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  • Shikonin
  • 紫草素(混旋); C.I. 75535;Isoarnebin 4
  • 货号: abs814608
    CAS号: 517-89-5
    分子式: C16H16O5
    分子量: 288.3
    产品说明书
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    货号-规格 货期 价格 数量
    abs814608-25mg 1-2周 ¥788.00
    - +
    abs814608-100mg 1-2周 ¥2264.00
    - +
    abs814608-1g 1-2周 ¥5600.00
    - +
    ! 该货号为 abs42027231 的新货号。
    大包装询价
    产品描述
    描述

    Shikonin, a potent and specific Pyruvate kinase M2 (PKM2) inhibitor, is a major component of zicao (purple gromwell, the dried root of Lithospermum erythrorhizon), a Chinese herbal medicine with various biological activities. It is also an inhibitor of TMEM16A chloride channel activity using cell-based fluorescent-quenching assay.

    纯度
    ≥98%
    储存/保存方法
    Store at -20°C
    基本信息
    别名
    紫草素(混旋); C.I. 75535;Isoarnebin 4
    外观
    red powder
    可溶性/溶解性
    DMSO : ≥ 31 mg/mL (107.53 mM)
    生物活性
    靶点
    TMEM16A chloride channel,PKM2,NF-κB,TNF-α
    In vitro(体外研究)
    Shikonin (>50 μM) markedly inhibits normal human keratinocytes (NHKs) viability, compare with that of control (P<0.05). Pretreatment with Shikonin for 2 h attenuates TNF-α-induced NF-κB p65 nuclear translocation. Shikonin (5/7.5 μM) markedly inhibits the cell viability starting from 12 h and the inhibitory effects are presented in time-dependent patterns compare with the 0 h group in both cell lines. It is found that 5 μM Shikonin displays greater inhibition compare to 2.5 μM at the time points from 24 to 48 h. The invasiveness of U87 and U251 cells is significantly attenuated when treated with Shikonin (2.5/5/7.5 μM) compare with the control group at 24 and 48 h (p<0.01).
    In vivo(体内研究)
    Shikonin markedly inhibits the increase in TNF-α and IL-1β expression levels in the rat model of osteoarthritis, compared with those in the osteoarthritis group (P<0.01). The NF-κB protein expression level is significantly suppressed by Shikonin in the rat model of osteoarthritis, compare with that in the osteoarthritis group (P<0.01). The induction of the iNOS level is suppressed by treatment with Shikonin in the rat model of osteoarthritis, compare with that in the osteoarthritis group (P<0.01). The administration of Shikonin markedly weakens the up-regulation of COX-2 protein expression in the rat model of osteoarthritis, as compared with that in the osteoarthritis group (P<0.01). The elevation of caspase-3 activity is significantly reduced by Shikonin treatment in the rat model of osteoarthritis, compare with that in the osteoarthritis group (P<0.01). The downregulation of Akt phosphorylation is also significantly recovered by treatment with Shikonin in the rat model of osteoarthritis, compared with that in the osteoarthritis group (P<0.01).
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