Shikonin

For research use only.

Catalog No.S8279 Synonyms: Anchusin, Anchusa acid, Alkanna Red, C.I. 75535, Isoarnebin 4, NSC 252844

6 publications

Shikonin Chemical Structure

CAS No. 54952-43-1

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. 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.

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Choose Selective PKM Inhibitors

Biological Activity

Description 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. 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] PKM2 [3]
(FBP absence)
PKM2 [3]
(FBP presence)
TMEM16A chloride channel [2]
()
0.3 μM 0.8 μM 6.5 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 cell M2fqeGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVHJcohq[mm2aX;uJI9nKGi3bXHuJGEyODGGIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD63NVIhdk1? M33nenNCVkeHUh?=
TE-441-T cell Ml2xS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MY\Jcohq[mm2aX;uJI9nKGi3bXHuJHRGNTR2MT3UJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk4zPCCwTR?= NVTEdJhQW0GQR1XS
NALM-6 cell M1jaSWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFX4ZmRKdmirYnn0bY9vKG:oIHj1cYFvKE6DTF2tOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvQCCwTR?= M4jENXNCVkeHUh?=
SW1710 cell NGTwRllIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXjmelhbUW6qaXLpeIlwdiCxZjDoeY1idiCVV{G3NVAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zNjlzIH7N NWLVbpJ4W0GQR1XS
ST486 cell M3S3U2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NH;RZ4ZKdmirYnn0bY9vKG:oIHj1cYFvKFOWNEi2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Ok4yQCCwTR?= M33RPXNCVkeHUh?=
SK-UT-1 cell growth NYPic5hwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4SxSmlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvVWStNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVcvPDRibl2= MVvTRW5ITVJ?
A253 cell NHLuNmxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mm\oTY5pcWKrdHnvckBw\iCqdX3hckBCOjV|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Nz60PUBvVQ>? NUjXUHIyW0GQR1XS
KU812 cell M3LEOGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NH7yUHdKdmirYnn0bY9vKG:oIHj1cYFvKEuXOEGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PE4{OSCwTR?= MX7TRW5ITVJ?
A427 cell NIPLemtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmiyTY5pcWKrdHnvckBw\iCqdX3hckBCPDJ5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUeuPVkhdk1? NV:5WFZTW0GQR1XS
MZ1-PC cell M13C[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmnHTY5pcWKrdHnvckBw\iCqdX3hckBOYjFvUFOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xPU4zQCCwTR?= NVf3fnFLW0GQR1XS
NCI-H2009 cell NFLIN|lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXPJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkCwPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIxNjV2IH7N MmX6V2FPT0WU
CAL-51 cell MYjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NW\LVYhNUW6qaXLpeIlwdiCxZjDoeY1idiCFQVytOVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOC56NTDuUS=> M1frbnNCVkeHUh?=
GCIY cell NHfvSFZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4j6OWlvcGmkaYTpc44hd2ZiaIXtZY4hT0OLWTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO1Mlk5KG6P M2HzXnNCVkeHUh?=
SK-PN-DW cell M2njeWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHnnXJRKdmirYnn0bY9vKG:oIHj1cYFvKFONLWDOMWRYKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzZwNUWgcm0> MnWxV2FPT0WU
MES-SA cell MmrWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3zYb2lvcGmkaYTpc44hd2ZiaIXtZY4hVUWVLWPBJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFEvOzJibl2= NEW3UGxUSU6JRWK=
KS-1 cell M3LGVWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHTP[|BKdmirYnn0bY9vKG:oIHj1cYFvKEuVLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20NU42KG6P MlLxV2FPT0WU
IGROV-1 cell M{PsN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2TBeGlvcGmkaYTpc44hd2ZiaIXtZY4hUUeUT2[tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVU2NjZzIH7N M3vrZnNCVkeHUh?=
HMV-II cell NITvR2FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYjYfW1[UW6qaXLpeIlwdiCxZjDoeY1idiCKTW[tTWkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02Pi52IH7N MX3TRW5ITVJ?
