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    产品编号 CFN92622
    CAS编号 517-89-5
    分子式 = 分子量 C16H16O5 = 288.3
    产品纯度 >=98%
    物理属性 Powder
    化合物类型 Quinones
    植物来源 The roots of Lithosperraum erythrorhizon Sieb. et Zucc.
    产品名称 产品编号 CAS编号 包装 QQ客服
    紫草素 CFN92622 517-89-5 10mg QQ客服:2932563308
    紫草素 CFN92622 517-89-5 20mg QQ客服:2932563308
    紫草素 CFN92622 517-89-5 50mg QQ客服:2932563308
    紫草素 CFN92622 517-89-5 100mg QQ客服:2932563308
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    Cell. 2018 Jan 11;172(1-2):249-261.e12.
    doi: 10.1016/j.cell.2017.12.019.

    PMID: 29328914

    Cell Metab. 2020 Mar 3;31(3):534-548.e5.
    doi: 10.1016/j.cmet.2020.01.002.

    PMID: 32004475

    Mol Cell. 2017 Nov 16;68(4):673-685.e6.
    doi: 10.1016/j.molcel.2017.10.022.

    PMID: 29149595

    ACS Nano. 2018 Apr 24;12(4): 3385-3396.
    doi: 10.1021/acsnano.7b08969.

    PMID: 29553709

    Nature Plants. 2016 Dec 22;3: 16206.
    doi: 10.1038/nplants.2016.205.

    PMID: 28005066

    Sci Adv. 2018 Oct 24;4(10): eaat6994.
    doi: 10.1126/sciadv.aat6994.

    PMID: 30417089
  • Uniwersytet Medyczny w ?odzi (Poland)
  • Instytut Nawozów Sztucznych w Pu?awach (Poland)
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  • Shanghai Institute of Biochemistry and Cell Biology (China)
  • Srinakharinwirot University (Thailand)
  • Universidade de Franca (Brazil)
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  • Julius Kühn-Institut (Germany)
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  • 生物活性
    Description: Shikonin(Shikonine), a potent and specific Pyruvate kinase M2 (PKM2) inhibitor, has antibacterial, antitumor, and anti-inflammatory effects, it provides neuroprotection by reducing the release of various proinflammatory molecules from activated microglia. Shikonin can inhibit VEGF-induced angiogenesis and suppress tumor growth in lewis lung carcinoma-bearing mice.
    Targets: Antifection | VEGFR | PKM2 | Cdk4 | HIV | CXCR4
    In vitro:
    Oncogene, 2011, 30(42):4297-306.
    Shikonin and its analogs inhibit cancer cell glycolysis by targeting tumor pyruvate kinase-M2.[Pubmed: 21516121]
    We recently reported that shikonin(Shikonine) and its analogs were a class of necroptotic inducers that could bypass cancer drug resistance. However, the molecular targets of shikonin are not known.
    Here, we showed that shikonin and its analogs are inhibitors of tumor-specific pyruvate kinase-M2 (PKM2), among which shikonin and its enantiomeric isomer alkannin were the most potent and showed promising selectivity, that is, shikonin and alkannin at concentrations that resulted in over 50% inhibition of PKM2 activity did not inhibit PKM1 and pyruvate kinase-L (PKL). Shikonin and alkannin significantly inhibited the glycolytic rate, as manifested by cellular lactate production and glucose consumption in drug-sensitive and resistant cancer cell lines (MCF-7, MCF-7/Adr, MCF-7/Bcl-2, MCF-7/Bcl-x(L) and A549) that primarily express PKM2. HeLa cells transfected with PKM1 showed reduced sensitivity to shikonin- or alkannin-induced cell death. To the best of our knowledge, shikonin and alkannin are the most potent and specific inhibitors to PKM2 reported so far.
    As PKM2 universally expresses in cancer cells and dictates the last rate-limiting step of glycolysis vital for cancer cell proliferation and survival, enantiomeric shikonin and alkannin may have potential in future clinical application.
    Front Pharmacol. 2016 Aug 23;7:270.
    Shikonin Inhibits Intestinal Calcium-Activated Chloride Channels and Prevents Rotaviral Diarrhea.[Pubmed: 27601995 ]
    Secretory diarrhea remains a global health burden and causes major mortality in children. There have been some focuses on antidiarrheal therapies that may reduce fluid losses and intestinal motility in diarrheal diseases.
    In the present study, we identified shikonin(Shikonine) as an inhibitor of TMEM16A chloride channel activity using cell-based fluorescent-quenching assay. The IC50 value of shikonin was 6.5 μM. Short-circuit current measurements demonstrated that shikonin inhibited Eact-induced Cl(-) current in a dose-dependent manner, with IC50 value of 1.5 μM. Short-circuit current measurement showed that shikonin exhibited inhibitory effect against CCh-induced Cl(-) currents in mouse colonic epithelia but did not affect cytoplasmic Ca(2+) concentration as well as the other major enterocyte chloride channel conductance regulator. Characterization study found that shikonin inhibited basolateral K(+) channel activity without affecting Na(+)/K(+)-ATPase activities. In vivo studies revealed that shikonin significantly delayed intestinal motility in mice and reduced stool water content in a neonatal mice model of rotaviral diarrhea without affecting the viral infection process in vivo.
    Taken together, the results suggested that shikonin inhibited enterocyte calcium-activated chloride channels, the inhibitory effect was partially through inhbition of basolateral K(+) channel activity, and shikonin could be a lead compound in the treatment of rotaviral secretory diarrhea.
    In vivo:
    PLoS One. 2015 May 11;10(5):e0126459.
    Shikonin Suppresses Skin Carcinogenesis via Inhibiting Cell Proliferation.[Pubmed: 25961580 ]
    The M2 isoform of pyruvate kinase M2 (PKM2) has been shown to be up-regulated in human skin cancers.
    To test whether PKM2 may be a target for chemoprevention, shikonin(Shikonine), a natural product from the root of Lithospermum erythrorhizon and a specific inhibitor of PKM2, was used in a chemically-induced mouse skin carcinogenesis study. The results revealed that shikonin treatment suppressed skin tumor formation. Morphological examinations and immunohistochemical staining of the skin epidermal tissues suggested that shikonin inhibited cell proliferation without inducing apoptosis. Although shikonin alone suppressed PKM2 activity, it did not suppress tumor promoter-induced PKM2 activation in the skin epidermal tissues at the end of the skin carcinogenesis study. To reveal the potential chemopreventive mechanism of shikonin, an antibody microarray analysis was performed, and the results showed that the transcription factor ATF2 and its downstream target Cdk4 were up-regulated by chemical carcinogen treatment; whereas these up-regulations were suppressed by shikonin. In a promotable skin cell model, the nuclear levels of ATF2 were increased during tumor promotion, whereas this increase was inhibited by shikonin. Furthermore, knockdown of ATF2 decreased the expression levels of Cdk4 and Fra-1 (a key subunit of the activator protein 1.
    In summary, these results suggest that shikonin, rather than inhibiting PKM2 in vivo, suppresses the ATF2 pathway in skin carcinogenesis.
    1 mg 5 mg 10 mg 20 mg 25 mg
    1 mM 3.4686 mL 17.343 mL 34.6861 mL 69.3722 mL 86.7152 mL
    5 mM 0.6937 mL 3.4686 mL 6.9372 mL 13.8744 mL 17.343 mL
    10 mM 0.3469 mL 1.7343 mL 3.4686 mL 6.9372 mL 8.6715 mL
    50 mM 0.0694 mL 0.3469 mL 0.6937 mL 1.3874 mL 1.7343 mL
    100 mM 0.0347 mL 0.1734 mL 0.3469 mL 0.6937 mL 0.8672 mL
    * Note: If you are in the process of experiment, it's need to make the dilution ratios of the samples. The dilution data of the sheet for your reference. Normally, it's can get a better solubility within lower of Concentrations.
    产品名称 产品编号 CAS编号 分子式 = 分子量 位单 联系QQ
    乙酰氧基异戊酰阿卡宁; Acetoxyisovalerylalkannin CFN92025 69091-17-4 C23H26O8 = 430.5 20mg QQ客服:3257982914
    黄钟花醌; Lapachol CFN97403 84-79-7 C15H14O3 = 242.3 20mg QQ客服:3257982914
    去氧紫草素; Deoxyshikonin CFN92024 43043-74-9 C16H16O4 = 272.3 20mg QQ客服:2056216494
    紫草素; Shikonine CFN92622 517-89-5 C16H16O5 = 288.3 20mg QQ客服:1413575084
    紫草素; Shikonin CFN99907 517-88-4 C16H16O5 = 288.31 20mg QQ客服:3257982914
    乙酰紫草素; Acetylshikonin CFN90308 54984-93-9 C18H18O6 = 330.33 20mg QQ客服:2159513211
    异丁酰紫草; Isobutylshikonin CFN92023 52438-12-7 C20H22O6 = 358.4 10mg QQ客服:1413575084
    β,β-二甲基丙烯酰紫草素; Dimethylacrylshikonin CFN90164 24502-79-2 C21H22O6 = 370.39 20mg QQ客服:1457312923
    β,β-二甲基丙烯酰阿卡宁; Beta,beta-Dimethylacrylalkannin CFN90626 34539-65-6 C21H22O6 = 370.4 20mg QQ客服:1413575084
    异戊酰紫草素; Isovalerylshikonin CFN95222 52387-14-1 C21H24O6 = 372.4 10mg QQ客服:3257982914





    在线QQ1: 2056216494 ; QQ2: 3257982914


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