PD98059

For research use only. Not for use in humans.

Catalog No.S1177

198 publications

PD98059 Chemical Structure

Molecular Weight(MW): 267.28

PD98059 is a non-ATP competitive MEK inhibitor with IC50 of 2 μM in a cell-free assay, specifically inhibits MEK-1-mediated activation of MAPK; does not directly inhibit ERK1 or ERK2.

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Selleck's PD98059 has been cited by 198 publications

Purity & Quality Control

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Biological Activity

Description PD98059 is a non-ATP competitive MEK inhibitor with IC50 of 2 μM in a cell-free assay, specifically inhibits MEK-1-mediated activation of MAPK; does not directly inhibit ERK1 or ERK2.
Features Does not inhibit c-Raf phosphorylated MEK1.
Targets
MEK1 [1]
(Cell-free assay)
2 μM
In vitro

PD98059 inhibits either basal MEK1 or a partially activated MEK produced by mutation of serine at residues 218 and 222 to glutamate (MEK-2E) with IC50 of 2 μM. PD98059 does not inhibit the MAPK homologues JNK and P38. PD98059 is highly selective against MEK, as it does not inhibit a number of other kinase activities including Raf kinase, cAMP-dependent kinase, protein kinase C, v-Src, epidermal growth factor (EGF) receptor kinase, insulin receptor kinase, PDGF receptor kinase, and phosphatidylinositol 3-kinase. PD98059 inhibits PDGF-stimulated activation of MAPK and thymidine incorporation into 3T3 cells with IC50 of ~10 μM and ~7 μM, respectively. [1] PD98059 potently prevents the activation of MEK1 by Raf or MEK kinase with IC50 of 4 μM, and weakly inhibits the activation of MEK2 by Raf with IC50 of 50 μM. PD98059 does not inhibit the activation of MEK homologues MKK4 and RK kinase that participate in stress and interleukin-1-stimulated kinase cascades in KB and PC12 cells, and the activation of p70 S6 kinase by insulin or epidermal growth factor in Swiss 3T3 cells. [2] PD98059 completely blocks the nerve growth factor (NGF)-induced differentiation of PC12 cells without altering cell viability. [3] PD98059 inhibits the proliferation of RAW264.7 cells in the culture containing RANKL in a dose-dependent manner, resulting in an apparent decrease of TRAP-positive cells. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
H1355 M2j6UGZ2dmO2aX;uJGF{e2G7 NWfRU|RwOjVizszN MmfmNUBp M2jmZ4JtfW62czD0bIUhSlujXWCtbY5lfWOnZDDpcoNz\WG|ZTDpckBxcG:|cHjvMWNpczFiYX7kJJBpd3OyaH:tSXJMKGW6cILld5Nqd25? MofKNlU4PjlzOEG=
MCF-7  NXnrfopJTnWwY4Tpc44hSXO|YYm= MkXkNVAh|ryP MUKxJIg> MYnpcohq[mm2czDJUE0yQC2nbnjhcoNm\CClZXzsJI1q\3KjdHnvci=> NF;JXFMzPTd{N{CxNS=>
HepG2  NELrNFJHfW6ldHnvckBCe3OjeR?= M4\XcVExKM7:TR?= NGrOSng2KGh? M3rnXIJtd2OtczDwbI9{eGixconsZZRm\CCPQWDLd{BqdmS3Y3XkJIJ6KGW6b3flco92eyCWR1[t{tIy MlyxNlU2PjB2OEi=
HepG2  MlLuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\BWGhxOjBizszN MViyOEBp MonGd5VxeHKnc4Pld{BVT0ZvzsKxMYlv\HWlZXSgZ4VtdCCycn;sbYZmemG2aX;uJIFv\CCrbo\hd4lwdg>? NHzheJIzPTV4MES4PC=>
MDA-MB-231 NW\EUXZ{TnWwY4Tpc44hSXO|YYm= MVWyOUDPxE1? MUSyMVMhcA>? Mofw[IVkemWjc3XzJJAuTVKNMT:yJIFv\CCVMUCwRVQh\XiycnXzd4lwdg>? NGOx[lAzPTV3NUi3OS=>
SW480 M2LMdWZ2dmO2aX;uJGF{e2G7 NGfHOVUzOMLizszN NX\SeFJLOcLiaB?= M1rFcJJm\HWlZYOgeIhmKGW6cILld5Nqd25ib3[gRXRHOyCycn;0[Ylv NF75XVQzPTR2N{ixOi=>
HCT-15 MUnGeY5kfGmxbjDBd5NigQ>? MXSxJIg> MnXaZZR1\W63YYTld{BRT0V{LXnu[JVk\WRicHjvd5Bpd3K7bHH0bY9vKG:oIFXyb:Kh NX\kPFBwOjV2M{G0NlU>
HCT-15 NWDlZ3F[SXCxcITvd4l{KEG|c3H5 NE\IVIgyKGh? MnjiZYJwdGm|aHXzJJRp\SCycn;0[YN1cX[nIHXm[oVkfHNib3[gVGdGOsLiYXfhbY5{fCCldYLjeY1qdi2rbnT1Z4VlKGGyb4D0c5Nqew>? M37SRlI2PDNzNEK1
786-O Ml;nRZBweHSxc3nzJGF{e2G7 NGHZcHg2OMLizszN MkHVNlQhcA>? NHrrXnhxd3SnboTpZZRme8LidHjlJJBzdy2jcH;weI91cWNiZX\m[YN1eyCxZjDORy=> M1\BWlI1PTB6NEe2
A498 NYTTPHVvSXCxcITvd4l{KEG|c3H5 M4LnN|UxyqEQvF2= NHjMW4wzPCCq M2OwT5BwfGWwdHnheIV{yqC2aHWgdJJwNWGyb4D0c5Rq[yCnZn\lZ5R{KG:oIF7D MlfGNlQ2ODh2N{[=
NHBE M1j0cGZ2dmO2aX;uJGF{e2G7 M1XL[lIwOjBizszN NYLDO25OOiCq NGHDW|VifHSnboXheIV{KEmOLUOzJJN1cW23bHH0[YQhS1iFTEivTWwuQCC|ZXPy[ZRqd25? NHHmdWMzPDR5OUWyOi=>
A375 M{G3WmNmdGxiSX72ZZNqd25iQYPzZZk> NF7OSZQyOOLCk{KwJOK2VQ>? M4TQOVI1KGh? NIHrTnlz\WS3Y3XzJI1mdGGwb33hJINmdGxiaX72ZZNqd25? NX;C[G5MOjR2Nk[wN|Y>
HBMEC MV7GeY5kfGmxbjDBd5NigQ>? M2nCTlExKM7:TR?= NYHkNIhpOSCq MlLNZoxw[2u|IG\FS2YucW6mdXPl[EBGeGiDMjDlfJBz\XO|aX;u MVOyOFQ2QDl6Mh?=
HPAEpiCs  NInmbI9HfW6ldHnvckBCe3OjeR?= NXnocWNuOzBizszN NGnhepUyKGh? M3HrO4lvcGmkaYTzJHRPTi4QsTDzeIlufWyjdHXkJJA1Oi:yNESgUWFRUyCyaH;zdIhwenmuYYTpc44> MoXCNlQ1PDF6N{C=
BeWo NEXnU4JHfW6ldHnvckBCe3OjeR?= Mk\CNVDDqM7:TR?= NELZOJczKGh? MVjpcohq[mm2czDFVmsyNzJ? NVHSO5FrOjR2M{O4OFY>
PC3  NIrGSpJCeG:ydH;zbZMhSXO|YYm= NVHmPGdVPTBizszN M3[3NFAvPSCq NH3YTYJqdmirYnn0d{BOUFlvNES5MYlv\HWlZXSgZZBweHSxc3nzxsA> MV[yOFQzPDh6OR?=
HGC-27 NIr2WGVCeG:ydH;zbZMhSXO|YYm= MnXBNUDDvU1? MVKxJIg> NWLlU2Vxe3WycILld5NmeyCUQVSwNFEheGy3czDNT{0zOjB4LXnu[JVk\WRiY3XscEB3cWGkaXzpeJkhdG:|cx?= M1LLcFI1PDF4M{S5
MCF-7 NFfPcGtHfW6ldHnvckBCe3OjeR?= MmfrNVDDqM7:TR?= Mlz5NVAwOzBibXnu MnS5doVlfWOnczD0bIUhXVSSLXTldIVv\GWwdDDFVmsheGixc4Doc5J6dGG2aX;u M2raWVI1OzlyOEG5
HUVECs MXPGeY5kfGmxbjDBd5NigQ>? MXKxNOKh|ryP NXL4cJQ{OSCq NIf2TmNqdmirYnn0d{B1cGViSFTMJJJm\HWlZXSgR29ZNTJiZYjwdoV{e2mxbjDhcoQhWEeLLUKgdoVt\WG|ZR?= M{jTcVI1Ozh3MUC5
HeLa NHfIdI1HfW6ldHnvckBCe3OjeR?= M2DPcFUxKM7:TR?= NIH1d3ExNjViaB?= M2HmZoJtd2OtczDUVnguOSCwdXPs[YFzKG2rZ4LheIlwdiCjbnSgWHhPUVBiZH;3ck1z\We3bHH0bY9v M161U|I1Ozd4OEK3
HL-60  M1jlVGZ2dmO2aX;uJGF{e2G7 M1TpWlExNzJyIN88US=> NVG0V|JHOSCq M3TQR4lvcGmkaYTzJJRp\cLiTj6gZ4hqdmWwc3nz[Zh1emGldNMgbY5lfWOnZDDkbYZn\XKnboTpZZRqd25iaX70c{BoemGwdXzvZ5l1\XN? MV:yOFM2PzB{MB?=
HL-60 NXvlXpRWTnWwY4Tpc44hSXO|YYm= MXeyJOK2VQ>? NIn0eVAyPiCq MXjEUXNQ MWLpcohq[mm2czD0bIUh[XO|b3PpZZRqd25ib3[gdHM3OjFiUnHmMVEh[W6mIF7GRXRkOyxiYX7kJJRp\SCUQT3pcoR2[2WmIIDoc5NxcG:{eXzheIlwdiCxZjDueYNt\WG{IF7GRXRkOw>? M4XIXVI1OzNyME[4
HEK 293 NUTKUJlETnWwY4Tpc44hSXO|YYm= MlPHNVAh|ryP MnXSOUBp M3PNNmROW09? NHLFTHJqdmirYnn0d{BYdnRvaX7keYNm\CEQsj3jZZRmdmmwL2TDSlQh[WO2aY\peJkh[W6mIH71Z4xm[XJizsKtZ4F1\W6rbjDhZ4N2dXWuYYTpc44> M{i1elI1OzJ2M{[2
HEK 293 NWnKUFE3TnWwY4Tpc44hSXO|YYm= MXWxNEDPxE1? NEj2PIY2KGh? M1nQeGROW09? NV7zPIsye3WycILld5NmeyC2aHWgR3JVKGGldHn2bZR6 NXnHTI52OjR|MkSzOlY>
SW480 MkDQSpVv[3Srb36gRZN{[Xl? NGf5T4UyOCEQvF2= M4PZcVIxKGh? MV3EUXNQ NUfNXm9Ze3WycILld5NmeyC2aHWgR3JVKGGldHn2bZR6 NFfpU2ozPDN{NEO2Oi=>
HCSMCs MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYKxNEDPxE1? M1rUUVI1KGh? NITMPVRjdG:la4OgSmFDWDRvaX7keYNm\CCKQ1HTUWMheHKxbHnm[ZJifGmxbh?= Mmn0NlQ{OTJ|OEG=
PANC-1 MWfGeY5kfGmxbjDBd5NigQ>? NEPPfpgzOCEQvF2= NYD4VYxJPDhiaB?= Mof1bY5pcWKrdIOgeIhmKGW6cILld5Nqd25ib3[g{rQ3TCCrbjDy[ZNxd26|ZTD0c{B1cGViUGDBVu61yqCjZ3;ubZN1yqB? NGHLeZczPDJ7NEGzNy=>
A549 M{LuR2Z2dmO2aX;uJGF{e2G7 MnraN|Ah|ryP NXH4dpJGOC53IHi= NEXkT3dFVVOR NGHCSWxqdmirYnn0d{B1cGVidHjyc41jcW5vaX7keYNm\CCLTD24M2NZS0x6LVz1Z{Bi[3Srdnn0fS=> M1zUXFI1Ojd5Nkm2
A549 MkHVSpVv[3Srb36gRZN{[Xl? NI\sPXU{OCEQvF2= MlHwNE42KGh? NFfhUWVFVVOR NFjJ[HVqdmirYnn0d{B1cHKxbXLpck1qdmS3Y3XkJGMwTUKSzsKgWIhzOjN3wrDwbI9{eGixconsZZRqd25? NWDGXVBWOjR{N{e2PVY>
MC-3 NFjaPGpCeG:ydH;zbZMhSXO|YYm= M{j3UlExKM7:TR?= MYKyOEBp MXfwc5RmdnSrYYTl[EBOTVOFLXnu[JVk\WRiYYDvdJRwe2m|IHnuJEBk\Wyucx?= MoHWNlQzPzB3MkO=
Raji  NV;1V2RUTnWwY4Tpc44hSXO|YYm= MlniNVAh|ryP NH22[4wyKGh? MV7icI9kc3NiaIPCRWZHKGmwZIXj[YQhTXKtMT:yJJBpd3OyaH;yfYxifGmxbh?= NISy[4gzPDJ4OU[zNC=>
Raji  M{TnUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYixNEDPxE1? MXWxJIg> MmK4bY5pcWKrdIOgeIhmKGKjc3HsJI9zKGi|QlHGSk1{fGmvdXzheIVlKGOnbHygdJJwdGmoZYLheIlwdiCjbnSgeoli[mmuaYT5 MXqyOFI3QTZ|MB?=
HT29 MkfFSpVv[3Srb36gRZN{[Xl? MXOxNEDPxE1? M3WxZlIhcA>? NVLv[HVkcW6qaXLpeJMhd2ZiSlHLNkwhTVKNMT:yJIFv\CCVVFHUN{BxcG:|cHjvdplt[XSrb36= NYDyfJBYOjR{NkWyPVM>
HepG2 NUHGUmp1SXCxcITvd4l{KEG|c3H5 M1PzTVIxKM7:TR?= MXqyOEBp MXnpcohq[mm2czDFVmsyNzJicHjvd5Bpd3K7bHH0bY9vKGGwZDDlcohidmOnczDWRlEucW6mdXPl[EBieG:ydH;zbZM> Ml24NlQzPDd7MEm=
HepG2 MU\GeY5kfGmxbjDBd5NigQ>? NGfiTJAzOCEQvF2= NVm4W29sOiCq NHu3SmdmdmijbnPld{BXSjFvaX7keYNm\CCIT2jPN4EhfHKjboPjdolxfGmxbnHsJIFkfGm4aYT5 NFTO[Y0zPDJ2N{mwPS=>
TE4 M2i1NWZ2dmO2aX;uJGF{e2G7 M{\pdlIxNzVyL{GwNEDPxE1? MXy0PEBp MmPYSG1UVw>? NYjCVG9HcW6qaXLpeJMheC2HcnugZY5lKHexcoTtZY5vcW5iZH;3cpJm\3WuYYTl[EBxNUGtdDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= M2\1fFI1OjR2MEKz
TE1 Ml7GSpVv[3Srb36gRZN{[Xl? M2fSZlIxNzVyL{GwNEDPxE1? M4fKSFQ5KGh? NH76NodFVVOR M1XUdolvcGmkaYTzJJAuTXKtIHHu[EB4d3K2bXHucolvKGSxd37y[Yd2dGG2ZXSgdE1Cc3RiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NFjES5gzPDJ2NECyNy=>