SW982 cell MmXKS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoL3TY5pcWKrdHnvckBw\iCqdX3hckBUXzl6MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPU[wMlI{KG6P NXnRTFVzW0GQR1XS
NCI-H2052 cell Mn\jS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NU\VVIJMUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIxPTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD14MT6xN{BvVQ>? NITk[HdUSU6JRWK=
RT-112 cell M{LMemdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHPOTXlKdmirYnn0bY9vKG:oIHj1cYFvKFKWLUGxNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVcxNjN5IH7N MVvTRW5ITVJ?
AN3-CA cell MlrjS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MX3Jcohq[mm2aX;uJI9nKGi3bXHuJGFPOy2FQTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUe5MlY2KG6P MofuV2FPT0WU
A498 cell MnfIS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXnJcohq[mm2aX;uJI9nKGi3bXHuJGE1QThiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD16MT65JI5O MUfTRW5ITVJ?
8-MG-BA cell NHvDW2tIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWnJcohq[mm2aX;uJI9nKGi3bXHuJFguVUdvQlGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME24OU42PiCwTR?= NIHB[lZUSU6JRWK=
HLE cell NIi3Zo9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXfJcohq[mm2aX;uJI9nKGi3bXHuJGhNTSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTh6LkOxJI5O NIfSfVBUSU6JRWK=
AM-38 cell M{i1WGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1vtbGlvcGmkaYTpc44hd2ZiaIXtZY4hSU1vM{igZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25Ok4{OSCwTR?= MVnTRW5ITVJ?
NCI-H1963 cell MUDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NInEPVJKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVk3OyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMUCwNVEh|ryP MkKzV2FPT0WU
NKM-1 cell MXzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVPJcohq[mm2aX;uJI9nKGi3bXHuJG5MVS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xNFEzKM7:TR?= MkfXV2FPT0WU
MRK-nu-1 cell NFHQeFJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1HOeGlvcGmkaYTpc44hd2ZiaIXtZY4hVVKNLX71MVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjFyMUmzJO69VQ>? NUDYS5cyW0GQR1XS
GR-ST cell MlzIS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2DpfmlvcGmkaYTpc44hd2ZiaIXtZY4hT1JvU2SgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlExOjF6IN88US=> M3\iO3NCVkeHUh?=
A431 cell NFXhOYlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYPzZWNlUW6qaXLpeIlwdiCxZjDoeY1idiCDNEOxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yODZ7NzFOwG0> MUXTRW5ITVJ?
SK-LMS-1 cell NYnWdItnT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlLvTY5pcWKrdHnvckBw\iCqdX3hckBUUy2OTWOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTB6NEGg{txO NVfFTohXW0GQR1XS
MZ7-mel cell NVPI[ohDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVrJcohq[mm2aX;uJI9nKGi3bXHuJG1bPy2vZXygZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlEyOzd{IN88US=> NE\sVXhUSU6JRWK=
KASUMI-1 cell MoPOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFi2OWtKdmirYnn0bY9vKG:oIHj1cYFvKEuDU2XNTU0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5zMkO3NUDPxE1? MYLTRW5ITVJ?
A204 cell MnO1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVHJcohq[mm2aX;uJI9nKGi3bXHuJGEzODRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkGyOlU1KM7:TR?= MofUV2FPT0WU
M059J cell NYnifo46T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3PnOmlvcGmkaYTpc44hd2ZiaIXtZY4hVTB3OVqgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlE{PDF7IN88US=> MlrwV2FPT0WU
NCI-H2342 cell NXrPNYJyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUP1OXlKUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFI{PDJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkGzOFQ2KM7:TR?= NWfUe2FKW0GQR1XS
KYSE-450 cell MnfRS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NX[zZml1UW6qaXLpeIlwdiCxZjDoeY1idiCNWWPFMVQ2OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMUO4NVUh|ryP MnrhV2FPT0WU
SR cell MXjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MX7Jcohq[mm2aX;uJI9nKGi3bXHuJHNTKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5zNEC3N{DPxE1? NFu2Z25USU6JRWK=
J82 cell NIHyPIxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVHJcohq[mm2aX;uJI9nKGi3bXHuJGo5OiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMUSyOVUh|ryP MV\TRW5ITVJ?
