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说明： PTEN inhibitor; induces necroptosis; anti-inflammatory
化学名： 5,8-Dihydroxy-2-[(1R)-1-hydroxy-4-methyl-3-penten-1-yl]-1,4-naphthalenedione
纯度： ≥98% (HPLC)
生物活性 for (R)-Shikonin
(R)-Shikonin is a PTEN and inflammasome inhibitor. Inhibits PTEN's phosphatase activity (IC50 = 2.7 μM) and NLRP3 activation. Also blocks TNF-α and NF-κB signaling. Attenuates HIV-1 replication at nanomolar concentrations. (R)-Shikonin suppresses glycolysis in cancer cells by inhibiting tumor-specific pyruvate kinase M2 (PKM2) (IC50 = 0.3 μM) and inhibits tumor proliferation. Induces necroptosis in MCF-7 and HEK293 cancer cell lines. (R)-Shikonin also displays anti-inflammatory activity in a mouse model of collagen-induced arthritis.
技术数据 for (R)-Shikonin
| 分子量 | 288.3 |
| 公式 | C16H16O5 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 517-89-5 |
| PubChem ID | 479503 |
| InChI Key | NEZONWMXZKDMKF-SNVBAGLBSA-N |
| Smiles | C/C(C)=C\C[C@H](C1=CC(C2=C(C=CC(O)=C2C1=O)O)=O)O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
产品说明书 for (R)-Shikonin
参考文献 for (R)-Shikonin
参考文献是支持产品生物活性的出版物。
McLoughlin et al (2018) The therapeutic potential of PTEN modulation: targeting strategies from gene to protein. Cell Chem.Biol. 25 19 PMID: 29153852
Nigorikawa et al (2006) A naphthoquinone derivative, shikonin, has insulin-like actions by inhibiting both phosphatase and tensin homolog deleted on chromosome 10 and tyrosine phosphatases. Mol.Pharmacol. 70 1143 PMID: 16804092
Hafner-Bratkovic et al (2018) NLRP3 lacking the leucine-rich repeat domain can be fully activated via the canonical inflammasome pathway. Nat.Commun. 9 5182 PMID: 30518920
Chen et al (2011) Shikonin and its analogs inhibit cancer cell glycolysis by targeting tumor pyruvate kinase-M2. Oncogene 30 4297 PMID: 21516121
Han et al (2007) Shikonin circumvents cancer drug resistance by induction of a necroptotic death. Mol. Cancer Ther. 6 1641 PMID: 17513612
Chen et al (2003) Shikonin, a Component of Chinese Herbal Medicine, Inhibits Chemokine Receptor Function and Suppresses Human Immunodeficiency Virus Type 1 Antimicrob. Agents Chemother. 47 2810 PMID: 12936978
Kim et al (2010) The efficacy of shikonin on cartilage protection in a mouse model of rheumatoid arthritis. Korean J.Physiol.Pharmacol. 14 199 PMID: 20827333
Zhao et al (2018) Shikonin inhibits tumor growth in mice by suppressing pyruvate kinase M2-mediated aerobic glycolysis. Sci.Rep. 8 14517 PMID: 30266938
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关键词: (R)-Shikonin, (R)-Shikonin supplier, PTEN, inhibitors, inhibits, inducers, necroptosis, anti-inflammatory, NLRP3, TNF-α, NF-κB, HIV-1, replication, pyruvate, kinase, M2, PKM2, NF-kappaB, TNF-alpha, alfa, Protein, Tyrosine, Phosphatases, Inflammasomes, NF-kB/IkB, Cytokines, Other, Kinases, Necroptosis, HIV, 6829, Tocris Bioscience
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