(R)-Shikonin

Key Product Details

Product Description

(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.

Product Specifications for (R)-Shikonin

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for (R)-Shikonin

The following data is based on the product molecular weight 288.30.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	3.47 mL	17.34 mL	34.69 mL
5 mM	0.69 mL	3.47 mL	6.94 mL
10 mM	0.35 mL	1.73 mL	3.47 mL
50 mM	0.07 mL	0.35 mL	0.69 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Zhao Shikonin inhibits tumor growth in mice by suppressing pyruvate kinase M2-mediated aerobic glycolysis. Sci.Rep. 2018 PMID: 30266938
• Chen Shikonin, a Component of Chinese Herbal Medicine, Inhibits Chemokine Receptor Function and Suppresses Human Immunodeficiency Virus Type 1 Antimicrob. Agents Chemother. 2003 PMID: 12936978
• Kim The efficacy of shikonin on cartilage protection in a mouse model of rheumatoid arthritis. Korean J.Physiol.Pharmacol. 2010 PMID: 20827333
• Han Shikonin circumvents cancer drug resistance by induction of a necroptotic death. Mol. Cancer Ther. 2007 PMID: 17513612
• Chen Shikonin and its analogs inhibit cancer cell glycolysis by targeting tumor pyruvate kinase-M2. Oncogene 2011 PMID: 21516121
• Hafner-Bratkovic NLRP3 lacking the leucine-rich repeat domain can be fully activated via the canonical inflammasome pathway. Nat.Commun. 2018 PMID: 30518920
• Nigorikawa A naphthoquinone derivative, shikonin, has insulin-like actions by inhibiting both phosphatase and tensin homolog deleted on chromosome 10 and tyrosine phosphatases. Mol.Pharmacol. 2006 PMID: 16804092
• McLoughlin The therapeutic potential of PTEN modulation: targeting strategies from gene to protein. Cell Chem.Biol. 2018 PMID: 29153852

Product Documents for (R)-Shikonin