Shikonin (C.I. 75535)

Catalog No.S8279 Synonyms: Anchusin, Anchusa acid, Alkanna Red, Isoarnebin 4, NSC 252844

For research use only.

Shikonin (C.I. 75535, Anchusin, Anchusa acid, Alkanna Red, Isoarnebin 4, NSC 252844), 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. Shikonin exerts an anti-inflammatory effect by inhibiting tumor necrosis factor-α (TNF-α) and prevents activation of nuclear factor-κB (NF-κB) pathway via proteasome inhibition.

Shikonin (C.I. 75535) Chemical Structure

CAS No. 54952-43-1

Selleck's Shikonin (C.I. 75535) has been cited by 19 publications

Purity & Quality Control

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Biological Activity

Description Shikonin (C.I. 75535, Anchusin, Anchusa acid, Alkanna Red, Isoarnebin 4, NSC 252844), 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. Shikonin exerts an anti-inflammatory effect by inhibiting tumor necrosis factor-α (TNF-α) and prevents activation of nuclear factor-κB (NF-κB) pathway via proteasome inhibition.
Targets
chemokine receptor [1] TNF-α [4] Proteasome [4] NF-κB [1] PKM2 [3]
(FBP absence)
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0.3 μM
In vitro

At nanomolar concentrations, shikonin inhibits monocyte chemotaxis and calcium flux in response to a variety of CC chemokines (CCL2 [monocyte chemoattractant protein 1], CCL3 [macrophage inflammatory protein 1α], and CCL5 [regulated upon activation, normal T-cell expressed and secreted protein]), the CXC chemokine (CXCL12 [stromal cell-derived factor 1α]), and classic chemoattractants (formylmethionyl-leucine-phenylalanine and complement fraction C5a). Shikonin down-regulates surface expression of CCR5, a primary HIV-1 coreceptor, on macrophages. The anti-HIV and anti-inflammatory activities of shikonin may be related to its interference with chemokine receptor expression and function[1]. Shikonin inhibits enterocyte calcium-activated chloride channels, the inhibitory effect is partially through inhibition of basolateral K+ channel activity[2].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A101D NIO2UVBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVjFd25mUW6qaXLpeIlwdiCxZjDoeY1idiCDMUCxSEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvODByN{GyNe69VS5? MkPiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVQ4OC9pPmPBUmdGWjxxYU6=
TE-441-T MWTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYTaSXkxUW6qaXLpeIlwdiCxZjDoeY1idiCWRT20OFEuXCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMECyNlM5|ryPLh?= MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5OFcxNyd-U1HOS2VTRC:jPh?=
NALM-6 NXPUWHBYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{Lye2lvcGmkaYTpc44hd2ZiaIXtZY4hVkGOTT22JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xODJ5OUhOwG0v NX7EUVNbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTR5MD:nQnNCVkeHUkyvZV4>
SW1710 MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnXuTY5pcWKrdHnvckBw\iCqdX3hckBUXzF5MUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlAxOjlzzszNMi=> Mn\nQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVQ4OC9pPmPBUmdGWjxxYU6=
ST486 NH7BUIRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1v0RmlvcGmkaYTpc44hd2ZiaIXtZY4hW1R2OE[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlAxPjF5Od88UU4> MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5OFcxNyd-U1HOS2VTRC:jPh?=
SK-UT-1 MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFvnZWxKdmirYnn0bY9vKG:oIHj1cYFvKFONLWXUMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjByN{SzPO69VS5? NYHqcHRYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTR5MD:nQnNCVkeHUkyvZV4>
A253 Mk\mS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1z5W2lvcGmkaYTpc44hd2ZiaIXtZY4hSTJ3MzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNFA4PDl|zszNMi=> M1fw[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk1PzBxJ{7TRW5ITVJ:L3G+
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MDA231 M4\MWGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MlnKNlQhcHK| MofKRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGyN|Eh[2WubIOgZYZ1\XJiMkSgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD16Lke1{txONg>? MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTJ4OEGzNEc,Ojl{NkixN|A9N2F-
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PBMC NFXCdWdEgXSxdH;4bYNqfHliYYPzZZk> MUSyOEBpenN? NVTuU4QyS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWEKPQzDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[2WubDD2bYFjcWyrdImgbY5kfWKjdHXkJIZweiB{NDDodpMh[nliQ3XscHRqfGW{LVfsc{BtfW2rbnXzZ4VvfCClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13zszNMi=> NE\4S2M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUW2N|AyOyd-M{G1OlMxOTN:L3G+
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Sf9 NUjsRnZHTnWwY4Tpc44h[XO|YYm= MmnlN|AhdWmwcx?= NVTUOpZDUW6qaXLpeIlwdiCxZjDDMZRmem2rbnHsJGhqey22YXfn[YQhVi22ZYLtbY5idCCJU2SteIFo\2WmIHj1cYFvKEWJRmKgLFY3QCC2bzCxNlExKHKnc3nkeYV{MSCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhW2Z7IHPlcIx{KGGodHXyJFMxKG2rboOgbY4heHKnc3XuZ4Uhd2ZiZ3HtcYEuYzN{cD3BWHBeKGKrbnTpcoch[XO|YYmsJGlEPTB;MD6xN|kz|ryPLh?= MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTZ2OEi3O{c,OzF4NEi4O|c9N2F-
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LO2 M2\ocmN6fG:2b4jpZ4l1gSCjc4PhfS=> Ml23NlQhcHK| MX7DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDMU|Ih[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGGodHXyJFI1KGi{czDifUBOXFRiYYPzZZktKEOFNUC9NVIvOs7:TT6= M4ThUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNkS4PFc4Lz5|MU[0PFg4PzxxYU6=
Assay
Methods Test Index PMID
Western blot Bcl2 / Bax / CytC / Apaf1 / AIF / Caspase-9 / Caspase-3 / Caspase-7 ; p-PERK / PERK / p-eIF2α / eIF2α / GRP78 / CHOP ; MMP-2 / MMP-9 ; p-β-catenin / β-catenin 25879420 26473829
Growth inhibition assay Cell viability 25879420
In vivo

Shikonin significantly delays intestinal motility in mice and reduces stool water content in a neonatal mice model of rotaviral diarrhea without affecting the viral infection process in vivo. Shikonin has been reported to have antioxidant, antibacterial, antiparasitic, antiviral and wound-healing activities. Shikonin inhibits allergic action as well as tracheal hyperresponsiveness in vivo. Intraperitonal injection of shikonin has been demonstrated to result in some toxicity, with an LD50 of 20 mg/kg. Shikonin absorption is fast if given by oral gavage and muscle injection, as it is barely detected in the plasma after 1 min, with a oral gavage yielding a bioavailability of about 34%[2].

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: Human monocytes
  • Concentrations: 10, 1, 0.1, 0.01 μM
  • Incubation Time: 12 and 24 hours
  • Method:

    Freshly isolated human monocytes are plated in a 96-microwell plate (Costar) at 105 cells per well with shikonin at a final concentration of 10, 1, 0.1, 0.01 μM. The numbers of viable cells, as detected by MTS test and the trypan blue exclusion assay, were measured 12 and 24 h after incubation at 37°C in humidified air with 5% CO2.

Animal Research:

[2]

  • Animal Models: Neonatal ICR mice
  • Dosages: 0.4 and 1.7 μg in 30 μL PBS
  • Administration: oral administration

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5% DMSO+40% PEG 300+5% Tween 80+50% ddH2O
For best results, use promptly after mixing.

0.23mg/mL

Chemical Information

Molecular Weight 288.30
Formula

C16H16O5

CAS No. 54952-43-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(=CCC(C1=CC(=O)C2=C(C=CC(=C2C1=O)O)O)O)C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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