Staurosporine (AM-2282)

Catalog No.S1421 Synonyms: Antibiotic AM-2282, STS

For research use only.

Staurosporine (AM-2282, Antibiotic AM-2282, STS) is a potent PKC inhibitor for PKCα, PKCγ and PKCη with IC50 of 2 nM, 5 nM and 4 nM, less potent to PKCδ (20 nM), PKCε (73 nM) and little active to PKCζ (1086 nM) in cell-free assays. Also shows inhibitory activities on other kinases, such as PKA, PKG, S6K, CaMKII, etc. Phase 3.

Staurosporine (AM-2282) Chemical Structure

CAS No. 62996-74-1

Selleck's Staurosporine (AM-2282) has been cited by 113 publications

Purity & Quality Control

Choose Selective Antineoplastic and Immunosuppressive Antibiotics Inhibitors

Biological Activity

Description Staurosporine (AM-2282, Antibiotic AM-2282, STS) is a potent PKC inhibitor for PKCα, PKCγ and PKCη with IC50 of 2 nM, 5 nM and 4 nM, less potent to PKCδ (20 nM), PKCε (73 nM) and little active to PKCζ (1086 nM) in cell-free assays. Also shows inhibitory activities on other kinases, such as PKA, PKG, S6K, CaMKII, etc. Phase 3.
Targets
PKCα [1]
(Cell-free assay)
c-Fgr [2]
(Cell-free assay)
phosphorylase kinase [2]
(Cell-free assay)
PKCη [1]
(Cell-free assay)
PKCγ [1]
(Cell-free assay)
Click to View More Targets
2 nM 2 nM 3 nM 4 nM 5 nM
In vitro

Staurosporine, a microbial alkaloid, significantly inhibits protein kinase C from rat brain with IC50 of 2.7 nM. Staurosporine displays strong inhibitory effect against HeLa S3 cells with IC50 of 4 nM. [1] Staurosporine also inhibits a variety of other protein kinases, including PKA, PKG, phosphorylase kinase, S6 kinase, Myosin light chain kinase (MLCK), CAM PKII, cdc2, v-Src, Lyn, c-Fgr, and Syk with IC50 of 15 nM, 18 nM, 3 nM, 5 nM, 21 nM, 20 nM, 9 nM, 6 nM, 20 nM, 2 nM, and 16 nM, respectively. [2] Staurosporine (1 μM) induces >90% apoptosis in PC12 cells. Consistently, Staurosporine treatment induces a rapid and prolonged elevation of intracellular free calcium levels [Ca2+]i, accumulation of mitochondrial reactive oxygen species (ROS), and subsequent mitochondrial dysfunction. [3] The apoptosis of MCF7 cells induced by Staurosporine can be enhanced by the expression of functional caspase-3 via caspase-8 activation and Bid cleavage. [4] Staurosporine treatment at 1 μM only partially inhibits IL-3-stimulated Bcl2 phosphorylation but completely blocks PKC-mediated Bcl2 phosphorylation. [5] Staurosporine induces apoptosis of human foreskin fibroblasts AG-1518, depending on the lysosomal cathepsins D mediated cytochrome c release and caspase activation. [6] In addition to activating the classical mitochondrial apoptosis pathway, Staurosporine triggers a novel intrinsic apoptosis pathway, relying on the activation of caspase-9 in the absence of Apaf-1. [7]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human colon carcinoma cell line HCT116 MW\GeY5kfGmxbjDhd5NigQ>? M3voVWNwdmOnboTyZZRqd25icnXxeYlz\WRiZn;yJIdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJINwdG:wIHPhdoNqdm:vYTDj[YxtKGyrbnWgTGNVOTF4LDDJR|UxRTZibl2u NWXWfnpwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUW1N|c{PDVpPkG1OVM4OzR3PD;hQi=>
human PBMC MmDPSpVv[3Srb36gZZN{[Xl? NHzvV4gzPCCq M2LVUHN2eHC{ZYPzbY9vKG:oIFnMNkBxem:mdXP0bY9vKGmwIHj1cYFvKFCETVOgZYZ1\XJiMkSgbJJ{KGK7IFXMTXNCNCCLQ{WwQVE3KG6PLh?= M3;4PVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6NUi1NFQ3Lz5zOEW4OVA1PjxxYU6=
endothelial cells MVLGeY5kfGmxbjDhd5NigQ>? NXTtUJdlTW[oZXP0bZZmKGSxc3WgZYdicW6|dDDwcIF{dWmwb3flckBi[3SrdnH0c5Ih[WO2aY\peJkhe3SrbYXsZZRm\CCkeTDwbI9z[m:uIHXzeIVzKGmwIHXu[I91cGWuaXHsJINmdGy|LDDFSFUxKD1iNz61JO69VS5? NUXFOpJ5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxOEewPVA6PSd-OEewPVA6PTxxYU6=
Sf9 insect cells M4XZe2Z2dmO2aX;uJIF{e2G7 NEjrOpNKdmirYnn0bY9vKG:oIIDyc5RmcW5ia3nuZZNmKENqMUqxcYl5fHW{ZTDv[kBRU0NiYXzwbIEhLiCkZYThLUBmgHC{ZYPz[YQhcW5iU3[5JIlve2WldDDj[YxteyxiSVO1NEA:KDBwMEKg{txONg>? NGDNXlU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi97OEezOlA2Lz57OEezOlA2RC:jPh?=
LoVo cells M1ruU2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NWjFXFNbSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDjc4xwdiClYX7j[ZIh[2WubDDsbY5mKCiOb2\vJINmdGy|KTD1d4lv\yCPVGSgZZN{[XluIFnDOVAhRSByLkCwNUDPxE1w NXLYcnFYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUG1PVE2ODVpPkGxOVkyPTB3PD;hQi=>
umbilical vein endothelial cells M1P6e2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 MVPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKHWvYnnsbYNidCC4ZXnuJIVv\G:2aHXsbYFtKGOnbHzzJEhJXV[HQ4OpJJV{cW6pIF3UWEBie3OjeTygTWM2OCB;IECuNFA1KM7:TT6= MlXFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTF3OUG1NFUoRjFzNUmxOVA2RC:jPh?=
ST-486 cells M3Ti[mFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NWrqSmlJSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBjfXKtaYSgcJlueGixbXGgZ4VtdCCuaX7lJEhUXC12OE[gZ4VtdHNrIIXzbY5oKE2WVDDhd5NigSxiSVO1NEA:KDBwMEC3JO69VS5? NYPUTXRkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUG1PVE2ODVpPkGxOVkyPTB3PD;hQi=>
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HEK293 cells M4PmU2Z2dmO2aX;uJIF{e2G7 NEG0fVNKdmirYnn0bY9vKG:oIGDLR{1j\XSjIFnJJI1m\GmjdHXkJGlNNThicnXs[YF{\SCocn;tJGhGUzJ7MzDj[YxteyCkeTDFUGlUSSxiSVO1NEA:KDBwMEe3JO69VS5? NWPNPIxQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUK5OFE{OzFpPkGyPVQyOzNzPD;hQi=>
P19 cells NHO2U|FHfW6ldHnvckBie3OjeR?= NYL5PFl6UW6qaXLpeIlwdiCxZjDQcIF1\WyndD3k[ZJqfmWmIHfyc5d1cCCoYXP0c5IhemWlZYD0c5IhcW5iUEG5JINmdGy|LDDJR|UxKD1iMD6wNFIh|ryPLh?= NUn6PZByRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUW3O|E1OTlpPkG1O|cyPDF7PD;hQi=>
P19 cells NIjZc4FHfW6ldHnvckBie3OjeR?= NGrjbFdKdmirYnn0bY9vKG:oIGDsZZRmdGW2LXTldol3\WRiZ4Lve5RpKG[jY4TvdkBz\WOncITvdkBqdiCSMUmgZ4VtdHNuIFnDOVAhRSByLkCwNkDPxE1w NVXkSlZYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUW3O|E1OTlpPkG1O|cyPDF7PD;hQi=>
P19 cells MnnMSpVv[3Srb36gZZN{[Xl? NHPsUIJKdmirYnn0bY9vKG:oIGDyc5RmcW5iS3nuZZNmKEFiaX6gVFE6KGOnbHzzMEBKSzVyIE2gNE4xODRizszNMi=> NFroPVg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNUe3NVQyQSd-MUW3O|E1OTl:L3G+
P19 cells M2nEW2Z2dmO2aX;uJIF{e2G7 NFHUWplKdmirYnn0bY9vKG:oIFPhcINqfW1xY3HscY9lfWyrbj3k[ZBmdmSnboSgdJJwfGWrbjDrbY5ie2VidInw[UBKUSCrbjDQNVkh[2WubIOsJGlEPTBiPTCwMlAxPiEQvF2u MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTd5MUSxPUc,OTV5N{G0NVk9N2F-
P19 cells MlLHSpVv[3Srb36gZZN{[Xl? MmDiTY5pcWKrdHnvckBw\iCFeXPsbY4u\GWyZX7k[Y51KGurbnHz[UAyKGmwIGCxPUBk\WyuczygTWM2OCB;IECuNFA5KM7:TT6= M4rIcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3N{exOFE6Lz5zNUe3NVQyQTxxYU6=
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HEK293 cells MYjGeY5kfGmxbjDhd5NigQ>? NFGxWFBKdmirYnn0bY9vKG:oIFnMMVghemWuZXHz[UBjgSCKRVuyPVMh[2WubIOg[ZhxemW|c3nu[{BRU0NvYnX0ZVItKEmFNUCgQUAxNjB5NzFOwG0v NGDSNmE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNUe3NVQyQSd-MUW3O|E1OTl:L3G+
P19 cells NX\HRolHTnWwY4Tpc44h[XO|YYm= NWXnWFllUW6qaXLpeIlwdiCxZjDJcpN2dGmwIILlZ4VxfG:{IHvpcoF{\SCrbjDQNVkh[2WubIOsJGlEPTBiPTCwMlIh|ryPLh?= MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTd5MUSxPUc,OTV5N{G0NVk9N2F-
P19 cells NV[3RmZyTnWwY4Tpc44h[XO|YYm= M3HIeWlvcGmkaYTpc44hd2ZiQ3Hz[YlvKGurbnHz[UAyKGmwIGCxPUBk\WyuczygTWM2OCB;IEGuOEDPxE1w M2jpW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3N{exOFE6Lz5zNUe3NVQyQTxxYU6=
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FL5.12-Akt1 cells M120U2Z2dmO2aX;uJIF{e2G7 NV;6Z29FSWO2aY\peJkh[WejaX7zeEBIW0t|IIDoc5NxcG:{eXzheIlwdiCrbjDGUFUvOTJvQXv0NUBk\WyuczygSWM2OCB;IECuOFYh|ryPLh?= NEnaZ489[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNkSxN|c5OCd-MU[0NVM4QDB:L3G+
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MCF7 cells MknUSpVv[3Srb36gZZN{[Xl? MmS3TY5pcWKrdHnvckBw\iCSS1GgbY4hcHWvYX6gUWNHPyClZXzsd{BjgSCjcoLhfU1j[XOnZDDmcJVwemW|Y3XuZ4Uh[XO|YYmsJGtqKD1iMD6wNFUh|ryPLh?= MnTGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh4NU[zOlkoRjF6NkW2N|Y6RC:jPh?=
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Jurkat cells MXTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MX;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IFrBT|Mh\XiycnXzd4lv\yCqdX3hckBz\XO2aX7nJGp2emujdDDj[YxteyxiSVO1NEA:KDBwM{GxJO69VS5? MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTR{N{KwN{c,OTl2MkeyNFM9N2F-
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A431 cells MU\DfZRwfG:6aXPpeJkh[XO|YYm= MV2yOEBp MlP5R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVQ{OSClZXzsd{Bi\nSncjCyOEBpenNidYPpcochSW6wZYjpckBX\U[LVFOvdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZzDifUBOXFRiYYPzZZktKEmFNUCgQUAxNjB5IN88UU4> M1jVZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUSxNFUyLz5{MkW0NVA2OTxxYU6=
MCF7 cells MlnXR5l1d3SxeHnjbZR6KGG|c3H5 M3LtPFI1KGh? MWnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IEK0JIhzeyC3c3nu[{BCdm6neHnuJHZmTkmWQz;wdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pIHL5JG1VXCCjc4PhfUwhUUN3MDC9JFAvOThizszNMi=> M3vYflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUSxNFUyLz5{MkW0NVA2OTxxYU6=
BJ cells NX\nNGU2S3m2b4TvfIlkcXS7IHHzd4F6 M1XKR|czKGh? MmL1R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRmoh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPhcINmcW5iQV2gZZN{[XluIFnDOVAhRSByLkCwNkDPxE1w MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjl{MUC4NUc,OjJ7MkGwPFE9N2F-
CEM cells MoW5R5l1d3SxeHnjbZR6KGG|c3H5 NVX1dYtbPzJiaB?= MVHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDDSW0h[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPhcINmcW5iQV2gZZN{[XluIFnDOVAhRSByLkCyN{DPxE1w Ml\rQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ7MkGwPFEoRjJ{OUKxNFgyRC:jPh?=
MCF7 cells MkDSR5l1d3SxeHnjbZR6KGG|c3H5 MY[3NkBp M1yzXWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JGNidGOnaX6gRW0h[XO|YYmsJGlEPTBiPTCwMlA3PCEQvF2u M{\5TFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OUKxNFgyLz5{MkmyNVA5OTxxYU6=
HeLa cells MVnDfZRwfG:6aXPpeJkh[XO|YYm= MWe3NkBp Mm\hR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTIVN[SClZXzsd{Bi\nSncjC3NkBpenNiYomgR4Ft[2WrbjDBUUBie3OjeTygTWM2OCB;IECuNVc2KM7:TT6= MoTVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ7MkGwPFEoRjJ{OUKxNFgyRC:jPh?=
