Shikonin (C.I. 75535)

For research use only. Not for use in humans.

目录号:S8279 别名: Anchusin, Anchusa acid, Alkanna Red, Isoarnebin 4, NSC 252844 中文名称:紫草素

Shikonin (C.I. 75535) Chemical Structure

CAS No. 54952-43-1

Shikonin (C.I. 75535, Anchusin, Anchusa acid, Alkanna Red, Isoarnebin 4, NSC 252844)是一种 Pyruvate kinase M2 (PKM2) 有效的、特异的抑制剂。它是紫草的主要成分,紫草是一种中草药,具有多种生物活性。在细胞荧光淬灭试验中,Shikonin也是TMEM16A氯离子通道的抑制剂。Shikonin 通过抑制 tumor necrosis factor-α (TNF-α) 发挥抗炎作用,并可通过抑制 proteasome 来阻止 nuclear factor-κB (NF-κB) 信号途径的激活。

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RMB 2433.41 现货
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客户使用Selleck生产的Shikonin (C.I. 75535)发表文献10篇:

产品安全说明书

PKM抑制剂选择性比较

生物活性

产品描述 Shikonin (C.I. 75535, Anchusin, Anchusa acid, Alkanna Red, Isoarnebin 4, NSC 252844)是一种 Pyruvate kinase M2 (PKM2) 有效的、特异的抑制剂。它是紫草的主要成分,紫草是一种中草药,具有多种生物活性。在细胞荧光淬灭试验中,Shikonin也是TMEM16A氯离子通道的抑制剂。Shikonin 通过抑制 tumor necrosis factor-α (TNF-α) 发挥抗炎作用,并可通过抑制 proteasome 来阻止 nuclear factor-κB (NF-κB) 信号途径的激活。
靶点
chemokine receptor [1]
()
TNF-α [4]
()
Proteasome [4]
()
NF-κB [1]
()
PKM2 [3]
(FBP absence)
0.3 μM
体外研究

在摩尔浓度下,shikonin在多种CC趋化因子(CCL2单核细胞趋化蛋白1), CCL3(巨噬细胞炎性蛋白1α),CCL5(活性调节蛋白,正常T细胞表达并分泌的蛋白),CXC趋化因子(CXCL12基质细胞衍生因子1α)以及经典的化学引诱物的影响的情况下抑制单核细胞趋化性以及钙流动。Shikonin下调巨噬细胞表面CCR5(主要的HIV-1协同受体)的表达。Shikonin 的抗HIV和抗炎症活性可能与它干扰趋化因子受体的表达和功能相关[1]。Shikonin抑制肠上皮细胞钙激活的氯离子通道,这一抑制效应部分通过抑制基地侧的钾离子通道活性来实现[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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NALM-6 NFftVFZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3rWcmlvcGmkaYTpc44hd2ZiaIXtZY4hVkGOTT22JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xODJ5OUhOwG0v NWjOb|A6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTR5MD:nQnNCVkeHUkyvZV4>
SW1710 NEPXfWZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUXJcohq[mm2aX;uJI9nKGi3bXHuJHNYOTdzMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNFAzQTIQvF2u MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5OFcxNyd-U1HOS2VTRC:jPh?=
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CAL-51 MlzQS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYnaTmQxUW6qaXLpeIlwdiCxZjDoeY1idiCFQVytOVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjB{MEi1{txONg>? MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5OFcxNyd-U1HOS2VTRC:jPh?=
GCIY MkjxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoHVTY5pcWKrdHnvckBw\iCqdX3hckBIS0m\IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6wN|U6QM7:TT6= MnTvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVQ4OC9pPmPBUmdGWjxxYU6=
SK-PN-DW NV63coZpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXzjT3h5UW6qaXLpeIlwdiCxZjDoeY1idiCVSz3QUk1FXyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMEO2OVXPxE1w NX30flQzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTR5MD:nQnNCVkeHUkyvZV4>
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... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Bcl2 / Bax / CytC / Apaf1 / AIF / Caspase-9 / Caspase-3 / Caspase-7 ; 

PubMed: 25879420     


Shikonin treatment alters expression of mitochondrial proteins in DU-145 and PC-3 cells. Cells were treated with Shikonin for 0-24 h, expression of indicated mitochondrial proteins were performed as described in Methods. Experiments were repeated minimum two-four times.

p-PERK / PERK / p-eIF2α / eIF2α / GRP78 / CHOP ; 

PubMed: 25879420     


Shikonin treatment induces ER stress associated protein expression. Western blot experiments in prostate cancer cells treated with 2.5 μM of Shikonin increased the phosphorylation of PERK, and its substrate eIF2α, increased expression of GRP78/Bip and CHOP/GADD135 in a time-dependent manner.

MMP-2 / MMP-9 ; 

PubMed: 26473829     


Shikonin inhibited the expression and activity of MMP-2 and MMP-9. U87 and U251 cells were treated with shikonin at 2.5, 5, and 7.5 μmol/L for 48 h. Serum free DMEM served as a negative control. Expressions of MMP-2 and MMP-9 were checked with Western Blot. (A) Effects of shikonin on the expression of MMP-2 in U87 cells; (B) Effects of shikonin on the expression of MMP-9 in U87 cells; (C) The changing pattern of MMP-2 in U251 cells; (D) The changing pattern of MMP-9 in U251 cells; (E) Effects of shikonin on the activities of MMP-2 and MMP-9 in U87 cells; (F) Effects of shikonin on the activities of MMP-2 and MMP-9 in U251 cells. Statistical analysis showed that shikonin significantly reduced the expression levels and activity of both MMP-2 and MMP-9 proteins compared with the control group in a dose-dependent manner. * p < 0.05, ** p < 0.01 (compared with control group); # p < 0.05 (compared with 2.5 μmol/L groups) (n = 5).

p-β-catenin / β-catenin ; 

PubMed: 26473829     


(A) Western blot assay results of β-catenin and p-β-catenin Y333 in U87 cells. (D) Western blot assay results of β-catenin and p-β-catenin Ser45 in U87 cells.

25879420 26473829
Growth inhibition assay
Cell viability; 

PubMed: 25879420     


Shikonin treatment inhibits prostate cancer cell viability without affecting normal prostate epithelial cells. DU-145, PC-3 and PrEC cells were treated with various doses (0.5, 1, 2.5, 5 and 10 μM) of Shikonin for 24 h and CCK-8 assay was used for the measurement of cell viability.

25879420
体内研究

Shikonin在小鼠中显著延迟肠动力、在具有轮状病毒腹泻症状的新生小鼠模型中减少粪便含水量,而不影响病毒感染过程。Shikonin被报导具有抗氧化、抗菌、抗寄生物、抗病毒和伤口愈合活性。Shikonin在体内抑制过敏作用和气管高反应性。腹腔注射shikonin会导致一些毒性作用,LD50为20 mg/kg。如果通过口服和肌肉注射给药,shikonin的吸收速度很快,在给药后1分钟,在血浆中很少能检测shikonin。口服shikonin的生物利用度为34%[2]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:

[1]

- 合并
  • Cell lines: 人单核细胞
  • Concentrations: 10, 1, 0.1, 0.01 μM
  • Incubation Time: 12和24小时
  • Method:

    将新鲜分离的人单核细胞以105/孔的密度铺于96孔板中,加入终浓度为10, 1, 0.1, 0.01 μM的shikonin。孵育12或24小时后(37℃,5% CO2),活细胞的数量用MTS实验和台盼蓝拒染法检测。


    (Only for Reference)
动物实验:

[2]

- 合并
  • Animal Models: ICR新生小鼠
  • Dosages: 0.4 和 1.7 μg/30 μL PBS
  • Administration: 口服
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 57 mg/mL (197.71 mM)
Ethanol 23 mg/mL (79.77 mM)
Water Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
5% DMSO+40% PEG 300+5% Tween 80+50% ddH2O
0.23mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 288.30
化学式

C16H16O5

CAS号 54952-43-1
储存条件 粉状
溶于溶剂
别名 Anchusin, Anchusa acid, Alkanna Red, Isoarnebin 4, NSC 252844

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

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