Staurosporine

Staurosporineは1種の有効なPKC阻害剤で、無細胞試験でPKCα、PKCγ とPKCηに作用します。そして、これらのIC50値は2 nM、5 nM と 4 nMそれぞれに分かれます。StaurosporineはPKCδ(20 nM)とPKCε(73 nM)に作用することが弱くて、PKCζ (1086 nM)に対する活性も低いですが、他のキナーゼ(例えば、PKA、PKG、S6K、CaMKII等)に抑制活性を現れます。臨床3期。

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USD 340 あり

Staurosporine 化学構造
分子量: 466.53

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製品説明

  • Compare PKC Inhibitors
    PKC製品生物活性の比較
  • 研究分野
  • Combination Therapy
    併用療法
  • Staurosporineのメカニズム

製品の説明

生物活性

製品説明 Staurosporineは1種の有効なPKC阻害剤で、無細胞試験でPKCα、PKCγ とPKCηに作用します。そして、これらのIC50値は2 nM、5 nM と 4 nMそれぞれに分かれます。StaurosporineはPKCδ(20 nM)とPKCε(73 nM)に作用することが弱くて、PKCζ (1086 nM)に対する活性も低いですが、他のキナーゼ(例えば、PKA、PKG、S6K、CaMKII等)に抑制活性を現れます。臨床3期。
ターゲット PKCα PKCγ PKCη PKCδ PKCε PKCζ
IC50 2 nM 5 nM 4 nM 20 nM 73 nM 1086 nM [1]

In vitro試験 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
human HeLa cells MXzDfZRwfG:6aXRCpIF{e2G7 MYO0PEBp NULIXHY2S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWOYTDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVRmNTB4IN88UU4> MmHONlE{QDhzOUG=
human colon cancer cell line (LoVo cells) MUPQdo9tcW[ncnH0bY9vKGG|c3H5 MkHYRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiClb3zvckBk[W6lZYKgZ4VtdCCuaX7lJEhNd1[xIHPlcIx{MSC3c3nu[{BOXFRiYYPzZZktKEmFNUC9NE4xODFizszNMi=> M3jLZVEyPTlzNUC1
human LoVo cells NYP6c41bWHKxbHnm[ZJifGmxbjDhd5NigQ>? NFzCWmY1QCC2bzC3NkBp MUPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEyxVn:gZ4VtdHNiYX\0[ZIhPDhidH:gO|IhcHK|IHL5JG1VXCCjc4PhfS=> NG\ZN3IzOjF6MkmyPS=>
P19 cells MXnGeY5kfGmxbjDhd5NigQ>? NHTSV2NKdmirYnn0bY9vKG:oIGDsZZRmdGW2LXTldol3\WRiZ4Lve5RpKG[jY4TvdkBz\WOncITvdkBqdiCSMUmgZ4VtdHNuIFnDOVA:OC5yMEKg{txONg>? NWLiUlZDOTV5N{G0NVk>
human BJ cells NIf2RVhEgXSxdH;4bYPDqGG|c3H5 NELMUVU4OiCq MUPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDCTkBk\WyuczDh[pRmeiB5MjDodpMh[nliQ3HsZ4VqdiCDTTDhd5NigSxiSVO1NF0xNjByMjFOwG0v MUmyNlkzOTB6MR?=
human HT-29 cells MnTJSpVv[3Srb36gZZN{[Xl? MmTUNkBp NEPHXmxG\m[nY4Sgc44hdWm2b3Poc45lemmjbDDt[Y1jemGwZTDwc5RmdnSrYXygbY4hcHWvYX6gTHQuOjliY3XscJMh[W[2ZYKgNkBpenNidYPpcochUkNvMTDzeIFqdmmwZzDifUBndHWxcnXzZ4Vv[2ViYYPzZZk> NVjieVc{OjF2MkizO|U>
human A549 cells M4jlcGN6fG:2b4jpZ:Kh[XO|YYm= NIPHfVA4OiCq MXTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDzeYxnd3Kqb3ThcYlv\SCEIH3leIhw\A>? M3HDRVE5PDh2N{e1
human HT-29 cells NXW5W5k5TnWwY4Tpc44h[XO|YYm= NWLYXVk1UW6qaXLpeIlwdiCxZjDtbZRw[2ixbnTybYFtKG2nbXLyZY5mKHCxdHXueIlidCCrbjDoeY1idiCKVD2yPUBk\WyuczD1d4lv\yCMQ{Gg[JlmKHO2YXnubY5oKGK7IH\seY9z\XOlZX7j[UBxdGG2ZTDy[YFl\XJiYYPzZZktKEmFNUC9Nk42KG6P MUmyNVUyOzJ7Mx?=
human HT-29 cells NHvNN3pHfW6ldHnvckBie3OjeR?= NHrvcHEzKGh? NVjTR5VqUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDIWE0zQSClZXzsd{Bie3Onc4Pl[EBz\WS3Y4Tpc44hd2ZibXn0c4Npd26mcnnhcEBu\W2kcnHu[UBxd3SnboTpZYwh[W[2ZYKgNkBpenNiYomgeZNqdmdiSlOxJJN1[WmwaX7nJIJ6KG[udX;y[ZNk\W6lZTDj[YxtNWKjc3XkJIF{e2G7LDDFR|UxRTJwNjDuUU4> M3LGbVIyQTd|MUCx
Sf9 cells NVe4[4x7TnWwY4Tpc44h[XO|YYm= MV3Jcohq[mm2aX;uJI9nKGi3bXHuJHN6cyCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzMEBKSzVyPUOgcm0v NUTGbJc5OTh6MkO3PFQ>
human HUVEC MWfQdo9tcW[ncnH0bY9vKGG|c3H5 NEjrRlQ1QCC2bzC3NkBp MWLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiXVlXDJIFnfGW{IES4JJRwKDd{IHjyd{BjgSCPVGSgZZN{[Xl? MorINlIyQDJ7Mkm=
P19 cells NIjnU3pHfW6ldHnvckBie3OjeR?= Mn\YTY5pcWKrdHnvckBw\iCScn;0[YlvKEurbnHz[UBCKGmwIGCxPUBk\WyuczygTWM2OD12IH7NMi=> M3LUN|E2PzdzNEG5
Sf9 cells NWnBT4pyTnWwY4Tpc44h[XO|YYm= NXTldmZwUW6qaXLpeIlwdiCxZjDoeY1idiCIeX6g[ZhxemW|c3XkJIlvKFOoOTDj[YxteyCjZoTldkAyKG2rbjDifUBGVEmVQTDpckBxemW|ZX7j[UBw\iBzIIXtc4wwVCCDVGC= M2f4TVE4OzF3OEWz
Sf21 cells MVXGeY5kfGmxbjDhd5NigQ>? M{fofWlvcGmkaYTpc44hd2ZiSlHLN{BmgHC{ZYPz[YQhcW5iU3[yNUBk\WyuczygTWM2OD14IH7NMi=> M3nUXlE4ODh6MEW5
human colon carcinoma cell line HCT116 NV34dWI5TnWwY4Tpc44h[XO|YYm= MXvDc45k\W62cnH0bY9vKHKncYXpdoVlKG[xcjDndo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDjc4xwdiClYYLjbY5wdWFiY3XscEBtcW6nIFjDWFEyPixiSVO1NF03KG6PLh?= M{DCO|E2PTN5M{S1
human ST486 cells MYfQdo9tcW[ncnH0bY9vKGG|c3H5 MXy0PEB1dyB5MjDo MXPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOWNEi2JINmdGy|IHHmeIVzKDR6IITvJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9O{BvVS5? NFzjOYYzOjF6MkmyPS=>
human MDA-MB-231 cells NWTXfJM3S3m2b4TvfIlkyqCjc4PhfS=> M2fWcFczKGh? MlnHR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDh[pRmeiB5MjDodpMh[nlic4Xs[o9zcG:mYX3pcoUhSiCvZYToc4QtKEeLNUC9O{4yKG6PLh?= MXexPFQ5PDd5NR?=
P19 cells MVzGeY5kfGmxbjDhd5NigQ>? NXv5TVZtUW6qaXLpeIlwdiCxZjDDfYNtcW5vZHXw[Y5l\W62IHvpcoF{\SBzIHnuJHAyQSClZXzsd{whUUN3ME24JI5ONg>? Mlv5NVU4PzF2MUm=
human DLD1 cells MWLQdo9tcW[ncnH0bY9vKGG|c3H5 MYS0PE04OiCq M2TyS2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iRFzENUBk\WyuczDh[pRmeiB2ODD0c{A4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVkhdk1w M2LlflIzOTh{OUK5
insect cells M4jmc2Z2dmO2aX;uJIF{e2G7 M2[wfmlvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiUHntNUBmgHC{ZYPz[YQhcW5iaX7z[YN1KGOnbHzzJIJ6KEiWUl[sJGlEPTB;MUCgcm0v NGjzOXYyQTF5OUC3Oi=>
V79 MZ cells MkW5SpVv[3Srb36gZZN{[Xl? MVjJcohq[mm2aX;uJI9nKGi3bXHuJIFt\G:|dHXyc45mKHO7boToZZNmKGW6cILld5Nm\CCrbjDWO|khVVpiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBidGSxc4Tldo9v\SC|eX70bIV{cXNuIFnDOVA:OTFibl2u MWCyOFQzOjVzOR?=
P19 cells Mmn2SpVv[3Srb36gZZN{[Xl? NF3jRmRKdmirYnn0bY9vKG:oIG\hd4N2dGG{IHXu[I91cGWuaXHsJIdzd3e2aDDmZYN1d3JicnXj[ZB1d3JiaX6gVFE6KGOnbHzzMEBKSzVyPUG0JI5ONg>? MnW0NVU4PzF2MUm=
Sf9 cells NXjyPYpqTnWwY4Tpc44h[XO|YYm= MmnyNlAhdWmwcx?= MVzJcohq[mm2aX;uJI9nKGi3bXHuJGZ6diCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJIFnfGW{IEKwJI1qdnNiYomgSWxKW0FiaX6gdJJme2WwY3Wgc4YhOSC3bX;sM2whSVSSLDDJR|UxRTF3IH7NMi=> NYexUpZ3OTd|MUW4OVM>
human PBMC NUjrbVlFTnWwY4Tpc44h[XO|YYm= MYqyOEBp MX\TeZBxemW|c3nvckBw\iCLTEKgdJJw\HWldHnvckBqdiCqdX3hckBRSk2FIHHmeIVzKDJ2IHjyd{BjgSCHTFnTRUwhUUN3ME2xOkBvVS5? MWexPFU5PTB2Nh?=
human A549 cells NUTvZnRsS3m2b4TvfIlkyqCjc4PhfS=> NG\MVIk1QCCq MUfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmgMEBKSzVyPUKwJI5ONg>? NYn0e3M3OjV6MkW5N|Q>
human CEM cells NX7jO21iS3m2b4TvfIlkyqCjc4PhfS=> MYC3NkBp M2n1N2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGNGVSClZXzsd{Bi\nSncjC3NkBpenNiYomgR4Ft[2WrbjDBUUBie3OjeTygTWM2OD1{MzDuUU4> NFKxOm8zOjl{MUC4NS=>
human HeLa cells M{jSTGN6fG:2b4jpZ:Kh[XO|YYm= NFHyNo41QCCq M3nicmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhmVGFiY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2yOUBvVS5? NGPDcFYzPTh{NUmzOC=>
human PC3 cells MWDDfZRwfG:6aXRCpIF{e2G7 MYS0PEBp MVzDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTCsJGlEPTB;M{Ggcm0v NV3OW|l4OjV6MkW5N|Q>
human SF268 cells Mnz0R5l1d3SxeHnjxsBie3OjeR?= MYO0PEBp M3X2NGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNHOjZ6IHPlcIx{KGGodHXyJFQ5KGi{czDifUBUWkJiYYPzZZktKEeLNUC9OFQhdk1w MV:yNVUyOzJ7NB?=
human MCF7 cells M1fhS2N6fG:2b4jpZ:Kh[XO|YYm= MUe0PEBp M2PBWGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME21NEBvVS5? MknyNlE{QDhzOUG=
HEK293 cells M3Tkc2N6fG:2b4jpZ:Kh[XO|YYm= NXnKV2doPzJiaB?= NYTtUYFCS3m2b4TvfIlkcXS7IHHnZYlve3RiSFXLNlk{KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDD[YxtXGm2ZYLHcI8h[XO|YYmsJGlEPTB;NU[gcm0v MlPMNlQ4PjN{NkK=
HUE cells MUHGeY5kfGmxbjDhd5NigQ>? NETReI06OCCvaX7z NFG4W3hKdmirYnn0bY9vKG:oIG\FS2ZTOiCrbjDIWWUh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDWSWdHNWmwZIXj[YQh[XW2b4Doc5NxcG:{eXzheIlwdiC2cnXheIVlKG[xcjC5NEBucW6|IHLl[o9z\SCYRVfGJINp[WyuZX7n[UBjgSCHTFnTRUwhUUN3ME23NEBvVS5? NYPoVXVwOjBzN{CxOlM>
human A431 cells MYLDfZRwfG:6aXRCpIF{e2G7 MnPVNlQhKGh? NFTQZndEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPDNzIHPlcIx{KGGodHXyJFI1KGi{czD1d4lv\yCDbn7lfIlvKF[nRlnUR{9xem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nJIJ6KE2WVDDhd5NigSxiSVO1NF04OCCwTT6= NWjUeZFWOjJ3NEGwOVE>
human Jurkat cells NF;IZ4lRem:uaX\ldoF1cW:wIHHzd4F6 NFHVZopCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JGpCUzNiZYjwdoV{e2mwZzDJUFIue3SrbYXsZZRm\CCqdX3hckBLfXKtYYSgZ4VtdHNuIFnDOVA:PzFibl2u MmK2NVk1Ojd{MEO=
HEK293 cells NF;YOZZHfW6ldHnvckBie3OjeR?= MVLJcohq[mm2aX;uJI9nKEmOLUigdoVt\WG|ZTDifUBJTUt{OUOgZ4VtdHNiZYjwdoV{e2mwZzDQT2Mu[mW2YUKsJGlEPTB;N{egcm0v MlSxNVU4PzF2MUm=
human KE-97 cells NHXY[ZpEgXSxdH;4bYPDqGG|c3H5 M{jablczKGh? NFXWZWpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMTS17NzDj[YxteyCjZoTldkA4OiCqcoOgZpkhS2WubGTpeJJmNUeubzDseY1qdmW|Y3XueEBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjF|IN88UU4> MVWyOFMzQDJ6Mx?=
human CHOK1 cells NYPwd4J1S3m2b4TvfIlkyqCjc4PhfS=> NEDqelc1QCCq NWPlc4RVS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hS0iRS{GgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KFOUQjDhd5Nige,:jDDJR|UxRTBwMUOg{txONg>? NYqxWnJEOjF3MUOyPVQ>
mouse NIH/3T3 cells Ml;mR5l1d3SxeHnjxsBie3OjeR?= MorwPVYhcA>? M1PhUGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJG5KUC9|VEOgZ4VtdHNiYX\0[ZIhQTZiaILzJIJ6KFOUQjDhd5NigSxiSVO1NF0xNjJizszNMi=> Mn60NlQ{PjF3MkG=
human A2780 cells NV7Gc3VlS3m2b4TvfIlkyqCjc4PhfS=> MV:5OkBp NInXPJZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCOjd6MDDj[YxteyCjZoTldkA6PiCqcoOgZpkhW1KEIHHzd4F6NCCLQ{WwQVAvOiEQvF2u M3;zWVI1OzZzNUKx
human 8505C cells NUm3OldiS3m2b4TvfIlkyqCjc4PhfS=> MYC5OkBp MWLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjC4OVA2SyClZXzsd{Bi\nSncjC5OkBpenNiYomgV3JDKGG|c3H5MEBKSzVyPUCuNkDPxE1w NIqxcZAzPDN4MUWyNS=>
human 518A2 cells NVf3UJVxS3m2b4TvfIlkyqCjc4PhfS=> MmrUPVYhcA>? M2jxSGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJFUyQEF{IHPlcIx{KGGodHXyJFk3KGi{czDifUBUWkJiYYPzZZnwxIxiSVO1NF0xNjJizszNMi=> MYiyOFM3OTV{MR?=
human HuH7 cells MmLIR5l1d3SxeHnjxsBie3OjeR?= M2XGU|czKGh? MlrFR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTJVJPyClZXzsd{Bi\nSncjC3NkBpenNiYomgR4VtdFSrdILlMWdtdyCudX3pcoV{[2WwdDDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlI{KM7:TT6= M2njSVI1OzJ6Mkiz
FL5.12-Akt1 cells MWHQdo9tcW[ncnH0bY9vKGG|c3H5 MX;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IF\MOU4yOi2Da4SxJINmdGy|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlI6KM7:TT6= NVLXUYdOOTZ2MEO2NlY>
human MiaPaCa-2 cells MoLOVJJwdGmoZYLheIlwdiCjc4PhfS=> MVfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2rYWDhR4EuOiClZXzsd{whUUN3ME2wMlM4KM7:TT6= NILSTm4yPjRzM{e4NC=>
human BGC823 cells NVLafZY{S3m2b4TvfIlkyqCjc4PhfS=> MXO3NkBp M{XQXGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGJISzh{MzDj[YxteyCjZoTldkA4OiCqcoOgZpkhS2WubGTpeJJmNUeubzDseY1qdmW|Y3XueEBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjN6IN88UU4> NFPLfWIzPDN{OEK4Ny=>
human MCF7 cells M3H5R2N6fG:2b4jpZ:Kh[XO|YYm= NWLTSYRRQTZiaB?= M{HtemN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[W[2ZYKgPVYhcHK|IHL5JHNTSiCjc4PhfUwhUUN3ME2wMlQh|ryPLh?= M4C5[|I1OzZzNUKx
human A549 cells M{fxSmN6fG:2b4jpZ:Kh[XO|YYm= MlL1PVYhcA>? MYHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIFnfGW{IEm2JIhzeyCkeTDTVmIh[XO|YYmsJGlEPTB;MD62JO69VS5? NUHGN3Y4OjR|NkG1NlE>
HEK293 cells NHXSU4FEgXSxdH;4bYPDqGG|c3H5 MYnDfZRwfG:6aXPpeJkh[WejaX7zeEBJTUt{OUOgZ4VtdHNuIFXDOVA:OiEQvF2u M4L5TFI2OzF4M{G3
human Raji cells  Ml7KR5l1d3SxeHnjxsBie3OjeR?= NYLte3prS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWmGsaTDj[YxteyxiRVO1NF0zKM7:TT6= NWrIPGY{OjV|MU[zNVc>
human HepG2 cells MoTjR5l1d3SxeHnjxsBie3OjeR?= NHTNZ2lEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJ\XCJMjDj[YxteyxiRVO1NF0zKM7:TT6= NYLCR3BPOjV|MU[zNVc>
human BJ cells M4TWc2N6fG:2b4jpZ:Kh[XO|YYm= Moq0R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRmoh[2WubIOsJGVEPTB;MjFOwG0v NEe5PXUzPTNzNkOxOy=>
human U937 cells MlTtR5l1d3SxeHnjxsBie3OjeR?= MkLZR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gWVk{PyClZXzsd{whUUN3ME2yJO69VS5? M3XESVE4ODh6ME[3

... Click to View More Cell Line Experimental Data

In vivo試験 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]
臨床試験
特集

プロトコル (参考用のみ)

キナーゼアッセイ:

[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.

細胞アッセイ:

[3]

細胞株 PC12
濃度 Dissolved in DMSO, final concentration 1 μM
反応時間 ~32 hours
実験の流れ

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.

動物実験:

[8]

動物モデル Male Mongolian gerbils or male Wistar rats subjected to transient ischemia
製剤 Dissolved in DMSO, and diluted in saline
投薬量 ~10 ng
投与方法 Stereotaxically administered into the bilateral CAl subfield of the hippocampus

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Staurosporine SDF
分子量 466.53
化学式

C28H26N4O3

CAS No. 62996-74-1
保管 3年-20℃
2年-80℃in solvent
別名 CGP 41251
溶解度 (25°C) * In vitro DMSO 4 mg/mL (8.57 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo
* <1 mg/ml means slightly soluble or 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.
化学名 9,13-Epoxy-1H,9H-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazonin-1-one, 2,3,10,11,12,13-hexahydro-10-methoxy-9-methyl-11-(methylamino)-, [9S-(9α,10β,11β,13α)]-

文献中の引用 (8)

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