HepG2 cells NYTnNnVFTnWwY4Tpc44h[XO|YYm= MVqyOEBp M2fvT2lvcGmkaYTpc44hd2ZidHXsc41memG|ZTDpckBpfW2jbjDI[ZBIOiClZXzsd{Bi\nSncjCyOEBpenNiYomgWHJCWC2SQ2KtSWxKW0FiYYPzZZktKEmFNUCgQUA1NjF2IN88UU4> Mn\tQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyMUiwPVYoRjJ|MEG4NFk3RC:jPh?=
SW1116 cells MlS2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? MnjtOFghcA>? M2fLfWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU2exNVE3KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQhdWW2aH;kMEBKSzVyIE2gOE46PSEQvF2u MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzBzOEC5Okc,OjNyMUiwPVY9N2F-
HepG2 cells M374PWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NIHNTpc1QCCq NFTa[IhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjldGczKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQhdWW2aH;kMEBKSzVyIE2gOk44OyEQvF2u M1m3OlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MEG4NFk3Lz5{M{CxPFA6PjxxYU6=
BGC823 cells M1WyVGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NHr0TFc1QCCq NE\6emNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFLHR|gzOyClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRVKG2ndHjv[EwhUUN3MDC9JFYvQDNizszNMi=> MmH0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyMUiwPVYoRjJ|MEG4NFk3RC:jPh?=
HeLa cells NGf1fZJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= M1ThOVQ5KGh? NHyxOJhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjlUIEh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBu\XSqb3SsJGlEPTBiPTC5MlEzKM7:TT6= MnnWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyMUiwPVYoRjJ|MEG4NFk3RC:jPh?=
HCT116 cells MYjGeY5kfGmxbjDhd5NigQ>? MXzJcohq[mm2aX;uJI9nKFSQSVutcYVlcWG2ZXSgWGNHPC:kZYThMYNie2WrbjD0doFve2O{aYD0bY9vKGmwIHj1cYFvKEiFVEGxOkBk\WyuczDifUBj\XSjLXzhZ5RidWG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBKSzVyIE2gNE4xOzlizszNMi=> MorxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{M{KwOlAoRjJ|MkOyNFYxRC:jPh?=
HepG2 cells NXi0U29zTnWwY4Tpc44h[XO|YYm= MWi0PEBp MX7Jcohq[mm2aX;uJI9nKHSnbH;t[ZJie2ViaX6gbJVu[W5iSHXwS|Ih[2WubIOgZYZ1\XJiNEigbJJ{KGK7IGTSRXAuWEOULVXMTXNCNCCLQ{WwJF0hQC5|IN88UU4> M4jQ[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|Mke5PFY1Lz5{M{K3PVg3PDxxYU6=
SW1116 cells NGT3SpFHfW6ldHnvckBie3OjeR?= MWeyOEBp NGf2UHdKdmirYnn0bY9vKG:oIITlcI9u\XKjc3WgbY4hcHWvYX6gV3cyOTF4IHPlcIx{KGGodHXyJFI1KGi{czDifUBVWkGSLWDDVk1GVEmVQTDhd5NigSxiSVO1NEA:KDRwMUig{txONg>? M4TmVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2Mki2O|YyLz5{NEK4Olc3OTxxYU6=
KE-97 cells MnjiR5l1d3SxeHnjbZR6KGG|c3H5 NITtT|Q4OiCq NX2xV3ZmS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hU0VvOUegZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KEOnbHzUbZRz\S2JbH:gcJVucW6nc3PlcpQh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSByLkGzJO69VS5? MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN{OEK4N{c,OjR|MkiyPFM9N2F-
Jurkat cells MVHDfZRwfG:6aXPpeJkh[XO|YYm= NES5N5I4OiCq NUnUV5BlS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUnW{a3H0JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1emVvR3zvJIx2dWmwZYPj[Y51KGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxKD1iMD6xOEDPxE1w M4rWSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{K4Nlg{Lz5{NEOyPFI5OzxxYU6=
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MCF7 cells MkLJR5l1d3SxeHnjbZR6KGG|c3H5 NF7JPZQ4OiCq M1fLOmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JGNmdGyWaYTy[U1IdG9ibIXtbY5me2OnboSgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUCgQUAxNjV{IN88UU4> NV\yRWNJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzNlgzQDNpPkK0N|I5Ojh|PD;hQi=>
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A2780 cells MXHDfZRwfG:6aXPpeJkh[XO|YYm= M{W4Rlk3KGh? M{nzdGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGEzPzhyIHPlcIx{KGGodHXyJFk3KGi{czDifUBUWkJiYYPzZZktKEmFNUCgQUAxNjJizszNMi=> NWXrU49{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlE2OjFpPkK0N|YyPTJzPD;hQi=>
HT-29 cells M2rHZWN6fG:2b4jpZ4l1gSCjc4PhfS=> NWLZVItVQTZiaB?= NE[5T2VEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJXC1{OTDj[YxteyCjZoTldkA6PiCqcoOgZpkhW1KEIHHzd4F6NCCLQ{WwJF0hOC5{IN88UU4> MlHGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NkG1NlEoRjJ2M{[xOVIyRC:jPh?=
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MCF7 cells M4\je2N6fG:2b4jpZ4l1gSCjc4PhfS=> M{W4bVk3KGh? M4PyNGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[W[2ZYKgPVYhcHK|IHL5JHNTSiCjc4PhfUwhUUN3MDC9JFAvPCEQvF2u MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4MUWyNUc,OjR|NkG1NlE9N2F-
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Raji cells MYTDfZRwfG:6aXPpeJkh[XO|YYm= MV;DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDSZYpqKGOnbHzzMEBGSzVyIE2gNkDPxE1w MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTNzNkOxO{c,OjV|MU[zNVc9N2F-
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A549 cells NV\Vfm5CS3m2b4TvfIlkcXS7IHHzd4F6 M4rvc|Q5KGh? NYDvd252S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTV2OTDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOC5yMjFOwG0v MkW3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6MkW5N|QoRjJ3OEK1PVM1RC:jPh?=
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PC3 cells NUmxeXQzS3m2b4TvfIlkcXS7IHHzd4F6 Moe2OFghcA>? NXracoZTS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWEN|IHPlcIx{KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUAxNjB|MTFOwG0v NVHTTpNtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4NlU6OzRpPkK1PFI2QTN2PD;hQi=>
MGC-803 cells NI\ZbG1HfW6ldHnvckBie3OjeR?= NE[3PVgzPCCq Mn;yTY5pcWKrdHnvckBw\iC2ZXzvcYVz[XOnIHnuJIh2dWGwIF3HR{05ODNiY3XscJMh[W[2ZYKgNlQhcHK|IHL5JHRTSVBvUFPSMWVNUVODIHHzd4F6NCCLQ{WwJF0hQC57NzFOwG0v MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjlyME[1Okc,OjZ7MEC2OVY9N2F-
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MDA-MB-231 cells M2Xle2Z2dmO2aX;uJIF{e2G7 MX[xOkBp MV3Jcohq[mm2aX;uJI9nKHKndHnuc4Jt[XO2b33hJJBzd3SnaX6gdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYX\0[ZIhOTZiaILzJIJ6KEixZXPod5QhOzN|NEKgd5RicW6rbnegZoF{\WRiZnz1c5Jme2OnbnPlJIF{e2G7LDDJR|UxKD1iMD6wOlYh|ryPLh?= MkG4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2M{GzOFIoRjJ6NEOxN|QzRC:jPh?=
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HEK293 cells NYn6VXhIS3m2b4TvfIlkcXS7IHHzd4F6 NEXJdow4OiCq MVrDfZRwfG:6aXPpeJkh[WejaX7zeEBJTUt{OUOgZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4h[2WubDD2bYFjcWyrdImgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSncjDHcI8hdHWvaX7ld4NmdnRiYYPzZZktKEOFNUCgQUAxNjByM{W0JO69VS5? NXS3Wld[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki2NlQ4ODFpPkK4OlI1PzBzPD;hQi=>
BT549 cells M{D5bmN6fG:2b4jpZ4l1gSCjc4PhfS=> NETXO5EzPCCq M1PHUWN6fG:2b4jpZ{Bi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFLUOVQ6KGOnbHzzJIlv[3WkYYTl[EBnd3JiMkSgbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IECuNFgh|ryPLh?= MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDdyNUSzNkc,Ojh5MEW0N|I9N2F-
MDA-MB-468 cells M{n6cWN6fG:2b4jpZ4l1gSCjc4PhfS=> NV3N[IFSOjRiaB?= Mkm3R5l1d3SxeHnjJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTR4ODDj[YxteyCrbnP1ZoF1\WRiZn;yJFI1KGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUAxNjF3IN88UU4> M1PGV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6N{C1OFMzLz5{OEewOVQ{OjxxYU6=
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L929 cells M1zYdGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 MXG1JIRigXN? M1LvfGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgcY92e2ViTEmyPUBk\WyuczDh[pRmeiB3IHThfZMh[nliV2PUMVEh[XO|YYmsJGlEPTBiPTCwMlIh|ryPLh?= NIHXZlk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEm1OlkyPSd-Mki5OVY6OTV:L3G+
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HepG2 cells NVf4ZnpLS3m2b4TvfIlkcXS7IHHzd4F6 NVfUc5o2OTByIIXN M1zBO|Mh\GG7cx?= NGfNbJFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJ\XCJMjDj[YxteyCjdDCxNFAhfU1iYX\0[ZIhOyCmYYnzJIJ6KEOnbHzUbZRmei2JbH:gcJVucW6nc3PlcpQh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVAhRSByLkCxPEDPxE1w NGrx[Y89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEm5N|ExPid-Mki5PVMyODZ:L3G+
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Assay
Methods Test Index PMID
Western blot FAK / RIP ; p-Akt / Akt / PARP /Cleaved PARP ; Ambra1 15121855 24174874 24587252
Growth inhibition assay Cell viability 25215174
Immunofluorescence Phalloidin / Type II collagen ; Tubulin / Actin ; FAK 4.47 ; cleaved-caspase 3 ; Annexin ; Pyk2 22684244 25215174 15121855 19840952 15140398 19880522
In vivo In the gerbil and rat ischemia models, Staurosporine pretreatment (0.1-10 ng) before ischemia prevents neuronal damage in a dose-dependent manner, suggesting the involvement of PKC in CAl pyramidal cell death after ischemia. [8]

Protocol (from reference)

Kinase Assay:

[1]

  • Enzyme assay and binding assay:

    Protein kinase C is assayed in a reaction mixture (0.25 mL) containing 5 μmol of Tris/HCl, pH 7.5, 2.5 μmol of magnesium acetate, 50 μg of histone II S, 20 μg of phosphatidylserine, 0.88 μg of diolein, 125 nmol of CaCl2, 1.25 nmol of [γ-32]ATP (5-10 × 104 cpm/nmol) and 5 μg of partially purified enzyme. The binding of [3H]PDBu to protein kinase C is determined: Reaction mixture (200 μL contained 4 μmo1 of Tris/malate, pH 6.8, 20 μmol of KCl, 30 nmol of CaC12, 20 μg of phosphatidylserine, 5 μg of partially purified protein kinase C, 0.5% (final concentration) of DMSO,10 pmol of [3H]PDBu (l-3 × 104 cpm/pmol) and 10 μL of various amounts of Staurosporine.

Cell Research:

[3]

  • Cell lines: PC12
  • Concentrations: Dissolved in DMSO, final concentration 1 μM
  • Incubation Time: ~32 hours
  • Method:

    Cells are exposed to Staurosporine for ~32 hours. Cells are fixed in 4% paraformaldehyde and stained with the DNA-binding dye Hoechst 33342. Cells are visualized under epifluorescence illumination, and the percentage of apoptotic cells (cells with condensed and fragmented DNA) is determined.

Animal Research:

[8]

  • Animal Models: Male Mongolian gerbils or male Wistar rats subjected to transient ischemia
  • Dosages: ~10 ng
  • Administration: Stereotaxically administered into the bilateral CAl subfield of the hippocampus

Solubility (25°C)

In vitro

DMSO 4 mg/mL
(8.57 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 466.53
Formula

C28H26N4O3

CAS No. 62996-74-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC12C(C(CC(O1)N3C4=CC=CC=C4C5=C6C(=C7C8=CC=CC=C8N2C7=C53)CNC6=O)NC)OC

In vivo Formulation Calculator (Clear solution)

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

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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

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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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