Daphnetin

CAS No. 486-35-1

Daphnetin( 7,8-Dihydroxycoumarin | NSC 633563 )

Catalog No. M14627 CAS No. 486-35-1

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.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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10MG 39 In Stock
25MG 78 In Stock
50MG 152 In Stock
100MG 230 In Stock
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Biological Information

  • Product Name
    Daphnetin
  • Note
    Research use only, not for human use.
  • Brief 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.
  • 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.(In Vitro):Daphnetin (7,8-dihydroxycoumarin) (0-40 μg/mL; 24-48 hours) inhibits the proliferation of ovarian cancer cells.Daphnetin (7,8-dihydroxycoumarin) (0-40 μg/mL; 24 hours; A2780 cells) induces apoptosis and increases ROS production in a dose-dependent manner.Daphnetin (7,8-dihydroxycoumarin) (0-40 μg/mL; 24 hours; A2780 cells) induces autophagy through modulation of the AMPK/Akt/mTOR pathway.Daphnetin (7,8-dihydroxycoumarin) (1-10 μM; plasmodium falciparum) exhibits schizontocidal activity in a dose-dependent manner. (In Vivo):Daphnetin (7,8-dihydroxycoumarin) (30 mg/kg; i.p.; daily; for 12 days; BALB/c nude mice) has antitumour activities in a xenograft animal model.Daphnetin (7,8-dihydroxycoumarin) (2.5-10 mg/kg; i.p.; daily; for three days; C57BL/6 mice) inhibits cisplatin-induced inflammation, decreases TNF-α, IL-1β, ROS and MDA production in a dose-dependent manner in kidney tissues. Daphnetin inhibits cisplatin-induced NF-κB activation and up-regulated Nrf2 and HO-1.Daphnetin (7,8-dihydroxycoumarin) (10-100 mg/kg; i.g. and i.p.; every four days, for 30 days; male Kunming outbred strain mice) displays certain schizontocidal activity in vivo.
  • In Vitro
    Daphnetin (7,8-dihydroxycoumarin) (0-40 μg/mL; 24-48 hours) inhibits the proliferation of ovarian cancer cells.Daphnetin (7,8-dihydroxycoumarin) (0-40 μg/mL; 24 hours; A2780 cells) induces apoptosis and increases ROS production in a dose-dependent manner.Daphnetin (7,8-dihydroxycoumarin) (0-40 μg/mL; 24 hours; A2780 cells) induces autophagy through modulation of the AMPK/Akt/mTOR pathway.Daphnetin (7,8-dihydroxycoumarin) (1-10 μM; plasmodium falciparum) exhibits schizontocidal activity in a dose-dependent manner. Cell Viability Assay Cell Line:IOSE8C, A2780, SKOV3 and OVCAR8 cells Concentration:0, 5, 10, 20 and 40 μg/mL Incubation Time:24 h and 48 hours Result:Inhibited growth in ovarian cancer cells but not in normal cells.Apoptosis AnalysisCell Line:A2780 and SKOV3 cells Concentration:0, 10, 20 and 40 μg/mL Incubation Time: 24 hours Result:Increased apoptosis in a dose-dependent manner in A2780 and SKOV3 cells.Western Blot Analysis Cell Line:A2780 and SKOV3 cells Concentration:0, 10, 20 and 40 μg/mL Incubation Time:24 hours Result:Increased proapoptotic protein (Caspase 3, Bax, and PARP) expression but decreased antiapoptotic protein (Bcl2) expression.Western Blot Analysis Cell Line:A2780 cells Concentration:0, 10, 20 and 40 μg/mL Incubation Time:24 hours Result:Increased LC3 II and p62 expression in a dose-dependent manner and reduced the expression levels of p-Akt, p-mTOR, but increased the expression level of p-AMPK.
  • In Vivo
    Daphnetin (7,8-dihydroxycoumarin) (30 mg/kg; i.p.; daily; for 12 days; BALB/c nude mice) has antitumour activities in a xenograft animal model.Daphnetin (7,8-dihydroxycoumarin) (2.5-10 mg/kg; i.p.; daily; for three days; C57BL/6 mice) inhibits cisplatin-induced inflammation, decreases TNF-α, IL-1β, ROS and MDA production in a dose-dependent manner in kidney tissues. Daphnetin inhibits cisplatin-induced NF-κB activation and up-regulated Nrf2 and HO-1.Daphnetin (7,8-dihydroxycoumarin) (10-100 mg/kg; i.g. and i.p.; every four days, for 30 days; male Kunming outbred strain mice) displays certain schizontocidal activity in vivo. Animal Model:BALB/c nude mice Dosage:30 mg/kg Administration:Intraperitoneal injection; Daily; for 12 days Result:Decreased tumor volume and weight in a xenograft animal model.Animal Model:Male Kunming outbred strain mice Dosage:10, 50 or 100 mg/kg Administration:Oral gavage and intraperitoneal injection; every four days, for 30 days Result:Reduced the number of parasites in mice.
  • Synonyms
    7,8-Dihydroxycoumarin | NSC 633563
  • Pathway
    Angiogenesis
  • Target
    EGFR
  • Recptor
    EGFR| PKA| PKC
  • Research Area
    Inflammation/Immunology
  • Indication
    ——

Chemical Information

  • CAS Number
    486-35-1
  • Formula Weight
    178.14
  • Molecular Formula
    C9H6O4
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: 35 mg/mL (196.47 mM)
  • SMILES
    O=C1C=CC2=CC=C(O)C(O)=C2O1
  • Chemical Name
    7,8-dihydroxy-2H-1-benzopyran-2-one

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Yang EB, et al. Biochem Biophys Res Commun, 1999, 260(3), 682-685.
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