NTERA-S-cl-D1 cell NUfkcXA3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXnJcohq[mm2aX;uJI9nKGi3bXHuJG5VTVKDLWOtZ4wuTDFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkG0N|U4KM7:TR?= NFz5UJhUSU6JRWK=
ACHN cell NXnWXIVHT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXv6T3V4UW6qaXLpeIlwdiCxZjDoeY1idiCDQ1jOJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yPDZ|ODFOwG0> MVjTRW5ITVJ?
REH cell MnPXS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXvJcohq[mm2aX;uJI9nKGi3bXHuJHJGUCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMUS2PVYh|ryP MWPTRW5ITVJ?
MEL-HO cell MXzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWDa[mxZUW6qaXLpeIlwdiCxZjDoeY1idiCPRVytTG8h[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjF2OEiyJO69VQ>? MkTPV2FPT0WU
DEL cell MlfnS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkjBTY5pcWKrdHnvckBw\iCqdX3hckBFTUxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkG1N|gyKM7:TR?= MmLYV2FPT0WU
IGR-1 cell M4fTdGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXrOdJE3UW6qaXLpeIlwdiCxZjDoeY1idiCLR2KtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTV|OUig{txO MXTTRW5ITVJ?
RPMI-7951 cell MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoPBTY5pcWKrdHnvckBw\iCqdX3hckBTWE2LLUe5OVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjF3NkC5{txO Mk[4V2FPT0WU
Daoy cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGrqcWlKdmirYnn0bY9vKG:oIHj1cYFvKESjb4mgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlE2QDd5IN88US=> MY\TRW5ITVJ?
CAL-85-1 cell M3TGXWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEj0NZJKdmirYnn0bY9vKG:oIHj1cYFvKEODTD24OU0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5zNkC3N{DPxE1? MlrEV2FPT0WU
SNU-423 cell M2TIeGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGHjc|BKdmirYnn0bY9vKG:oIHj1cYFvKFOQVT20NlMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjF4M{C3JO69VQ>? NITCXXRUSU6JRWK=
PANC-03-27 cell NVr2[W5zT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4DlfmlvcGmkaYTpc44hd2ZiaIXtZY4hWEGQQz2wN{0zPyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMU[3OEDPxE1? M4W4SnNCVkeHUh?=
CHL-1 cell NHPLO|dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXK5XphjUW6qaXLpeIlwdiCxZjDoeY1idiCFSFytNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTZ5ODFOwG0> NYTOOHhOW0GQR1XS
SIG-M5 cell M3zUeWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3rZV2lvcGmkaYTpc44hd2ZiaIXtZY4hW0mJLV21JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yPjl6NjFOwG0> MXnTRW5ITVJ?
DU-4475 cell NVzMWFdJT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUPWRYJKUW6qaXLpeIlwdiCxZjDoeY1idiCGVT20OFc2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5zN{m4OEDPxE1? NILZcVdUSU6JRWK=
QIMR-WIL cell NG\TNY1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVS1S4tlUW6qaXLpeIlwdiCxZjDoeY1idiCTSV3SMXdKVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMUixPFkh|ryP M1q3bnNCVkeHUh?=
COLO-679 cell NYP4NXZwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYXmPHFQUW6qaXLpeIlwdiCxZjDoeY1idiCFT1zPMVY4QSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMUi0NFEh|ryP NGTmRlFUSU6JRWK=
HOS cell M3:ycGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3TuRWlvcGmkaYTpc44hd2ZiaIXtZY4hUE:VIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xPFYxQCEQvF2= Ml;TV2FPT0WU
CA46 cell NH;WblVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NI\EPGpKdmirYnn0bY9vKG:oIHj1cYFvKEODNE[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlE6OTh3IN88US=> MkjwV2FPT0WU
DU-145 cell MVfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnnITY5pcWKrdHnvckBw\iCqdX3hckBFXS1zNEWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlE6OzB7IN88US=> MX3TRW5ITVJ?
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SCC-9 cell M2XBT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVnsTGk3UW6qaXLpeIlwdiCxZjDoeY1idiCVQ1OtPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTl4N{Wg{txO NV3EU3RqW0GQR1XS
IST-SL2 cell M3LLOmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MX3Jcohq[mm2aX;uJI9nKGi3bXHuJGlUXC2VTEKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlIxODF2IN88US=> MlGzV2FPT0WU
PA-1 cell M3;pR2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NU\hVXg5UW6qaXLpeIlwdiCxZjDoeY1idiCSQT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zODF{ODFOwG0> NX;KVYxVW0GQR1XS
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EFM-19 cell NFvVU45Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{TRV2lvcGmkaYTpc44hd2ZiaIXtZY4hTU[PLUG5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zOTJzIN88US=> M1LSOHNCVkeHUh?=
NB69 cell NVvGV4RuT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkDuTY5pcWKrdHnvckBw\iCqdX3hckBPSjZ7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6yNVI4OyEQvF2= NGHqVo1USU6JRWK=
SBC-5 cell NF33OVdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHS1ZYNKdmirYnn0bY9vKG:oIHj1cYFvKFOEQz21JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zOTV2NjFOwG0> MYfTRW5ITVJ?
KYSE-270 cell MmnkS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NETzfnNKdmirYnn0bY9vKG:oIHj1cYFvKEu\U1WtNlcxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5{MU[5NkDPxE1? MmfoV2FPT0WU
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T47D cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYrne2c5UW6qaXLpeIlwdiCxZjDoeY1idiCWNEfEJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zOjNyNjFOwG0> M37ibHNCVkeHUh?=
HSC-2 cell NFTUTIhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4DWR2lvcGmkaYTpc44hd2ZiaIXtZY4hUFOFLUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlIzOzF6IN88US=> NGHRT|BUSU6JRWK=
HGC-27 cell NVezdoNFT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUnJcohq[mm2aX;uJI9nKGi3bXHuJGhISy1{NzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNlI5OzRizszN NFzWWFhUSU6JRWK=
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COR-L105 cell NX3qVZNIT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4\wWGlvcGmkaYTpc44hd2ZiaIXtZY4hS0:ULVyxNFUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjJ|MEO0JO69VQ>? M2joXXNCVkeHUh?=
LB647-SCLC cell MlvvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M13SV2lvcGmkaYTpc44hd2ZiaIXtZY4hVEJ4NEetV2NNSyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMkOyO|gh|ryP NX;wPXdGW0GQR1XS
G-401 cell MlHxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVzyTpJIUW6qaXLpeIlwdiCxZjDoeY1idiCJLUSwNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjN2OUKg{txO M2jXb3NCVkeHUh?=
MKN1 cell NF;mcopIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NX7x[JU{UW6qaXLpeIlwdiCxZjDoeY1idiCPS16xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4zOzV5NjFOwG0> MkD0V2FPT0WU
HepG2 cell M3[3dGN6fG:2b4jpZ4l1gSCjc4PhfS=> M334WFI1KGh? M13D[GN6fG:2b4jpZ4l1gSCjZ3HpcpN1KE2GUkGgVIdxKG:4ZYLlfJBz\XO|aX7nJIh2dWGwIFjldGczKGOnbHzzJIFnfGW{IEK0JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6yOEDPxE1? M{DxfFE4QTR7OEW4
HL60 cells Mm\SR5l1d3SxeHnjbZR6KGG|c3H5 NFL2dodEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJVDZyIHPlcIx{KGK7IF3UWEBie3OjeTygTWM2OD1yLkS0JO69VQ>? MVKxPVEyOTR4NB?=
MCF7 cells NFnE[XZEgXSxdH;4bYNqfHliYYPzZZk> MkSyO|IhcA>? NUXsWJU3S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVEvPDVizszN NWHhPXZHOjB2MEO2OFY>
mouse L929 cells M4PJ[WN6fG:2b4jpZ4l1gSCjc4PhfS=> NH31dlQzPCCq NULXXVlOS3m2b4TvfIlkcXS7IHHnZYlve3RibX;1d4UhVDl{OTDj[YxteyCjZoTldkAzPCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVMvOiEQvF2= NVvZfoZROjF4MkC1N|A>
MDA-MB-231 cells M3i3bWZ2dmO2aX;uJIF{e2G7 NH3tb5UzPCCq MoTkRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCjZoTldkAzPCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVYvPiEQvF2= MlToNlE3OjB3M{C=
HCT15 cells MXjGeY5kfGmxbjDhd5NigQ>? NXu0TIwyOjRiaB?= M37yVGFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFE2KGOnbHzzJIFnfGW{IEK0JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;Nz6zJO69VQ>? MXyyNVYzODV|MB?=

... 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]

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  • 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]

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  • 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):
2% DMSO+30% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.
3mg/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, C.I. 75535, 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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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID