose polymerase and caspase 3, and inhibited the phosphorylation of p38 MAPK and c-Jun N-terminal kinases (JNK) in H2O2-induced PC12 cells. In addition, daphnetin induced the expression of HSP70 in a dose- and time-dependent manner, and daphnetin-induced HSP70 expression was reduced by ERK 1/2 inhibitor U0126 in PC12 cells^[5]. Both in vitro and in vivo results indicate that DAP exerts a protective effect against IL-1β in chondrocytes. In vitro ,DAP inhibits the expression of IL-6, IL-12, MMP-3, MMP-9 and MMP-13, induced by IL-1β in rabbit chondrocytes, and stimulates the production of IL-10. The inhibitory effect of DAP on the MMPs is partially regulated by the inhibition of the PI3K/AKT, MAPK and NF-κB signaling pathways. The effect of DAP on OA may be attributed to the suppression of inflammatory factor secretion, chondrocyte apoptosis observed by the decrease in pro-apoptotic Caspase-3 and BAX, and the activation of anti-apoptotic BCL-2^[6].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 5.6135 mL
- 28.0676 mL
- 56.1352 mL
- 5 mM
- 1.1227 mL
- 5.6135 mL
- 11.2270 mL
- 10 mM
- 0.5614 mL
- 2.8068 mL
- 5.6135 mL

技术信息

CAS号

486-35-1

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C9H6O4

运输

蓝冰

分子量

178.14

别名

7,8-Dihydroxycoumarin;NSC 633563;瑞香素

溶解度

DMSO	35.0 mg/mL (196.5 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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靶点	Description	IC50
EGFR		IC50:7.67μM
PKA		IC50:9.33μM
PKC		IC50:25.01μM

瑞香素 Catalog No. CSN10745

靶点选择性

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