Staurosporine

Catalog No.S1421 Synonyms: CGP 41251

Staurosporine Chemical Structure

Molecular Weight(MW): 466.53

Staurosporine 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.

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Cited by 19 Publications

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Biological Activity

Description Staurosporine 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)
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 HeLa cells M3K0[mN6fG:2b4jpZ:Kh[XO|YYm= Ml21OFghcA>? MXvDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDI[WxiKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;NHWtNFYh|ryPLh?= MlfyNlE{QDhzOUG=
human colon cancer cell line (LoVo cells) MVLQdo9tcW[ncnH0bY9vKGG|c3H5 NYrCNolnSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDjc4xwdiClYX7j[ZIh[2WubDDsbY5mKCiOb2\vJINmdGy|KTD1d4lv\yCPVGSgZZN{[XluIFnDOVA:OC5yMEGg{txONg>? M3rtSlEyPTlzNUC1
human LoVo cells MlnMVJJwdGmoZYLheIlwdiCjc4PhfS=> NVj3[JVEPDhidH:gO|IhcA>? NXzlUFJ2SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDMc3ZwKGOnbHzzJIFnfGW{IES4JJRwKDd{IHjyd{BjgSCPVGSgZZN{[Xl? NFrESIszOjF6MkmyPS=>
P19 cells M{TMZWZ2dmO2aX;uJIF{e2G7 M1;UbGlvcGmkaYTpc44hd2ZiUHzheIVt\XRvZHXybZZm\CCpcn;3eIgh\mGldH;yJJJm[2WydH;yJIlvKFBzOTDj[YxteyxiSVO1NF0xNjByMjFOwG0v NXPieJpEOTV5N{G0NVk>
human BJ cells MljRR5l1d3SxeHnjxsBie3OjeR?= M4LuNFczKGh? MX\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDCTkBk\WyuczDh[pRmeiB5MjDodpMh[nliQ3HsZ4VqdiCDTTDhd5NigSxiSVO1NF0xNjByMjFOwG0v NFvFbXIzOjl{MUC4NS=>
human HT-29 cells MVHGeY5kfGmxbjDhd5NigQ>? M{LGZlIhcA>? MYTF[oZm[3Rib36gcYl1d2Oqb37kdolidCCvZX3idoFv\SCyb4TlcpRq[WxiaX6gbJVu[W5iSGStNlkh[2WubIOgZYZ1\XJiMjDodpMhfXOrbnegTmMuOSC|dHHpcolv\yCkeTDmcJVwemW|Y3XuZ4Uh[XO|YYm= NHjZSVYzOTR{OEO3OS=>
human A549 cells NXHhVmRGS3m2b4TvfIlkyqCjc4PhfS=> MlezO|IhcA>? NU[xWJF5S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTV2OTDj[YxteyCjZoTldkA4OiCqcoOgZpkhe3WuZn;ybI9l[W2rbnWgRkBu\XSqb3S= M3;TbFE5PDh2N{e1
human HT-29 cells NHK1cZZHfW6ldHnvckBie3OjeR?= NWPCdVV5UW6qaXLpeIlwdiCxZjDtbZRw[2ixbnTybYFtKG2nbXLyZY5mKHCxdHXueIlidCCrbjDoeY1idiCKVD2yPUBk\WyuczD1d4lv\yCMQ{Gg[JlmKHO2YXnubY5oKGK7IH\seY9z\XOlZX7j[UBxdGG2ZTDy[YFl\XJiYYPzZZktKEmFNUC9Nk42KG6P MojNNlE2OTN{OUO=
human HT-29 cells M2i3WGZ2dmO2aX;uJIF{e2G7 M{PHPVIhcA>? NW[xc2pCUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDIWE0zQSClZXzsd{Bie3Onc4Pl[EBz\WS3Y4Tpc44hd2ZibXn0c4Npd26mcnnhcEBu\W2kcnHu[UBxd3SnboTpZYwh[W[2ZYKgNkBpenNiYomgeZNqdmdiSlOxJJN1[WmwaX7nJIJ6KG[udX;y[ZNk\W6lZTDj[YxtNWKjc3XkJIF{e2G7LDDFR|UxRTJwNjDuUU4> NEPaO4ozOTl5M{GwNS=>
Sf9 cells NXLGeVJvTnWwY4Tpc44h[XO|YYm= NIfPUodKdmirYnn0bY9vKG:oIHj1cYFvKFO7azDlfJBz\XO|ZXSgbY4hW2Z7IHPlcIx{NCCLQ{WwQVMhdk1w NYrpXoxXOTh6MkO3PFQ>
human HUVEC NXLXd2lIWHKxbHnm[ZJifGmxbjDhd5NigQ>? MkDTOFghfG9iN{KgbC=> MV;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiXVlXDJIFnfGW{IES4JJRwKDd{IHjyd{BjgSCPVGSgZZN{[Xl? NYr6dWNJOjJzOEK5Nlk>
P19 cells M{n1XGZ2dmO2aX;uJIF{e2G7 MoLlTY5pcWKrdHnvckBw\iCScn;0[YlvKEurbnHz[UBCKGmwIGCxPUBk\WyuczygTWM2OD12IH7NMi=> M2fyfFE2PzdzNEG5
Sf9 cells MY\GeY5kfGmxbjDhd5NigQ>? MojITY5pcWKrdHnvckBw\iCqdX3hckBHgW5iZYjwdoV{e2WmIHnuJHNnQSClZXzsd{Bi\nSncjCxJI1qdiCkeTDFUGlUSSCrbjDwdoV{\W6lZTDv[kAyKHWvb3yvUEBCXFB? MmfHNVc{OTV6NUO=
Sf21 cells NWLifm1[TnWwY4Tpc44h[XO|YYm= MVnJcohq[mm2aX;uJI9nKEqDS{Og[ZhxemW|c3XkJIlvKFOoMkGgZ4VtdHNuIFnDOVA:PiCwTT6= MYGxO|A5QDB3OR?=
human colon carcinoma cell line HCT116 NWW5OVBGTnWwY4Tpc44h[XO|YYm= NF\sR|NEd26lZX70doF1cW:wIILldZVqemWmIH\vdkBoem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBkd2yxbjDjZZJkcW6xbXGgZ4VtdCCuaX7lJGhEXDFzNjygTWM2OD14IH7NMi=> MUmxOVU{PzN2NR?=
human ST486 cells NIPjZmRRem:uaX\ldoF1cW:wIHHzd4F6 MnL4OFghfG9iN{KgbC=> MkHjRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVVES4OkBk\WyuczDh[pRmeiB2ODD0c{A4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVchdk1w Ml7aNlIyQDJ7Mkm=
human MDA-MB-231 cells NFjBbZNEgXSxdH;4bYPDqGG|c3H5 MX63NkBp MorSR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDh[pRmeiB5MjDodpMh[nlic4Xs[o9zcG:mYX3pcoUhSiCvZYToc4QtKEeLNUC9O{4yKG6PLh?= NX;od5MzOTh2OES3O|U>
P19 cells MmTQSpVv[3Srb36gZZN{[Xl? MWfJcohq[mm2aX;uJI9nKEO7Y3zpck1l\XCnbnTlcpQhc2mwYYPlJFEhcW5iUEG5JINmdGy|LDDJR|UxRThibl2u MmjZNVU4PzF2MUm=
human DLD1 cells MmrZVJJwdGmoZYLheIlwdiCjc4PhfS=> MnTIOFguPzJiaB?= M{jyeWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iRFzENUBk\WyuczDh[pRmeiB2ODD0c{A4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVkhdk1w NUDBRWVDOjJzOEK5Nlk>
insect cells NVjuO|Q6TnWwY4Tpc44h[XO|YYm= M2rN[2lvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiUHntNUBmgHC{ZYPz[YQhcW5iaX7z[YN1KGOnbHzzJIJ6KEiWUl[sJGlEPTB;MUCgcm0v MlXqNVkyPzlyN{[=
V79 MZ cells MYLGeY5kfGmxbjDhd5NigQ>? M2Dsb2lvcGmkaYTpc44hd2ZiaIXtZY4h[Wymb4P0[ZJwdmVic4nueIhie2ViZYjwdoV{e2WmIHnuJHY4QSCPWjDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGGuZH;zeIVzd26nIIP5cpRp\XOrczygTWM2OD1zMTDuUU4> NFjjOY8zPDR{MkWxPS=>
P19 cells MV3GeY5kfGmxbjDhd5NigQ>? Mo[xTY5pcWKrdHnvckBw\iCYYYPjeYxieiCnbnTveIhmdGmjbDDndo94fGhiZnHjeI9zKHKnY3XweI9zKGmwIGCxPUBk\WyuczygTWM2OD1zNDDuUU4> M2f6UVE2PzdzNEG5
Sf9 cells MlztSpVv[3Srb36gZZN{[Xl? NXnhTI5ZOjBibXnudy=> M4jEbGlvcGmkaYTpc44hd2ZiaIXtZY4hTnmwIHX4dJJme3OnZDDpckBU\jliY3XscJMh[W[2ZYKgNlAhdWmwczDifUBGVEmVQTDpckBxemW|ZX7j[UBw\iBzIIXtc4wwVCCDVGCsJGlEPTB;MUWgcm0v NX7OWoZjOTd|MUW4OVM>
human PBMC MoHGSpVv[3Srb36gZZN{[Xl? NF\2SW8zPCCq M2jlRnN2eHC{ZYPzbY9vKG:oIFnMNkBxem:mdXP0bY9vKGmwIHj1cYFvKFCETVOgZYZ1\XJiMkSgbJJ{KGK7IFXMTXNCNCCLQ{WwQVE3KG6PLh?= M{ToT|E5PTh3MES2
human A549 cells MX7DfZRwfG:6aXRCpIF{e2G7 M4\RWFQ5KGh? MU\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmgMEBKSzVyPUKwJI5ONg>? NXz1ZmpHOjV6MkW5N|Q>
human CEM cells MXnDfZRwfG:6aXRCpIF{e2G7 M4HPXVczKGh? M{fDcWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGNGVSClZXzsd{Bi\nSncjC3NkBpenNiYomgR4Ft[2WrbjDBUUBie3OjeTygTWM2OD1{MzDuUU4> NGDNcIMzOjl{MUC4NS=>
human HeLa cells MmPTR5l1d3SxeHnjxsBie3OjeR?= MnfvOFghcA>? NWTHSXJlS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWOYTDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVI2KG6PLh?= NWj0d2tnOjV6MkW5N|Q>
human PC3 cells M{XD[WN6fG:2b4jpZ:Kh[XO|YYm= MWm0PEBp NInNPZFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSzNiY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUAtKEmFNUC9N|Ehdk1w M1j2U|I2QDJ3OUO0
human SF268 cells NHS1XIdEgXSxdH;4bYPDqGG|c3H5 M{XrT|Q5KGh? MnrCR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2YzPjhiY3XscJMh[W[2ZYKgOFghcHK|IHL5JHNTSiCjc4PhfUwhT0l3ME20OEBvVS5? NEK2R44zOTVzM{K5OC=>
human MCF7 cells NWnKRYd5S3m2b4TvfIlkyqCjc4PhfS=> MYS0PEBp NW\0W3p4S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVUxKG6PLh?= MUmyNVM5QDF7MR?=
HEK293 cells NELk[oVEgXSxdH;4bYPDqGG|c3H5 MXm3NkBp NGrmUpBEgXSxdH;4bYNqfHliYXfhbY5{fCCKRVuyPVMh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxVcXSnclfsc{Bie3OjeTygTWM2OD13NjDuUU4> NITue2gzPDd4M{K2Ni=>
HUE cells MUfGeY5kfGmxbjDhd5NigQ>? M2[wT|kxKG2rboO= MVjJcohq[mm2aX;uJI9nKF[HR1\SNkBqdiCKVVWgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCYRVfGMYlv\HWlZXSgZZV1d3Cqb4PwbI9zgWyjdHnvckB1emWjdHXkJIZweiB7MDDtbY5{KGKnZn;y[UBXTUeIIHPoZYxt\W6pZTDifUBGVEmVQTygTWM2OD15MDDuUU4> MYiyNFE4ODF4Mx?=
human A431 cells MVzDfZRwfG:6aXRCpIF{e2G7 MUOyOEAhcA>? NHfqeI1EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPDNzIHPlcIx{KGGodHXyJFI1KGi{czD1d4lv\yCDbn7lfIlvKF[nRlnUR{9xem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nJIJ6KE2WVDDhd5NigSxiSVO1NF04OCCwTT6= NWjPbJZ2OjJ3NEGwOVE>
human Jurkat cells NVrUPHlGWHKxbHnm[ZJifGmxbjDhd5NigQ>? M3;3N2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgTmFMOyCneIDy[ZN{cW6pIFnMNk1{fGmvdXzheIVlKGi3bXHuJGp2emujdDDj[YxteyxiSVO1NF04OSCwTT6= MVGxPVQzPzJyMx?=
HEK293 cells MV3GeY5kfGmxbjDhd5NigQ>? M{HWNWlvcGmkaYTpc44hd2ZiSVytPEBz\WynYYPlJIJ6KEiHS{K5N{Bk\WyuczDlfJBz\XO|aX7nJHBMSy2kZYThNkwhUUN3ME23O{BvVS5? MkHTNVU4PzF2MUm=
human KE-97 cells NHvjPFVEgXSxdH;4bYPDqGG|c3H5 NETCRZg4OiCq NUXnOHZ1S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hU0VvOUegZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KEOnbHzUbZRz\S2JbH:gcJVucW6nc3PlcpQh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5zMzFOwG0v NFLoNpgzPDN{OEK4Ny=>
human CHOK1 cells MlvhR5l1d3SxeHnjxsBie3OjeR?= NYn1VGpRPDhiaB?= M{fsSWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGNJV0tzIHPlcIx{KGGodHXyJFQ5KGi{czDifUBUWkJiYYPzZZnwxIxiSVO1NF0xNjF|IN88UU4> MkLHNlE2OTN{OUS=
mouse NIH/3T3 cells NWnXc3pSS3m2b4TvfIlkyqCjc4PhfS=> NF;YeFY6PiCq NEnmOHREgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBPUUhxM2SzJINmdGy|IHHmeIVzKDl4IHjyd{BjgSCVUlKgZZN{[XluIFnDOVA:OC5{IN88UU4> NVvmOZdMOjR|NkG1NlE>
human A2780 cells NVHCfZozS3m2b4TvfIlkyqCjc4PhfS=> M1LnPFk3KGh? NVjpeYZCS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTJ5OECgZ4VtdHNiYX\0[ZIhQTZiaILzJIJ6KFOUQjDhd5NigSxiSVO1NF0xNjJizszNMi=> Mn7zNlQ{PjF3MkG=
human 8505C cells NUXKeFY5S3m2b4TvfIlkyqCjc4PhfS=> MmfyPVYhcA>? M1K2VGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJFg2ODWFIHPlcIx{KGGodHXyJFk3KGi{czDifUBUWkJiYYPzZZktKEmFNUC9NE4zKM7:TT6= MnHNNlQ{PjF3MkG=
human 518A2 cells NWDLXWhDS3m2b4TvfIlkyqCjc4PhfS=> NH3V[lc6PiCq NE\iNpBEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckA2OTiDMjDj[YxteyCjZoTldkA6PiCqcoOgZpkhW1KEIHHzd4F697zOIFnDOVA:OC5{IN88UU4> NF3Y[m4zPDN4MUWyNS=>
human HuH7 cells M4\5cGN6fG:2b4jpZ:Kh[XO|YYm= M{Xt[VczKGh? NEX2fW5EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJfUh5IHPlcIx{KGGodHXyJFczKGi{czDifUBE\WyuVHn0doUuT2yxIHz1cYlv\XOlZX70JINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjNizszNMi=> MnXQNlQ{Ojh{OEO=
FL5.12-Akt1 cells NVf4XnJ4WHKxbHnm[ZJifGmxbjDhd5NigQ>? NID2WVRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JGZNPS5zMj3Bb5QyKGOnbHzzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjJ7IN88UU4> M1LKe|E3PDB|NkK2
human MiaPaCa-2 cells NVzi[3p4WHKxbHnm[ZJifGmxbjDhd5NigQ>? NEXvfW1CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3pZXBiS2FvMjDj[YxteyxiSVO1NF0xNjN5IN88UU4> MkDLNVY1OTN5OEC=
human BGC823 cells M3W4Z2N6fG:2b4jpZ:Kh[XO|YYm= M2TiRVczKGh? NXT2WIx5S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSkeFOEKzJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCFZXzsWIl1emVvR3zvJIx2dWmwZYPj[Y51KGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwM{ig{txONg>? MVSyOFMzQDJ6Mx?=
human MCF7 cells Mlf2R5l1d3SxeHnjxsBie3OjeR?= NX;NRWllQTZiaB?= MoPUR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{Bi\nSncjC5OkBpenNiYomgV3JDKGG|c3H5MEBKSzVyPUCuOEDPxE1w MlX3NlQ{PjF3MkG=
human A549 cells MmPnR5l1d3SxeHnjxsBie3OjeR?= MUm5OkBp Mk\UR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVU1QSClZXzsd{Bi\nSncjC5OkBpenNiYomgV3JDKGG|c3H5MEBKSzVyPUCuOkDPxE1w MUSyOFM3OTV{MR?=
HEK293 cells MkW1R5l1d3SxeHnjxsBie3OjeR?= M3rVN2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KEiHS{K5N{Bk\WyuczygSWM2OD1{IN88UU4> M{DGZVI2OzF4M{G3
human Raji cells  NEDBcJlEgXSxdH;4bYPDqGG|c3H5 NW[1fYlXS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWmGsaTDj[YxteyxiRVO1NF0zKM7:TT6= MYGyOVMyPjNzNx?=
human HepG2 cells NXi0R3VsS3m2b4TvfIlkyqCjc4PhfS=> MVXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDI[ZBIOiClZXzsd{whTUN3ME2yJO69VS5? M3jJV|I2OzF4M{G3
human BJ cells MlPrR5l1d3SxeHnjxsBie3OjeR?= M135cWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGJLKGOnbHzzMEBGSzVyPUKg{txONg>? NY\FdXYxOjV|MU[zNVc>
human U937 cells NHTKO4VEgXSxdH;4bYPDqGG|c3H5 MmmzR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gWVk{PyClZXzsd{whUUN3ME2yJO69VS5? M4LLb|E4ODh6ME[3

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-Akt / Akt / PARP /Cleaved PARP; 

PubMed: 24174874     


Western blot analysis for Akt, P-Akt, and cleaved poly(ADP-ribose) polymerase. U87 cells were incubated with 200 nM, 10 nM, and 0.1 nM of staurosporine encapsulated in liposomes and staurosporine for 32 hours.

FAK / RIP; 

PubMed: 15121855     


Western blot (WB) analysis of BT-20 and BT-474 lysates treated with staurosporine (200 nM). Control cells were treated with dimethyl sulfoxide for 18 h.

Ambra1; 

PubMed: 24587252     


SW620 cells treated with various doses of staurosporine for 6 h. Ambra1 levels were measured by Western blot. 

24174874 15121855 24587252
Growth inhibition assay
Cell viability; 

PubMed: 25215174     


Staurosporine reduces cerebellar astrocytes viability. (a) Cerebellar astrocytes were treated with staurosporine 0.1 μM, 0.25 μM, and 0.5 μM for 24 h and the cell viability was measured by MTT transformation. (b) Cerebellar astrocytes were treated with staurosporine 0.5 μM for 6, 12, and 24 h and the cell viability was measured by MTT transformation. Data are presented as mean ± SEM of four independent experiments. ∗ is significantly different from control (P < 0.05).

25215174
Immunofluorescence
Tubulin / Actin; 

PubMed: 25215174     


Morphological changes of astrocytes induced by St are evidenced by the rearrangement of cytoskeletal proteins. Astrocytes were treated with St (0.5 μM) for 12 hours and then were labelled with rhodamine-phalloidin or immunostained for tubulin. Representative images of phase contrast, rhodamine-phalloidin, and tubulin are shown in control and St treated astrocytes. Scale bar represents 50 μm.

Phalloidin / Type II collagen; 

PubMed: 22684244     


Cell were cultured in the absence (a-f) or presence of staurosporine (STSN, 5 × 10-9M) or cytochalasin D (CD, 1 µg/ml) for 1 (upper panel) or 2 (lower panel) days at low density and stained for F-actin (Phalloidin) and type II collagen (Type II). STSN: Staurosporine.

Pyk2; 

PubMed: 19880522     


Pyk2 translocates to the nucleus upon staurosporine addition to ID8 cells. Confocal immunofluorescent analysis of endogenous Pyk2 upon DMSO (control) or 1 μm staurosporine addition for 2 h. The scale bar is 10 μm. 

Annexin; 

PubMed: 15140398     


Induction of apoptosis with staurosporine resulting in activation of the ICE-NIRF probe. Gli36 cells were treated with 50 µM staurosporine for 24 hours (A-C) or with the same percentage of DMSO (0.01%) to which experimental wells were exposed (D-488nm laser, E-633nm laser and F-bright field). To examine the role of caspase-1 in staurosporine-induced apoptosis and probe activation, cells were coincubated in caspase-1 inhibitor (10 µM) and staurosporine (G-I). Staurosporine induces apoptosis, indicated by the positive annexin staining viewed with the 488-nm laser (A), which colocalized with activated probe viewed with the 633-nm laser (B). Coincubation of the caspase-1 inhibitor with staurosporine did not completely block apoptosis, indicated by the relatively higher number of apoptotic cells stained with annexin (G), as those that activated the probe (H). Magnification, x 40; scale bar, 50 µM.

cleaved-caspase 3; 

PubMed: 19840952     


Representative images (×1000 magnification) showing vehicle treated (C) and staurosporine treated (D) cells stained with anti-cleaved caspase 3 antibody and DAPI.

FAK 4.47; 

PubMed: 15121855     


BT-20 or BT-474 cell culture were plated on six-well plates and were treated with staurosporine (200 nM) after 24 h. After 6 h of treatment, cells were immunostained with anti-FAK 4.47 antibody (white arrowheads mark some focal adhesions).

25215174 22684244 19880522 15140398 19840952 15121855
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

Kinase Assay:

[1]

+ Expand

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]

+ Expand
  • 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.


    (Only for Reference)
Animal Research:

[8]

+ Expand
  • Animal Models: Male Mongolian gerbils or male Wistar rats subjected to transient ischemia
  • Formulation: Dissolved in DMSO, and diluted in saline
  • Dosages: ~10 ng
  • Administration: Stereotaxically administered into the bilateral CAl subfield of the hippocampus
    (Only for Reference)

Solubility (25°C)

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

* 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 466.53
Formula

C28H26N4O3

CAS No. 62996-74-1
Storage powder
in solvent
Synonyms CGP 41251

Bio Calculators

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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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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00301938 Completed Accelerated Phase Chronic Myelogenous Leukemia|Adult Acute Megakaryoblastic Leukemia (M7)|Adult Acute Minimally Differentiated Myeloid Leukemia (M0)|Adult Acute Monoblastic Leukemia (M5a)|Adult Acute Monocytic Leukemia (M5b)|Adult Acute Myeloblastic Leukemia With Maturation (M2)|Adult Acute Myeloblastic Leukemia Without Maturation (M1)|Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)|Adult Acute Myeloid Leukemia With t(15;17)(q22;q12)|Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)|Adult Acute Myelomonocytic Leukemia (M4)|Adult Acute Promyelocytic Leukemia (M3)|Adult Erythroleukemia (M6a)|Adult Pure Erythroid Leukemia (M6b)|Blastic Phase Chronic Myelogenous Leukemia|Myelodysplastic/Myeloproliferative Neoplasms|Previously Treated Myelodysplastic Syndromes|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Adult Acute Myeloid Leukemia|Relapsing Chronic Myelogenous Leukemia|Secondary Acute Myeloid Leukemia|T-cell Adult Acute Lymphoblastic Leukemia|Untreated Adult Acute Lymphoblastic Leukemia|Untreated Adult Acute Myeloid Leukemia National Cancer Institute (NCI) December 2005 Phase 1
NCT00301938 Completed Accelerated Phase Chronic Myelogenous Leukemia|Adult Acute Megakaryoblastic Leukemia (M7)|Adult Acute Minimally Differentiated Myeloid Leukemia (M0)|Adult Acute Monoblastic Leukemia (M5a)|Adult Acute Monocytic Leukemia (M5b)|Adult Acute Myeloblastic Leukemia With Maturation (M2)|Adult Acute Myeloblastic Leukemia Without Maturation (M1)|Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)|Adult Acute Myeloid Leukemia With t(15;17)(q22;q12)|Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)|Adult Acute Myelomonocytic Leukemia (M4)|Adult Acute Promyelocytic Leukemia (M3)|Adult Erythroleukemia (M6a)|Adult Pure Erythroid Leukemia (M6b)|Blastic Phase Chronic Myelogenous Leukemia|Myelodysplastic/Myeloproliferative Neoplasms|Previously Treated Myelodysplastic Syndromes|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Adult Acute Myeloid Leukemia|Relapsing Chronic Myelogenous Leukemia|Secondary Acute Myeloid Leukemia|T-cell Adult Acute Lymphoblastic Leukemia|Untreated Adult Acute Lymphoblastic Leukemia|Untreated Adult Acute Myeloid Leukemia National Cancer Institute (NCI) December 2005 Phase 1
NCT00098956 Completed Extensive Stage Small Cell Lung Cancer|Recurrent Small Cell Lung Cancer National Cancer Institute (NCI) January 2005 Phase 2
NCT00098956 Completed Extensive Stage Small Cell Lung Cancer|Recurrent Small Cell Lung Cancer National Cancer Institute (NCI) January 2005 Phase 2
NCT00082017 Terminated Lymphoma Large-Cell Ki-1|Lymphoma T-Cell National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) April 5 2004 Phase 2
NCT00082017 Terminated Lymphoma Large-Cell Ki-1|Lymphoma T-Cell National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) April 5 2004 Phase 2

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