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 14 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 NUnMeHRtT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYfnfVhPUW6qaXLpeIlwdiCxZjDoeY1idiCDMUCxSEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvODByN{GyNe69VS5? NIOyTlQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6PDdyLze+V2FPT0WUPD;hQi=>
TE-441-T MmjES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUXJcohq[mm2aX;uJI9nKGi3bXHuJHRGNTR2MT3UJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xODJ{M{lOwG0v NWjPU3dJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTR5MD:nQnNCVkeHUkyvZV4>
NALM-6 MnOzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEG3WZJKdmirYnn0bY9vKG:oIHj1cYFvKE6DTF2tOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvODB{N{m3{txONg>? NIHFc3E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6PDdyLze+V2FPT0WUPD;hQi=>
SW1710 NIq1cXhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NI\v[FVKdmirYnn0bY9vKG:oIHj1cYFvKFOZMUexNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvODB{OUJOwG0v NIrq[Go9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6PDdyLze+V2FPT0WUPD;hQi=>
ST486 MWPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnnXTY5pcWKrdHnvckBw\iCqdX3hckBUXDR6NjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNFA3OTd7zszNMi=> M1z5OlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk1PzBxJ{7TRW5ITVJ:L3G+
SK-UT-1 MnnXS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUXORmNQUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3VWE0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5yMEe0N|jPxE1w MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5OFcxNyd-U1HOS2VTRC:jPh?=
A253 M1O5cWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3jRXGlvcGmkaYTpc44hd2ZiaIXtZY4hSTJ3MzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNFA4PDl|zszNMi=> NFvmUpE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6PDdyLze+V2FPT0WUPD;hQi=>
KU812 Mm[3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUPJcohq[mm2aX;uJI9nKGi3bXHuJGtWQDF{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6wNFg{ODcQvF2u NEXlSG89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6PDdyLze+V2FPT0WUPD;hQi=>
A427 M4e2Tmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlTqTY5pcWKrdHnvckBw\iCqdX3hckBCPDJ5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6wNVc6Qc7:TT6= MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5OFcxNyd-U1HOS2VTRC:jPh?=
MZ1-PC NI\LNoVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHj5WlZKdmirYnn0bY9vKG:oIHj1cYFvKE2cMT3QR{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvODF7MklOwG0v NFG2THA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6PDdyLze+V2FPT0WUPD;hQi=>
NCI-H2009 NHewUGlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnLETY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKwNFkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjB{MEW0{txONg>? NUX5S4x[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTR5MD:nQnNCVkeHUkyvZV4>
CAL-51 NVrCTpBDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYq1b2RQUW6qaXLpeIlwdiCxZjDoeY1idiCFQVytOVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjB{MEi1{txONg>? NHfZe5M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6PDdyLze+V2FPT0WUPD;hQi=>
GCIY M1jEU2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Ml:wTY5pcWKrdHnvckBw\iCqdX3hckBIS0m\IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6wN|U6QM7:TT6= M2L3Z|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk1PzBxJ{7TRW5ITVJ:L3G+
SK-PN-DW M2fjfGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFq5eYZKdmirYnn0bY9vKG:oIHj1cYFvKFONLWDOMWRYKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5yM{[1Oe69VS5? NWPYc|gxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTR5MD:nQnNCVkeHUkyvZV4>
MES-SA NU[3b3Z4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHnyd5lKdmirYnn0bY9vKG:oIHj1cYFvKE2HUz3TRUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvODRzM{NOwG0v M3TQbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk1PzBxJ{7TRW5ITVJ:L3G+
KS-1 MWjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGnRTY5KdmirYnn0bY9vKG:oIHj1cYFvKEuVLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlA1OTYQvF2u NYjmPW1SRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTR5MD:nQnNCVkeHUkyvZV4>
IGROV-1 M1;lSmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXvJcohq[mm2aX;uJI9nKGi3bXHuJGlIWk:YLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlA2PTZzzszNMi=> MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5OFcxNyd-U1HOS2VTRC:jPh?=
HMV-II NYjO[lAzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2\0U2lvcGmkaYTpc44hd2ZiaIXtZY4hUE2YLVnJJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xPTZ2zszNMi=> NGrvWXE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6PDdyLze+V2FPT0WUPD;hQi=>
SW982 MVrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmjmTY5pcWKrdHnvckBw\iCqdX3hckBUXzl6MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNFYxOjQQvF2u NGLhV5E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6PDdyLze+V2FPT0WUPD;hQi=>
NCI-H2052 MlXIS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NU\KeYZrUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIxPTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkC2NVE{|ryPLh?= NH;SSmY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6PDdyLze+V2FPT0WUPD;hQi=>
RT-112 MnmxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYX5eZZUUW6qaXLpeIlwdiCxZjDoeY1idiCUVD2xNVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjB5MEO3{txONg>? MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly5OFcxNyd-U1HOS2VTRC:jPh?=
AN3-CA MVfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYK3fGY{UW6qaXLpeIlwdiCxZjDoeY1idiCDTkOtR2Eh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjB5OU[1{txONg>? M16wcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk1PzBxJ{7TRW5ITVJ:L3G+
A498 NVrkT21JT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUnJcohq[mm2aX;uJI9nKGi3bXHuJGE1QThiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkC4NVnPxE1w NWm0e2dXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTR5MD:nQnNCVkeHUkyvZV4>
8-MG-BA NH;MflNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWHJcohq[mm2aX;uJI9nKGi3bXHuJFguVUdvQlGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlA5PTV4zszNMi=> NXLWWm11RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTR5MD:nQnNCVkeHUkyvZV4>
HLE NXfGZnpTT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoDxTY5pcWKrdHnvckBw\iCqdX3hckBJVEViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkC4PFMy|ryPLh?= NYC1VZJFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTR5MD:nQnNCVkeHUkyvZV4>
AM-38 MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mny0TY5pcWKrdHnvckBw\iCqdX3hckBCVS1|ODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNFk3OzIQvF2u NHqwToQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw6PDdyLze+V2FPT0WUPD;hQi=>
NCI-H1963 MUXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYjRPHU1UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE6PjNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkGwNFEy|ryPLh?= NWj5e2pJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNQTR5MD:nQnNCVkeHUkyvZV4>
NKM-1 NH7qZpJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYLJcohq[mm2aX;uJI9nKGi3bXHuJG5MVS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xNFEz|ryPLh?= M4\OOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk1PzBxJ{7TRW5ITVJ:L3G+
MRK-nu-1 MV\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVjJNIpQUW6qaXLpeIlwdiCxZjDoeY1idiCPUlutcpUuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMUCxPVPPxE1w MoXGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMPVQ4OC9pPmPBUmdGWjxxYU6=
GR-ST MknBS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUTJcohq[mm2aX;uJI9nKGi3bXHuJGdTNVOWIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xNFIyQM7:TT6= M13LO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFk1PzBxJ{7TRW5ITVJ:L3G+
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NCI-H1975 MU\BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M4izfVI1KGi{cx?= M4Tze2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWgyQTd3IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBk\WyuII\pZYJqdGm2eTDh[pRmeiB{NDDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTRwMklOwG0v NHLaO|I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MU[0PFg4Pyd-M{G2OFg5Pzd:L3G+
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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.

  • (Only for Reference)
Animal Research:

[2]

  • 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 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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