Shikonin (C.I. 75535, Anchusin, Anchusa acid, Alkanna Red, Isoarnebin 4, NSC 252844) is an effective and specific inhibitor of Pyruvate kinase M2 (PKM2). Shikonin is the main ingredient of Lithosia, a Chinese herb with a variety of biological activities. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC50 of 6.5 μM. Shikonin acts as an anti-inflammatory by inhibiting tumor necrosis factor-α (TNF-α), and it can inhibit the activation of nuclear factor-κB (NF-κB) signaling pathway. Shikonin decreases exosome secretion through the inhibition of glycolysis. Shikonin also inhibits AIM2 inflammasome activation.
Molecular Weight | 288.30 |
Formula | C16H16O5 |
CAS Number | 517-89-5 |
Solubility (25°C) | DMSO 100 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Zhenzhen Mu, et al. Therapeutic Effects of Shikonin on Skin Diseases: A Review
[4] Joelle C Boulos, et al. Shikonin derivatives for cancer prevention and therapy
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