|Source:||The roots of Lithosperraum erythrorhizon Sieb. et Zucc.|
|Biological Activity or Inhibitors:||1. Shikonin and alkannin are the most potent and specific inhibitors to tumor-specific pyruvate kinase-M2 (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.
2. Shikonin, a naphthoquinone pigment from the root of Lithospermum erythrorhizon, it has antibacterial, antitumor, and anti-inflammatory effects, it provides neuroprotection by reducing the release of various proinflammatory molecules from activated microglia.
3. Shikonin can inhibit VEGF-induced angiogenesis and suppress tumor growth in lewis lung carcinoma-bearing mice.
|Solvent:||Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.|
|Storage:||Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months(2-8C).
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
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|After receiving:||The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.|
|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|
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 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.|