Shikonin (C.I. 75535)

For research use only.

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

10 publications

Shikonin (C.I. 75535) Chemical Structure

CAS No. 54952-43-1

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.

Selleck's Shikonin (C.I. 75535) has been cited by 10 publications

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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)
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 NFvPT|VIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NW[wdGh7UW6qaXLpeIlwdiCxZjDoeY1idiCDMUCxSEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvODByN{GyNe69VS5? M{jKUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk1PzBxJ{7TRW5ITVJ:L3G+
TE-441-T M3\nUGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MV\Jcohq[mm2aX;uJI9nKGi3bXHuJHRGNTR2MT3UJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xODJ{M{lOwG0v M{fNd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk1PzBxJ{7TRW5ITVJ:L3G+
NALM-6 NVvoPFVJT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUTCT5g5UW6qaXLpeIlwdiCxZjDoeY1idiCQQVzNMVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjByMke5O:69VS5? M3nTZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk1PzBxJ{7TRW5ITVJ:L3G+
SW1710 NXXCfVJOT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYnNWVg5UW6qaXLpeIlwdiCxZjDoeY1idiCVV{G3NVAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjByMkmx{txONg>? MoPPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVQ4OC9pPmPBUmdGWjxxYU6=
ST486 NV;UNoJyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWnJcohq[mm2aX;uJI9nKGi3bXHuJHNVPDh4IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6wNFYyPzoQvF2u NWDhT2hCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTR5MD:nQnNCVkeHUkyvZV4>
SK-UT-1 MkDPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFe4O|lKdmirYnn0bY9vKG:oIHj1cYFvKFONLWXUMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjByN{SzPO69VS5? M37pelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk1PzBxJ{7TRW5ITVJ:L3G+
A253 Mn7pS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MU\Jcohq[mm2aX;uJI9nKGi3bXHuJGEzPTNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkCwO|Q6O87:TT6= M2TLTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk1PzBxJ{7TRW5ITVJ:L3G+
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Bel7402 M3XiWWN6fG:2b4jpZ4l1gSCjc4PhfS=> NID2VmQ1QCCqcoO= M37tVGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGJmdDd2MEKgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0yNjJ2zszNMi=> MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF5NEixN{c,OjlzN{S4NVM9N2F-
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A549 MV;BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NVu4[GN2OjRiaILz MkjHRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDNUS5JINmdGy|IHHmeIVzKDJ2IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:Oy53M988UU4> NGT3fmM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUK2PFE{OCd-MkmyOlgyOzB:L3G+
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A549 NUDRfINHS3m2b4TvfIlkcXS7IHHzd4F6 MYKyOEBpenN? Moq2R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVU1QSClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliaX7jeYJifGWmIH\vdkAzPCCqcoOgZpkhS2WubGTpeIVzNUeubzDseY1qdmW|Y3XueEBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF04NjQQvF2u MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTV4M{CxN{c,OzF3NkOwNVM9N2F-
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Sf9 NWnZb|V1TnWwY4Tpc44h[XO|YYm= NWHpXFNSOzBibXnudy=> NUHGcpNVUW6qaXLpeIlwdiCxZjDDMZRmem2rbnHsJGhqey22YXfn[YQhVi22ZYLtbY5idCCJU2SteIFo\2WmIHj1cYFvKEWJRmKgLFY3QCC2bzCxNlExKHKnc3nkeYV{MSCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhW2Z7IHPlcIx{KGGodHXyJFMxKG2rboOgbY4heHKnc3XuZ4Uhd2ZiZ3HtcYEuYzN{cD3BWHBeKGKrbnTpcoch[XO|YYmsJGlEPTB;MD6xN|kz|ryPLh?= MkG0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzF4NEi4O|coRjNzNkS4PFc4RC:jPh?=
NCI-H1975 NWTJcYVtSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NYrjdGNmOjRiaILz M2rRbmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWgyQTd3IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBk\WyuII\pZYJqdGm2eTDh[pRmeiB{NDDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTRwMklOwG0v NYL2XHN7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{G2OFg5PzdpPkOxOlQ5QDd5PD;hQi=>
H460 M3;h[2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 NHrJWoEzPCCqcoO= NFr4OoxCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFi0OlAh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGGodHXyJFI1KGi{czDifUBOXFRiYYPzZZktKEmFNUC9OU4xPM7:TT6= NYfZTYQ4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{G2OFg5PzdpPkOxOlQ5QDd5PD;hQi=>
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HeLa MkPoRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NX3D[Xp[OjRiaILz NWiyXVNrSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDI[WxiKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkAzPCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVcvQDUQvF2u NFzYfGo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MU[0PFg4Pyd-M{G2OFg5Pzd:L3G+
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LO2 MU\DfZRwfG:6aXPpeJkh[XO|YYm= M3;PSFI1KGi{cx?= M3rDPGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxQOiClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliYX\0[ZIhOjRiaILzJIJ6KE2WVDDhd5NigSxiQ1O1NF0yOi5{zszNMi=> M3fST|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNkS4PFc4Lz5|MU[0PFg4PzxxYU6=

... 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
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

Cell Research:

[1]

- Collapse
  • 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.


    (Only for Reference)
Animal Research:

[2]

- Collapse
  • Animal Models: Neonatal ICR mice
  • Dosages: 0.4 and 1.7 μg in 30 μL PBS
  • Administration: oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 57 mg/mL (197.71 mM)
Ethanol 23 mg/mL (79.77 mM)
Water Insoluble
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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 288.30
Formula

C16H16O5

CAS No. 54952-43-1
Storage powder
in solvent
Synonyms Anchusin, Anchusa acid, Alkanna Red, Isoarnebin 4, NSC 252844
Smiles CC(=CCC(C1=CC(=O)C2=C(C=CC(=C2C1=O)O)O)O)C

In vivo Formulation Calculator (Clear solution)

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID