PD98059

For research use only. Not for use in humans.

目录号:S1177

PD98059 Chemical Structure

CAS No. 167869-21-8

PD98059 是一种非ATP竞争性的MEK抑制剂,无细胞试验中IC50为2 μM,特异性抑制MEK-1介导的MAPK激活;不直接抑制ERK1或ERK2。PD98059 是一种aryl hydrocarbon receptor (AHR)的配体并起到拮抗剂的功能。

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RMB 1213.08 现货
RMB 3845.73 现货
RMB 5489.52 现货
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客户使用Selleck生产的PD98059发表文献299篇:

产品安全说明书

MEK抑制剂选择性比较

生物活性

产品描述 PD98059 是一种非ATP竞争性的MEK抑制剂,无细胞试验中IC50为2 μM,特异性抑制MEK-1介导的MAPK激活;不直接抑制ERK1或ERK2。PD98059 是一种aryl hydrocarbon receptor (AHR)的配体并起到拮抗剂的功能。
特性 PD98059不会抑制已经被c-Raf磷酸化的 MEK1
靶点
MEK1 [1]
(Cell-free assay)
2 μM
体外研究

PD98059 要么抑制本底的MEK1,要么抑制一种被部分激活的MEK突变体,该突变体是 218 和 222号位上丝氨酸突变为谷氨酸后形成的(MEK-2E), IC50 为2 μM. PD98059 不会抑制JNK和P38这两个 MAPK 的同系物. PD98059会高度选择性的抑制MEK, 因为对其它包括Raf 激酶, cAMP-依赖性激酶, 蛋白激酶C, v-Src, 表皮生长因子 (EGF) 受体激酶, 胰岛素受体激酶, PDGF 受体激酶, 和磷脂酰肌醇(-3)激酶等在内的一系列激酶都没有抑制性。 PD98059 会抑制经过PDGF刺激而活化的MAPK 和胸苷 进入 3T3 细胞, IC50分别为 ~10 μM 和 ~7 μM [1]。PD98059可以有效地阻止 MEK1 被Raf 或者MEK 激酶活化, IC50为4 μM, 可以微弱地 抑制MEK2被 Raf 活化, IC50 为50 μM。 在KB 和 PC12 细胞中, PD98059 不会抑制MKK4 和RK激酶这两个参与压力和白细胞介素-1介导的激酶级联反应的MEK的同系物的活化,在Swiss 3T3 细胞中也不会通过胰岛素或者表皮生长因子抑制p70 S6 激酶的活化[2]。PD98059会在不改变细胞生存能力的情况下完全阻断 神经生长因子(NGF)诱导的 PC12 细胞的分化[3] 。PD98059会以剂量依赖性的方式抑制培养在含有破骨细胞分化因子培养基中的 RAW264.7细胞的增值,进而导致TRAP阳性细胞数量明显下降[6]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
H1355 NETQ[W9HfW6ldHnvckBCe3OjeR?= NVG1clVFOjVizszN NEL2bJUyKGh? M1;1UIJtfW62czD0bIUhSlujXWCtbY5lfWOnZDDpcoNz\WG|ZTDpckBxcG:|cHjvMWNpczFiYX7kJJBpd3OyaH:tSXJMKGW6cILld5Nqd25? Ml;LNlU4PjlzOEG=
MCF-7  M2jJd2Z2dmO2aX;uJGF{e2G7 NHHoXnEyOCEQvF2= NITKW5cyKGh? MlXBbY5pcWKrdIOgTWwuOThvZX7oZY5k\WRiY3XscEBucWe{YYTpc44> NWXYbVA6OjV5MkewNVE>
HepG2  NGrqTVJHfW6ldHnvckBCe3OjeR?= MV[xNEDPxE1? NIG3VIs2KGh? NX;tfZpP[myxY3vzJJBpd3OyaH;yfYxifGWmIF3BVGt{KGmwZIXj[YQh[nliZYjv[4Vvd3W|IGTHSk3PujF? NWW0[m9kOjV3NkC0PFg>
HepG2  MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPpNlAh|ryP NWfl[FhROjRiaB?= MljMd5VxeHKnc4Pld{BVT0ZvzsKxMYlv\HWlZXSgZ4VtdCCycn;sbYZmemG2aX;uJIFv\CCrbo\hd4lwdg>? NWL6NXpsOjV3NkC0PFg>
MDA-MB-231 M4L3PGZ2dmO2aX;uJGF{e2G7 MVOyOUDPxE1? NWT0[VFGOi1|IHi= MWrk[YNz\WG|ZYOgdE1GWktzL{KgZY5lKFNzMEDBOEBmgHC{ZYPzbY9v MlHkNlU2PTV6N{W=
SW480 MV7GeY5kfGmxbjDBd5NigQ>? NVKwUnczOjEEoN88US=> NHPwUY0yyqCq NVjkW|l2emWmdXPld{B1cGViZYjwdoV{e2mxbjDv[kBCXEZ|IIDyc5RmcW5? NW\rV4VqOjV2NEe4NVY>
HCT-15 MYfGeY5kfGmxbjDBd5NigQ>? NWDhNlRUOSCq NX62boxy[XS2ZX71ZZRmeyCSR1WyMYlv\HWlZXSgdIhwe3Cqb4L5cIF1cW:wIH;mJGVzc8Li NGCxeYMzPTR|MUSyOS=>
HCT-15 NGXTW3hCeG:ydH;zbZMhSXO|YYm= MonINUBp M3:4dYFjd2yrc3jld{B1cGVicILveIVkfGm4ZTDl[oZm[3S|IH;mJHBITTMEoHHnZYlve3RiY4XyZ5VucW5vaX7keYNm\CCjcH;weI9{cXN? NEPQcmIzPTR|MUSyOS=>
786-O NHGwV|dCeG:ydH;zbZMhSXO|YYm= NIHMZWU2OMLizszN NXf0[HJxOjRiaB?= NWr4Ro1[eG:2ZX70bYF1\XQEoITo[UBxem9vYYDvdJRwfGmlIHXm[oVkfHNib3[gUmM> M{PXWlI1PTB6NEe2
A498 M3\BbmFxd3C2b4Ppd{BCe3OjeR?= NVrjOJV7PTEEoN88US=> MnX1NlQhcA>? MX7wc5RmdnSrYYTld:KhfGinIIDyc{1ieG:ydH;0bYMh\W[oZXP0d{Bw\iCQQx?= MWOyOFUxQDR5Nh?=
NHBE NUjkS3dGTnWwY4Tpc44hSXO|YYm= MnLiNk8zOCEQvF2= M3HySVIhcA>? Mk\RZZR1\W63YYTld{BKVC1|MzDzeIlufWyjdHXkJGNZS0x6L1nMMVghe2WlcnX0bY9v M1LVOlI1PDd7NUK2
A375 MlrZR4VtdCCLbo\hd4lwdiCDc4PhfS=> MWGxNQKBmzJyINM1US=> NGH0WVMzPCCq NEnke5Zz\WS3Y3XzJI1mdGGwb33hJINmdGxiaX72ZZNqd25? M2D4SlI1PDZ4MEO2
HBMEC NX7LNItyTnWwY4Tpc44hSXO|YYm= M3zSN|ExKM7:TR?= M{Pa[FEhcA>? NWDJe2Zz[myxY3vzJHZGT0ZvaX7keYNm\CCHcHjBNkBmgHC{ZYPzbY9v M2LrOFI1PDV6OUiy
HPAEpiCs  NHW5bZRHfW6ldHnvckBCe3OjeR?= MUCzNEDPxE1? MYOxJIg> MoPzbY5pcWKrdIOgWG5HNc7zIIP0bY12dGG2ZXSgdFQzN3B2NDDNRXBMKHCqb4PwbI9zgWyjdHnvci=> MlnnNlQ1PDF6N{C=
BeWo NYTqVItGTnWwY4Tpc44hSXO|YYm= NUX0RYduOTEEoN88US=> NE\JNIkzKGh? NYPWXGtLcW6qaXLpeJMhTVKNMT:y M3e4NlI1PDN|OES2
PC3  NFnpeY9CeG:ydH;zbZMhSXO|YYm= MVS1NEDPxE1? NHTIWHAxNjViaB?= NGj6UWhqdmirYnn0d{BOUFlvNES5MYlv\HWlZXSgZZBweHSxc3nzxsA> MUKyOFQzPDh6OR?=
HGC-27 MU\BdI9xfG:|aYOgRZN{[Xl? MlW0NUDDvU1? M3THcVEhcA>? NVvHNplSe3WycILld5NmeyCUQVSwNFEheGy3czDNT{0zOjB4LXnu[JVk\WRiY3XscEB3cWGkaXzpeJkhdG:|cx?= MmrNNlQ1OTZ|NEm=
MCF-7 NWTKenVWTnWwY4Tpc44hSXO|YYm= NVXpfFd{OTEEoN88US=> M33yOFExNzNyIH3pci=> MliwdoVlfWOnczD0bIUhXVSSLXTldIVv\GWwdDDFVmsheGixc4Doc5J6dGG2aX;u MYeyOFM6ODhzOR?=
HUVECs M{DNW2Z2dmO2aX;uJGF{e2G7 MVqxNOKh|ryP MVSxJIg> NFG4UGVqdmirYnn0d{B1cGViSFTMJJJm\HWlZXSgR29ZNTJiZYjwdoV{e2mxbjDhcoQhWEeLLUKgdoVt\WG|ZR?= MV[yOFM5PTFyOR?=
HeLa MlTySpVv[3Srb36gRZN{[Xl? NEDiVHg2OCEQvF2= MmPMNE42KGh? NETydm9jdG:la4OgWHJZNTFiboXjcIVieiCvaXfyZZRqd25iYX7kJHRZVkmSIHTve44uemWpdXzheIlwdg>? M2\zfFI1Ozd4OEK3
HL-60  NX;2dZlRTnWwY4Tpc44hSXO|YYm= M3u5dlExNzJyIN88US=> NWDnV3d5OSCq MnXibY5pcWKrdIOgeIhmyqCQLjDjbIlv\W6|aYPlfJRz[WO2wrDpcoR2[2WmIHTp[oZmemWwdHnheIlwdiCrboTvJIdz[W63bH;jfZRmew>? M3rMflI1OzV5MEKw
HL-60 M3LkWmZ2dmO2aX;uJGF{e2G7 M361O|IhyrWP NWS0V243OTZiaB?= MXnEUXNQ NH:zSoNqdmirYnn0d{B1cGViYYPzc4Nq[XSrb36gc4YheFN4MkGgVoFnNTFiYX7kJG5HSVSlMzygZY5lKHSqZTDSRU1qdmS3Y3XkJJBpd3OyaH;yfYxifGmxbjDv[kBvfWOuZXHyJG5HSVSlMx?= Mnz1NlQ{OzByNki=
HEK 293 NGL0c3VHfW6ldHnvckBCe3OjeR?= M{TySFExKM7:TR?= Mmq3OUBp Mn;jSG1UVw>? M1PWdolvcGmkaYTzJHdvfC2rbnT1Z4VlKM7{LXPheIVvcW5xVFPGOEBi[3Srdnn0fUBidmRiboXjcIVieiEQsj3jZZRmdmmwIHHjZ5VufWyjdHnvci=> MlrFNlQ{OjR|Nk[=
HEK 293 NUfEd|dkTnWwY4Tpc44hSXO|YYm= M13hOFExKM7:TR?= NGXGZ3Y2KGh? MY\EUXNQ NHvhcld{fXCycnXzd4V{KHSqZTDDVnQh[WO2aY\peJk> Ml;RNlQ{OjR|Nk[=
SW480 M1zn[2Z2dmO2aX;uJGF{e2G7 NXfiTVZ5OTBizszN M1HzVFIxKGh? NGPpOYhFVVOR MmfQd5VxeHKnc4Pld{B1cGViQ2LUJIFkfGm4aYT5 MYiyOFMzPDN4Nh?=
HCSMCs MlzhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWL2OXhqOTBizszN NGm3N|kzPCCq MnPSZoxw[2u|IF\BRnA1NWmwZIXj[YQhUEODU13DJJBzd2yrZnXyZZRqd25? MUOyOFMyOjN6MR?=
PANC-1 NIjxfJpHfW6ldHnvckBCe3OjeR?= NXHDNoZnOjBizszN MYq0PEBp Ml72bY5pcWKrdIOgeIhmKGW6cILld5Nqd25ib3[g{rQ3TCCrbjDy[ZNxd26|ZTD0c{B1cGViUGDBVu61yqCjZ3;ubZN1yqB? M1jVSVI1Ojl2MUOz
A549 MYXGeY5kfGmxbjDBd5NigQ>? M4ezfFMxKM7:TR?= MnH0NE42KGh? NXfJUYJ2TE2VTx?= MUTpcohq[mm2czD0bIUhfGi{b33ibY4ucW6mdXPl[EBKVC16L1PYR2w5NUy3YzDhZ5Rqfmm2eR?= NHfIZWczPDJ5N{[5Oi=>
A549 M4fObWZ2dmO2aX;uJGF{e2G7 MYizNEDPxE1? Mn3wNE42KGh? M{nNSGROW09? NWT5S|dCcW6qaXLpeJMhfGi{b33ibY4ucW6mdXPl[EBEN0WEUN8yJHRpejJ|NdMgdIhwe3Cqb4L5cIF1cW:w MUiyOFI4PzZ7Nh?=
MC-3 MYHBdI9xfG:|aYOgRZN{[Xl? NWq5eJM5OTBizszN NVHq[WxVOjRiaB?= MoK2dI91\W62aXH0[YQhVUWVQz3pcoR2[2WmIHHwc5B1d3OrczDpckAh[2WubIO= MmnHNlQzPzB3MkO=
Raji  NE\lTZNHfW6ldHnvckBCe3OjeR?= MnfSNVAh|ryP MX2xJIg> NGnwe2djdG:la4OgbJNDSU[IIHnu[JVk\WRiRYLrNU8zKHCqb4PwbI9zgWyjdHnvci=> MVSyOFI3QTZ|MB?=
Raji  NWLvNll1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVmxNEDPxE1? MYCxJIg> M3;aZolvcGmkaYTzJJRp\SCkYYPhcEBweiCqc1LBSmYue3SrbYXsZZRm\CClZXzsJJBzd2yrZnXyZZRqd25iYX7kJJZq[WKrbHn0fS=> NFvEWWszPDJ4OU[zNC=>
HT29 MW\GeY5kfGmxbjDBd5NigQ>? MofTNVAh|ryP M2KyVlIhcA>? M4HEcolvcGmkaYTzJI9nKEqDS{KsJGVTUzFxMjDhcoQhW1SDVEOgdIhwe3Cqb4L5cIF1cW:w MlHJNlQzPjV{OUO=
HepG2 NGTqV2xCeG:ydH;zbZMhSXO|YYm= NUTVNHR4OjBizszN MXOyOEBp NEfoXpdqdmirYnn0d{BGWktzL{KgdIhwe3Cqb4L5cIF1cW:wIHHu[EBmdmijbnPld{BXSjFvaX7keYNm\CCjcH;weI9{cXN? NG\4fI4zPDJ2N{mwPS=>
HepG2 MWDGeY5kfGmxbjDBd5NigQ>? MnLUNlAh|ryP NIjC[HQzKGh? NY\2NIly\W6qYX7j[ZMhXkJzLXnu[JVk\WRiRl;YU|NiKHS{YX7zZ5JqeHSrb37hcEBi[3Srdnn0fS=> M{[0dVI1OjR5OUC5
TE4 MUPGeY5kfGmxbjDBd5NigQ>? NXzOc2RpOjBxNUCvNVAxKM7:TR?= NHvuNG01QCCq M3jhVmROW09? M2TMbolvcGmkaYTzJJAuTXKtIHHu[EB4d3K2bXHucolvKGSxd37y[Yd2dGG2ZXSgdE1Cc3RiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MUGyOFI1PDB{Mx?=
TE1 M3f3ZWZ2dmO2aX;uJGF{e2G7 NGr3N2gzOC93MD:xNFAh|ryP MV60PEBp MY\EUXNQ MUXpcohq[mm2czDwMWVzcyCjbnSge49zfG2jbn7pckBld3ewcnXneYxifGWmIICtRYt1KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NUXSUJNjOjR{NESwNlM>
KYSE30 NHTl[VZHfW6ldHnvckBCe3OjeR?= MVWyNE82OC9zMECg{txO NYHPUow5PDhiaB?= NHnE[odFVVOR MYXpcohq[mm2czDwMWVzcyCjbnSge49zfG2jbn7pckBld3ewcnXneYxifGWmIICtRYt1KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MVqyOFI1PDB{Mx?=
TE1 MWXGeY5kfGmxbjDBd5NigQ>? NHnyUpg2OCEQvF2= MWW0PEBp NH[4V5ZFVVOR MU\1dJJm\3WuYYTld{B1cGViZYjwdoV{e2mxbjDv[kBJVEFiY3zhd5MhUQ>? M2HvRVI1OjR2MEKz
TE3 MV7GeY5kfGmxbjDBd5NigQ>? M4L4RlUxKM7:TR?= M37yNFQ5KGh? NVXGSIt7TE2VTx?= MlLUeZBz\We3bHH0[ZMhfGinIHX4dJJme3Orb36gc4YhUEyDIHPsZZN{KEl? M1vNOlI1OjR2MEKz
TE4 MYLGeY5kfGmxbjDBd5NigQ>? MUK1NEDPxE1? M4\FO|Q5KGh? NI\rfGdFVVOR M2DFbZVxemWpdXzheIV{KHSqZTDlfJBz\XO|aX;uJI9nKEiOQTDjcIF{eyCL MXWyOFI1PDB{Mx?=
TE5 M4XhRmZ2dmO2aX;uJGF{e2G7 MoHUOVAh|ryP MX20PEBp MXHEUXNQ NEm1b4x2eHKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCKTFGgZ4xie3NiSR?= M3qxV|I1OjR2MEKz
KYSE30 M4e2OGZ2dmO2aX;uJGF{e2G7 M4D5dlUxKM7:TR?= MXq0PEBp NFjQfYhFVVOR MXT1dJJm\3WuYYTld{B1cGViZYjwdoV{e2mxbjDv[kBJVEFiY3zhd5MhUQ>? NV;vSHA6OjR{NESwNlM>
MKN7 NFzMU41HfW6ldHnvckBCe3OjeR?= NGPTNIM2OCEQvF2= M3nuOlQ5KGh? NX7yVnJjTE2VTx?= M17ZVolv[3KnYYPld{BmgHC{ZYPzbY9vKG:oIFjMRU1CODJib4KgTGxCNUF{NDDtc4xm[3WuZYO= NWDQR3d7OjR{NESwNlM>
OE19 NYiwOGVLTnWwY4Tpc44hSXO|YYm= NE\qSpY2OCEQvF2= M3XsdlQ5KGh? MU\EUXNQ MWXpcoNz\WG|ZYOg[ZhxemW|c3nvckBw\iCKTFGtRVAzKG:{IFjMRU1COjRibX;s[YN2dGW| NITZTWEzPDJ2NECyNy=>
KATOIII  MlPMSpVv[3Srb36gRZN{[Xl? MWO1NEDPxE1? NUn6eldKPDhiaB?= MYrEUXNQ NF;Bc3JqdmO{ZXHz[ZMh\XiycnXzd4lwdiCxZjDIUGEuSTB{IH;yJGhNSS2DMkSgcY9t\WO3bHXz NEP4SFkzPDJ2NECyNy=>
NCI-N87  NXG0cZYzTnWwY4Tpc44hSXO|YYm= MX21NEDPxE1? MVO0PEBp MmfISG1UVw>? MUnpcoNz\WG|ZYOg[ZhxemW|c3nvckBw\iCKTFGtRVAzKG:{IFjMRU1COjRibX;s[YN2dGW| MXmyOFI1PDB{Mx?=
NUGC3 M4XvfmZ2dmO2aX;uJGF{e2G7 MUK1NEDPxE1? M4rkNFQ5KGh? NVyxPXhwTE2VTx?= NVnMeoRmcW6lcnXhd4V{KGW6cILld5Nqd25ib3[gTGxCNUFyMjDvdkBJVEFvQUK0JI1wdGWldXzldy=> MXeyOFI1PDB{Mx?=
NUGC2 M{DSSmZ2dmO2aX;uJGF{e2G7 MlXGOVAh|ryP NWXUR5dnPDhiaB?= MluxSG1UVw>? M3zTb4lv[3KnYYPld{BmgHC{ZYPzbY9vKG:oIFjMRU1CODJib4KgTGxCNUF{NDDtc4xm[3WuZYO= M3jke|I1OjR2MEKz
SGC-7901  M1rTTGFxd3C2b4Ppd{BCe3OjeR?= NYrlR2U3OjBizszN MUSyOEBp M2exUolvcGmkaYTzJGNRNW2nZHnheIVlKGGyb4D0c5Nqew>? M2rTcVI1OjRzM{Wx
MG-63 M37M[GZ2dmO2aX;uJGF{e2G7 M4nGd|IxKM7:TR?= M3zHZlAvPSCq MkOyZoxw[2u|IITo[UBEUC2rbnT1Z4VlKHCqb4PwbI9zgWyjdHXkJGVNUzFicILveIVqdiCneIDy[ZN{cW:w Mny0NlQzOzl4NEC=
ARPE-19 MXvGeY5kfGmxbjDBd5NigQ>? NU\0W2c1OjBizszN NFi5bm0xNjViaB?= M1eyOolvcGmkaYTzJGFx\Wyrbj3pcoR2[2WmIIDoc5NxcG:{eXzheIlwdiCxZjDFdosh[W6mIFHreC=> M1TzfFI1OjJ5OUG4
CRL-2302 NIPo[lVHfW6ldHnvckBCe3OjeR?= MUGyNEDPxE1? MlnpNE42KGh? MkK4bY5pcWKrdIOgRZBmdGmwLXnu[JVk\WRicHjvd5Bpd3K7bHH0bY9vKG:oIFXyb{BidmRiQXv0 MmLUNlQzOjd7MUi=
MCF-7 M2O4N2Z2dmO2aX;uJGF{e2G7 MVuyNEDPxE1? MlnoNUBp NELz[WJi[m:uaYPo[ZMh\XiycnXzd4lwdiCxZjDwbI9{eGixconsZZRm\CCHUlugZ48ufHKnYYTt[Y51KHerdHigZ49vcnWpYYTl Mn[wNlQzOTZ{OEm=
MCF-7 M3HEWmFxd3C2b4Ppd{BCe3OjeR?= M1TEXVIxKM7:TR?= M2HnblEhcA>? MXfpcoNz\WG|ZYOgZ4F{eGG|ZT25JIVvgnmvZTDhZ5Rqfmm2eR?= NWPRSlZVOjR{MU[yPFk>
DLD-1  M4mxRmZ2dmO2aX;uJGF{e2G7 NFTqb|MzOMLizszN NEL6TG01QCCq MYry[YR2[2W|IITo[UBDVkmSMzDlfJBz\XO|aX;uJJBz\S22cnXheIVlKHerdHigOU1igmFvZFO= Mo\2NlQzOTF3OEG=
HT-29 NHu0TFlHfW6ldHnvckBCe3OjeR?= MkCzNlDDqM7:TR?= M4S5TVQ5KGh? M3PqWZJm\HWlZYOgeIhmKEKQSWCzJIV5eHKnc4Ppc44heHKnLYTy[YF1\WRid3n0bEA2NWG8YT3kRy=> NVLC[5JwOjR{MUG1PFE>
7402 MkPLRZBweHSxc3nzJGF{e2G7 M{HlUFMxKM7:TR?= MYC1JIQ> MV7k[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;u M3LLRlI1OjFzMkWz
7721 M{nzOWFxd3C2b4Ppd{BCe3OjeR?= NHPrR2o{OCEQvF2= M1;TZlUh\A>? NVTQdpNo\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdg>? NUmyTlBrOjR{MUGyOVM>
SGC7901  NFnieHpCeG:ydH;zbZMhSXO|YYm= NHvBZ4I2OMLizszN NVLvOIJEOjRxNEivO|IhcA>? NHXpdpFFVVOR NXzmcmVpcW6mdXPld{BieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDKRWszKHOqUl7B NFKxbFUzPDF5OEK0NC=>
SMMC7721 MYfGeY5kfGmxbjDBd5NigQ>? NU\QUpJlOjVxNUCg{txO NHjkR5UzPCCq M3\KPJN2eHC{ZYPz[ZMhfGinIHX4dJJme3Orb36gc4YheC2Da4Sgc5IheC2HUluxM|LDqA>? M1HVeVI1OTZ6MEW2
MCF-7 MljLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEW5dWQyOCEQvF2= Ml;DOFhp NEWyTYtFVVOR MXXy[ZZmenOnczDCUmYucW6mdXPl[EBk\WyuIHP5Z4xmKGG{cnXzeC=> NX:wOIlVOjRzNkO0NFQ>
Caco-2 NYXXeHhrTnWwY4Tpc44hSXO|YYm= M{LifVUxyqEQvF2= MWO0PIg> NWjYfI42TE2VTx?= NGnNXVlmdmijbnPld{B1cGVibWLORUBt\X[nbIOgc4bDqFOFTl6xRUxHYFmGMz|CpGxEXC{EoFzPXEzDqEiLRkPBMOKhYkdzNj|CpHBFTT[DwrDhcoTDqEyJQVzTNVbDqGenbnXzxsBkdy22cnXheIVlKHerdHigSIV5 NYLCeZUyOjRzNkG2PVU>
HAECs M2D3T2Z2dmO2aX;uJGF{e2G7 MmCwNVAh|ryP M1PRRVEhcA>? MWZCpIF1fGWwdXH0[ZMhXE6ILd8xMZN1cW23bHH0[YQhUUODTT2xJIFv\CCYQ1HNMVEh\XiycnXzd4lwdg>? M32zVlI1OTN2NkW3
Ca9-22 NYr3U3hNTnWwY4Tpc44hSXO|YYm= MUWzJO69VQ>? MUixJIg> MVfhZo9tcXOqZYOgeIhmKGGkaXzpeJkhd2ZiSHLSJJRwKGmwZIXj[UBKVC16IIDyc4R2[3Srb36= MXuyOFEzPjV|Mh?=
Ca9-22 M2XDTWZ2dmO2aX;uJGF{e2G7 MnfCN{DPxE1? M1\LdlEwOiCq NGLzOWtz\WS3Y3XzJGhjWi2rbnT1Z4VlKEGWRj2yJJBpd3OyaH;yfYxifGmxbh?= NVW4OnJGOjRzMk[1N|I>
AGS NYGyRo1UTnWwY4Tpc44hSXO|YYm= NHv2e2UyOCEQvF5CpC=> NHT0OlYxNjViaB?= NVHRTXhmcW6qaXLpeJMhfGinIIXwdoVofWyjdHnvckBw\iC2aHWgTWwuQCCpZX7l NXLXUVRlOjRzME[xOlY>
Caco-2  NFTq[mZCeG:ydH;zbZMhSXO|YYm= MYKxNOKh|ryP M3zF[|I1yqCq NFvKRopl\WO{ZXHz[ZMh[2WubDDhdI9xfG:|aYOgbY5lfWOnZDDifUA2NU[X MojMNlQxQTV6NkO=
HCT-8 NVnaZVN1SXCxcITvd4l{KEG|c3H5 MUexNOKh|ryP MXSyOOKhcA>? MWXk[YNz\WG|ZYOgZ4VtdCCjcH;weI9{cXNiaX7keYNm\CCkeTC1MWZW Mn71NlQxQTV6NkO=
A549 M{fmcWZ2dmO2aX;uJGF{e2G7 NGCzW3A2OMLizszN M2PvRVIhcA>? MoD2Zoxw[2u|IFXST{BxcG:|cHjvdplt[XSrb36gcYVlcWG2ZXSgZpkhOSx{LV7R NYr3UWVIOjRyNke3Nlc>
HPMC NUPPTnhWTnWwY4Tpc44hSXO|YYm= NFfKbXkyOMLizszN M4\YclQ5KGh? NH3ZcFBz\X[ncoPld{B1cGViY3jhcodmeyCrbjDj[YxtKG2xcoDoc4xw\3liaX7keYNm\CCkeTDIS3BFWw>? NH\DWFUzPDB2MkizPC=>
HPMC MWfBdI9xfG:|aYOgRZN{[Xl? M4\MSFExyqEQvF2= M3\jRlI1yqCq M1nzeJJmfmW{c3XzJIRm[3KnYYPlJIlvKGOnbHygeoli[mmuaYT5JIlv\HWlZXSgZpkhUEeSRGO= NWXXXI8{OjRyNEK4N|g>
MGC803  M2PFUmFxd3C2b4Ppd{BCe3OjeR?= MlHZNlDDqM7:TR?= NHvodHQyKGh? MY\pcohq[mm2czDhdI9xfG:|aYOgbY5lfWOnZDDifUBKTk5vzsJCpIFv\CB34pEyMWRHXVJ? MUOyOFAzPzd3MB?=
SGC7901 MnW5RZBweHSxc3nzJGF{e2G7 MnfENlDDqM7:TR?= NFzx[XkyKGh? MY\pcohq[mm2czDhdI9xfG:|aYOgbY5lfWOnZDDifUBKTk5vzsJCpIFv\CB34pEyMWRHXVJ? NYjGTGdZOjRyMke3OVA>
COLO205 NEno[HdCeG:ydH;zbZMhSXO|YYm= MXixNE8zOC92MDFOwG0> NVTINnp5OjRiaB?= M1KyNIlv\HWlZYOgSG5CKGyjZHTldkBnd3KvYYTpc44> NV7sfWh3OjRyMUmxNFg>
G292  NGnoPYVCeG:ydH;zbZMhSXO|YYm= NYjBXnlmOzEEoN88US=> M1uzfFIhcA>? NE\xO3hz\XO2b4Lld{Bk[XC|YXnjbY4ucW6mdXPl[EBk\WyuIHTlZZRp MYeyOFAyOjl|MB?=
BxPC-3 MWTGeY5kfGmxbjDBd5NigQ>? MWCxNEDPxE4EoB?= NFrLb5g3KGh? NHjaN3JqdmO{ZXHz[UBucVJvMUSzJIV5eHKnc4Ppc44> M1rCS|I{QTd|N{Gw
HPAF-II NWLnT4pRTnWwY4Tpc44hSXO|YYm= M2nvNVExKM7:TdMg NXXVbZFmPiCq NXrpW3JwcW6lcnXhd4UhdWmULUG0N{BmgHC{ZYPzbY9v M4PQXlI{QTd|N{Gw
HL-60 NGi2OoFCeG:ydH;zbZMhSXO|YYm= MojDOVDDqM7:TR?= M2XadFEhcA>? NULhfFgzemW|Y4Xld{BDSTF2NTDt[YRq[XSnZDDhdI9xfG:|aYO= MWGyN|k1QDd3MR?=
HepG2 MXHGeY5kfGmxbjDBd5NigQ>? NG\1eYI1OCEQvF2= NH7DVI43NzF{IHi= Ml\0bY5pcWKrdIOgeIhmKGmwY4LlZZNmKG:oIICtSXJMOSCjbnSgdE1kNUq3bjDwdo91\WmwIHX4dJJme3Orb36gZpkhWEx? MXeyN|k1Ojh3MR?=
HUVECs M33ueWZ2dmO2aX;uJGF{e2G7 MUOyOUDPxE1? NGnwUGIyKGh? MoLvbY5kemWjc3WgUmYu|rqEIIC2OUBvfWOuZXHyJJRz[W6|bH;jZZRqd25? NHu4NGYzOzlyMUCwPC=>
LNCaP  NIXUWJNHfW6ldHnvckBCe3OjeR?= NXP0XmRiOTBizszNxsA> MVyxJIg> MVXk[YNz\WG|ZYOgeIhmKEWJRjD1dJJm\3WuYYTl[EBxNVmELUG= MXqyN|g{QDNzOB?=
HL60  MmK4SpVv[3Srb36gRZN{[Xl? Ml;3NlDDqM7:TR?= MnjtO|IhcA>? MVjEUXNQ M1myeYlvcGmkaYTzJIRie2G2aX7pZk1qdmS3Y3XkJGNFOTGkIHX4dJJme3Orb36= M1GwNVI{QDJ3NUi1
NB4  MWTGeY5kfGmxbjDBd5NigQ>? NVLmd25HOTBizszNxsA> MYq3NkBp NXztWFRUTE2VTx?= NFrDOldqdmirYnn0d{Bl[XOjdHnubYIucW6mdXPl[EBETDFzYjDlfJBz\XO|aX;u M{\3T|I{QDJ3NUi1
EPOR/CR3 M4P1R2Z2dmO2aX;uJGF{e2G7 MV[1NOKh|ryP MVKzJIg> NECzPW9z\WS3Y3XzJGVRVyCjbnSvc5IhUUxvMz3pcoR2[2WmIITo[UB1gXKxc3nu[UBxcG:|cHjvdplt[XSrb39CpC=> NYLBNFVGOjN6MkC3N|E>
HUASMCs NVjrSJNYTnWwY4Tpc44hSXO|YYm= NXnzVWpCOTBizszNxsA> NHXrd2YzPCCq MoLt[IlucW6rc3jld{BCdmdiSVmtZ4F2e2WmIGPPR3M{KG2UTlGgZY5lKHC{b4TlbY4h\XiycnXzd4lwdsLi M2HPOFI{QDF4NE[4
HUASMCs MkjCSpVv[3Srb36gRZN{[Xl? M2\4[|ExKM7:TdMg M3:xflI1KGh? NHjzWllqdmirYnn0d{BCdmdiSVmtbY5lfWOnZDDFVmsyNzJicHjvd5Bpd3K7bHH0bY9vKGyndnXs MXKyN|gyPjR4OB?=
SGC7901 MYHGeY5kfGmxbjDBd5NigQ>? M3zYeVExKM7:TdMg MWGyOEBp NIryeopqdmirYnn0d{B1cGViZYjwdoV{e2mxbjDv[kBxcG:|cHjvdplt[XSnZDDFVmsyNzJ? NHvYZW8zOzd7MkW4PC=>
MKN45 M4jVc2Z2dmO2aX;uJGF{e2G7 MYixNEDPxE4EoB?= NFe0ZXMzPCCq MYXpcohq[mm2czD0bIUh\XiycnXzd4lwdiCxZjDwbI9{eGixconsZZRm\CCHUluxM|I> M1L2SVI{Pzl{NUi4
SGC7901 MnP2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LrOVExKM7:TdMg M1PaVlI1NzR6L{eyJIg> NWnvNnFbcW6qaXLpeJMh[2WubDDndo94fGhiY3:teJJm[XSnZDD3bZRpKESDUGS= MmXONlM4QTJ3OEi=
MKN45 MoS4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfVNplQOTBizszNxsA> MV[yOE81QC95MjDo NVLMWmdJcW6qaXLpeJMh[2WubDDndo94fGhiY3:teJJm[XSnZDD3bZRpKESDUGS= NYnvTYxYOjN5OUK1PFg>
SGC7901 NIXWc2NCeG:ydH;zbZMhSXO|YYm= MlTXNVAh|ryPwrC= M1\qZ|I1KGh? Mn3wbY5kemWjc3XzJJRp\SCGQWDUMYlv\HWlZXSgZ4VtdCCjcH;weI9{cXN? NVP1R2hzOjN5OUK1PFg>
MKN45 NYLFN3piSXCxcITvd4l{KEG|c3H5 MnS4NVAh|ryPwrC= NYTEUHN1OjRiaB?= NUG3blQycW6lcnXhd4V{KHSqZTDERXBVNWmwZIXj[YQh[2WubDDhdI9xfG:|aYO= MX:yN|c6OjV6OB?=
BxPC-3 cells NI\SSmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX:yNOKh|ryP MkfENE42KGh? MlzmbY5pcWKrdIOgWmVITi2DLYLl[5Vt[XSnZDDIWXZGSyCpcn;3eIgh[W6mIIT1ZoUh\m:{bXH0bY9vKGmwZIXj[YQh[nliUFHSMVIhSVB? M1X6blI{PzZ2MES2
NB4  NX;xSmRZSXCxcITvd4l{KEG|c3H5 MXqxNE8zOC94MDFOwG0> M4C0cFEvPSCq NF\ZPHlFVVOR MYjk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliY3:teJJm[XSnZDD3bZRpKFCjY3zpeIF5\Wx? M1nuNlI{PzN3NUSx
HepG2  MoLNSpVv[3Srb36gRZN{[Xl? MoG4NlDDqM7:TR?= M4DCe|I1KGh? Mmn2bY5pcWKrdIOgeIhmKEiRLUGgdJJwfGWrbjDlfJBz\XO|aX;uJINwNXS{ZXH0[YQhf2m2aDDt[ZRnd3KvaX6= NEDwOFAzOzdyN{[wPS=>
HUVECs MYHBdI9xfG:|aYOgRZN{[Xl? NFizSZozNzRizszN NV[0[417OjRxNEigbC=> M3jycolv\HWlZYOgZ4VtdCCmZXH0bC=> NYnnfnZFOjN5MEe1NlA>
KG-1  M1fmXWFxd3C2b4Ppd{BCe3OjeR?= Mlf1NlDDqM7:TR?= NXXzb4JwOTJiaB?= MnzQ[Y5p[W6lZYOgZ4VtdCCjcH;weI9{cXNiaX7keYNm\CCkeTDTNS=> M320NlI{PzB4Nkmx
AML 1# M2q4SGFxd3C2b4Ppd{BCe3OjeR?= M1z3W|IxyqEQvF2= NGnVSFIyOiCq M2HPT4VvcGGwY3XzJINmdGxiYYDvdJRwe2m|IHnu[JVk\WRiYomgV|E> MUeyN|cxPjZ7MR?=
A2780  NE[4RVBHfW6ldHnvckBCe3OjeR?= MUCyNOKh|ryP MVWxJIg> NFnWfWNjdG:la4OgSHRETC2rbnT1Z4VlKESUNTDlfJBz\XO|aX;u M2[3NVI{Pjl4OE[y

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
c-Jun / α-tubulin / p-ERK / ERK / p-AKT / AKT; 

PubMed: 17482134     


ERK regulates c-Jun levels in melanoma. The indicated melanoma cell lines were treated with 50μM PD98059 (PD) or 10μM LY294002 (LY) for 12h in the absence of serum. Protein samples were analyzed by Western blots using the indicated antibodies. α-Tubulin reveals equal loading.

p-JNK / JNK / Cyclin D1 ; 

PubMed: 17482134     


Inhibition of the MEK/ERK pathway affects c-Jun, P-JNK and cyclin D1 levels. The indicated melanoma cell lines were treated with 50μM PD98059 for 16h. Protein samples were analyzed by Western blots using the indicated antibodies. α-Tubulin reveals equal loading.

p-HER2 / HER2 ; 

PubMed: 24244023     


TE1cells were treated with wortmannin (Akt signal inhibitor), PD98059 (MAPK signal inhibitor), or lapatinib (EGFR and HER2 dual inhibitor) at the indicated doses or with DMSO as a negative control for 48 h. HER2-related signaling molecules were assessed by Western blot. 

MMP9 / XIAP / VEGF ; 

PubMed: 29695559     


SK-Hep1 cells were treated 10 μM PD98059 for 48 h.  Protein levels of MMP-9, XIAP, VEGF, cyclin-D1, and pERK were evaluated with western blotting assay.

17482134 24244023 29695559
体内研究 在大脑缺血前30分钟用PD98059处理小鼠可以明显减轻伤害, 使脑梗塞的体积减小[4]。基于胰腺的湿重和组织学研究发现,提前30分钟用PD98059预处理 (10 mg/kg 静脉注射) 然后每小时注射一次蛙皮素连续三次的小鼠可以明显改善蛙皮素诱导的急性胰腺炎[7]。卡拉胶损伤一小时后用PD98059 (10 mg/kg) 对小鼠进行治疗可以发现与炎症相关的所有指标均有所下降[11]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
- 合并

体外MEK激酶活性测定:

在含有44-kDa GST-MAPK 或者45-kDa GST-MEK1的体系中检测32P被掺入蛋白 MBP中的情况。 反应体系50 μL ,含有50 mM Tris, pH 7.4/10 mM MgCl2/2 mM EGTA/10 μM [γ-32P]ATP, 加入10 μg GST-MEK1, 0.5 μg GST-MAPK和 40 μg MBP。30°C 孵育15 分钟, 加入Laemmli SDS 样品缓冲液终止反应。磷酸化的MBP 进行10% SDS-PAGE分析
细胞实验:[1]
- 合并
  • Cell lines: K-Balb, KNRK, v-raf-3Y1, SRA/3Y1, EGFR/3T3, 和K562
  • Concentrations: 溶于DMSO, 终浓度~100 μM
  • Incubation Time: 3 天, 或者7-10天
  • Method: 细胞按10,000-20,000个/mL的密度接种在多孔平板中进行单层生长。48小时后把不同浓度的PD98059 加到细胞培养基孵育3天。 然后通过胰酶将细胞从平板中消化下来并用Coulter 计数器计数。 将细胞按5,000-10,000每皿的浓度接种在35 mm的培养皿中,培养基中含有0.3% 的琼脂和期望浓度的PD98059,让细胞在软琼脂上生长.经过7-10天的生长, 可以借助解剖显微镜将可见的菌落数出来。
    (Only for Reference)
动物实验:[7]
- 合并
  • Animal Models: 患有急性胰腺炎的雄性Sprague–Dawley 大鼠
  • Dosages: 10 mg/kg
  • Administration: 静脉注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 14 mg/mL warmed (52.37 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
1mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 267.28
化学式

C16H13NO3

CAS号 167869-21-8
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    How to formulate this inhibitor for i.p. injection?

  • 回答:

    You can prepare the stock by the vehicle 30% PEG400/0.5% Tween80/5% Propylene glycol, 0.5% CMC.

MEK Signaling Pathway Map

MEK Inhibitors with Unique Features

相关MEK产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID