Daphnetin - CAS 486-35-1
Catalog number:
486-35-1
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C9H6O4
Molecular Weight:
178.14
COA:
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Targets:
EGFR
Description:
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.
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Purity:
>98%
MSDS:
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1.Daphnetin inhibits invasion and migration of LM8 murine osteosarcoma cells by decreasing RhoA and Cdc42 expression.
Fukuda H1, Nakamura S2, Chisaki Y3, Takada T1, Toda Y4, Murata H5, Itoh K6, Yano Y3, Takata K1, Ashihara E7. Biochem Biophys Res Commun. 2016 Feb 26;471(1):63-7. doi: 10.1016/j.bbrc.2016.01.179. Epub 2016 Feb 1.
Daphnetin, 7,8-dihydroxycoumarin, present in main constituents of Daphne odora var. marginatai, has multiple pharmacological activities including anti-proliferative effects in cancer cells. In this study, using a Transwell system, we showed that daphnetin inhibited invasion and migration of highly metastatic murine osteosarcoma LM8 cells in a dose-dependent manner. Following treatment by daphnetin, cells that penetrated the Transwell membrane were rounder than non-treated cells. Immunofluorescence analysis revealed that daphnetin decreased the numbers of intracellular stress fibers and filopodia. Moreover, daphnetin treatment dramatically decreased the expression levels of RhoA and Cdc42. In summary, the dihydroxycoumarin derivative daphnetin inhibits the invasion and migration of LM8 cells, and therefore represents a promising agent for use against metastatic cancer.
2.Role of Daphnetin in Rat Severe Acute Pancreatitis Through the Regulation of TLR4/NF-[Formula: see text]B Signaling Pathway Activation.
Liu Z1,2, Liu J3,2, Zhao K1, Shi Q1, Zuo T1, Wang G2, Wang W1. Am J Chin Med. 2016 Feb;44(1):149-63. doi: 10.1142/S0192415X16500105.
Severe acute pancreatitis (SAP) often results in multiple-organ dysfunction syndrome with high mortality. There is no effective clinical therapy for SAP, yet daphnetin, a coumarin extracted from Dracaena marginata, has analgesic and anti-inflammatory effects, and has been used clinically in several diseases. The objective of this study was to investigate the role and underlying mechanisms of daphnetin in a rat SAP model. Male Wistar rats were pretreated with daphnetin via intraperitoneal injection, 30[Formula: see text]min before retrograde infusion of 5% sodium taurocholate into the biliopancreatic duct. Twelve hours after sodium taurocholate administration, rats were sacrificed and tissues and blood were harvested. Then, histological, chemical, and molecular analyses were performed. Daphnetin treatment reduced the levels of serum alanine transaminase and creatinine (CR), increased superoxide dismutase(SOD) activity, and decreased neutrophil infiltration and cell apoptosis of the pancreatic tissues in rat SAP.
3.[Dual role of daphnetin in suppressing HMGB1 release and HMGB1-induced inflammation in murine macrophage RAW264.7 cells and human monocytic THP-1 cells in vitro].
Qi Z1, Qi S, Ling L, Feng Z. Nan Fang Yi Ke Da Xue Xue Bao. 2015 Nov;35(11):1519-23.
OBJECTIVE: To investigate the dual role of daphnetin in suppressing high mobility group box-1 protein (HMGB1) release and blocking HMGB1-induced inflammatory response.
4.[Dual role of daphnetin in suppressing HMGB1 release and HMGB1-induced inflammation in murine macrophage RAW264.7 cells and human monocytic THP-1 cells in vitro].
Qi Z1, Qi S, Ling L, Feng Z. Nan Fang Yi Ke Da Xue Xue Bao. 2015 Nov;35(11):1519-23.
OBJECTIVE: To investigate the dual role of daphnetin in suppressing high mobility group box-1 protein (HMGB1) release and blocking HMGB1-induced inflammatory response.
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CAS 486-35-1 Daphnetin

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