KYSE30 NWTyZY8{TnWwY4Tpc44hSXO|YYm= NF7k[3MzOC93MD:xNFAh|ryP Mo\UOFghcA>? MWTEUXNQ MYXpcohq[mm2czDwMWVzcyCjbnSge49zfG2jbn7pckBld3ewcnXneYxifGWmIICtRYt1KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M3LJR|I1OjR2MEKz
TE1 NX22OVlvTnWwY4Tpc44hSXO|YYm= NYftZ2J{PTBizszN Mm\jOFghcA>? NGDCV3lFVVOR MmrEeZBz\We3bHH0[ZMhfGinIHX4dJJme3Orb36gc4YhUEyDIHPsZZN{KEl? NXzDTXBuOjR{NESwNlM>
TE3 MorQSpVv[3Srb36gRZN{[Xl? MojGOVAh|ryP MV20PEBp M1vLUmROW09? NX[2OY8zfXC{ZXf1cIF1\XNidHjlJIV5eHKnc4Ppc44hd2ZiSFzBJINt[XO|IFm= MkKwNlQzPDRyMkO=
TE4 M1vJTWZ2dmO2aX;uJGF{e2G7 Moi1OVAh|ryP NHXWR2M1QCCq Mm[ySG1UVw>? NInqUpl2eHKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCKTFGgZ4xie3NiSR?= MWeyOFI1PDB{Mx?=
TE5 Mo\2SpVv[3Srb36gRZN{[Xl? MoPWOVAh|ryP NGS2c|Q1QCCq MX;EUXNQ MUf1dJJm\3WuYYTld{B1cGViZYjwdoV{e2mxbjDv[kBJVEFiY3zhd5MhUQ>? MmH3NlQzPDRyMkO=
KYSE30 M2TkNmZ2dmO2aX;uJGF{e2G7 MnPIOVAh|ryP NHjPUFM1QCCq MmnrSG1UVw>? NUHKdpJFfXC{ZXf1cIF1\XNidHjlJIV5eHKnc4Ppc44hd2ZiSFzBJINt[XO|IFm= MWWyOFI1PDB{Mx?=
MKN7 NVW2OlM1TnWwY4Tpc44hSXO|YYm= M{PUfFUxKM7:TR?= NXG1dJU5PDhiaB?= Mof4SG1UVw>? MVzpcoNz\WG|ZYOg[ZhxemW|c3nvckBw\iCKTFGtRVAzKG:{IFjMRU1COjRibX;s[YN2dGW| M2qzPFI1OjR2MEKz
OE19 NIGzPZFHfW6ldHnvckBCe3OjeR?= MUO1NEDPxE1? MmPNOFghcA>? M13rRWROW09? M{fHS4lv[3KnYYPld{BmgHC{ZYPzbY9vKG:oIFjMRU1CODJib4KgTGxCNUF{NDDtc4xm[3WuZYO= M2HTR|I1OjR2MEKz
KATOIII  M{e3eGZ2dmO2aX;uJGF{e2G7 M3\mUVUxKM7:TR?= NEXWe2Y1QCCq NGfre|hFVVOR NFuzV4tqdmO{ZXHz[ZMh\XiycnXzd4lwdiCxZjDIUGEuSTB{IH;yJGhNSS2DMkSgcY9t\WO3bHXz NGKye2gzPDJ2NECyNy=>
NCI-N87  NVrWdIo1TnWwY4Tpc44hSXO|YYm= NYCzcopoPTBizszN NEHYeWk1QCCq NEPTbopFVVOR M1TCRolv[3KnYYPld{BmgHC{ZYPzbY9vKG:oIFjMRU1CODJib4KgTGxCNUF{NDDtc4xm[3WuZYO= NFfLWIEzPDJ2NECyNy=>
NUGC3 MYjGeY5kfGmxbjDBd5NigQ>? NYXtUYNtPTBizszN NW\BfGVHPDhiaB?= Mki4SG1UVw>? NWHRR4QzcW6lcnXhd4V{KGW6cILld5Nqd25ib3[gTGxCNUFyMjDvdkBJVEFvQUK0JI1wdGWldXzldy=> NXKxPWZVOjR{NESwNlM>
NUGC2 MmfSSpVv[3Srb36gRZN{[Xl? NF7QWFA2OCEQvF2= MnTKOFghcA>? MmHaSG1UVw>? NGjCeZdqdmO{ZXHz[ZMh\XiycnXzd4lwdiCxZjDIUGEuSTB{IH;yJGhNSS2DMkSgcY9t\WO3bHXz NID1coYzPDJ2NECyNy=>
SGC-7901  NVf3dpFmSXCxcITvd4l{KEG|c3H5 M3rBR|IxKM7:TR?= MV[yOEBp M2nBc4lvcGmkaYTzJGNRNW2nZHnheIVlKGGyb4D0c5Nqew>? NFPLTVYzPDJ2MUO1NS=>
MG-63 MYXGeY5kfGmxbjDBd5NigQ>? M3n0Z|IxKM7:TR?= NHi0W4UxNjViaB?= MYPicI9kc3NidHjlJGNJNWmwZIXj[YQheGixc4Doc5J6dGG2ZXSgSWxMOSCycn;0[YlvKGW6cILld5Nqd25? M1m2VVI1OjN7NkSw
ARPE-19 MWrGeY5kfGmxbjDBd5NigQ>? NYPjc4E2OjBizszN MYGwMlUhcA>? MmWxbY5pcWKrdIOgRZBmdGmwLXnu[JVk\WRicHjvd5Bpd3K7bHH0bY9vKG:oIFXyb{BidmRiQXv0 MWeyOFIzPzlzOB?=
CRL-2302 M1SwWWZ2dmO2aX;uJGF{e2G7 NFX0dY0zOCEQvF2= M1;xclAvPSCq M4nK[4lvcGmkaYTzJGFx\Wyrbj3pcoR2[2WmIIDoc5NxcG:{eXzheIlwdiCxZjDFdosh[W6mIFHreC=> MViyOFIzPzlzOB?=
MCF-7 MlrjSpVv[3Srb36gRZN{[Xl? MYKyNEDPxE1? MlTYNUBp MVjhZo9tcXOqZYOg[ZhxemW|c3nvckBw\iCyaH;zdIhwenmuYYTl[EBGWktiY3:teJJm[XSvZX70JJdqfGhiY3;ubpVo[XSn M3fFN|I1OjF4Mki5
MCF-7 MoTPRZBweHSxc3nzJGF{e2G7 MmXDNlAh|ryP MXSxJIg> NWfE[XJocW6lcnXhd4V{KGOjc4Dhd4UuQSCnbor5cYUh[WO2aY\peJk> NGLtOYozPDJzNkK4PS=>
DLD-1  NYTadJNVTnWwY4Tpc44hSXO|YYm= M3yy[|IxyqEQvF2= MXS0PEBp NIrsXJNz\WS3Y3XzJJRp\SCETlnQN{BmgHC{ZYPzbY9vKHC{ZT30doVifGWmIIfpeIghPS2jenGt[GM> M1TEeFI1OjFzNUix
HT-29 MlzRSpVv[3Srb36gRZN{[Xl? MVKyNOKh|ryP MWO0PEBp NEH2e|Rz\WS3Y3XzJJRp\SCETlnQN{BmgHC{ZYPzbY9vKHC{ZT30doVifGWmIIfpeIghPS2jenGt[GM> Mn;CNlQzOTF3OEG=
7402 Mm\XRZBweHSxc3nzJGF{e2G7 NYDxN3dwOzBizszN M1;hVFUh\A>? MnrD[IVkemWjc3XzJINmdGxicILvcIln\XKjdHnvci=> MofmNlQzOTF{NUO=
7721 NFPReplCeG:ydH;zbZMhSXO|YYm= NWHzV5llOzBizszN MXu1JIQ> MYHk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;u Ml3DNlQzOTF{NUO=
SGC7901  NVTVdWF5SXCxcITvd4l{KEG|c3H5 M3zNeFUxyqEQvF2= NInYN5EzPC92OD:3NkBp MnGzSG1UVw>? M4nifYlv\HWlZYOgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiSlHLNkB{cFKQQR?= NIDEVJozPDF5OEK0NC=>
SMMC7721 M3S2cmZ2dmO2aX;uJGF{e2G7 Mn\2NlUwPTBizszN NH;BfIszPCCq NXW0bGNbe3WycILld5NmeyC2aHWg[ZhxemW|c3nvckBw\iCyLVHreEBweiCyLVXST|EwOsLi NH;RVWwzPDF4OEC1Oi=>
MCF-7 M4LUfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXqxNEDPxE1? NX3mVW9pPDiq MVfEUXNQ M13qNpJmfmW{c3XzJGJPTi2rbnT1Z4VlKGOnbHygZ5lkdGViYYLy[ZN1 MWCyOFE3OzRyNB?=
Caco-2 NUC1TlZjTnWwY4Tpc44hSXO|YYm= MWm1NOKh|ryP M3fWXlQ5cA>? MlnQSG1UVw>? MYrlcohidmOnczD0bIUhdVKQQTDs[ZZmdHNib3dCpHNEVk5zQTzGXHlFOy{EoFzDWEzDqEyRWD|CpGhKTjODLNMgXmcyPi{EoGDESVZCyqCjbnVCpGxISUyVMUdCpIdmdmW|wrDjc{11emWjdHXkJJdqfGhiRHX4 NX\JToZ1OjRzNkG2PVU>
HAECs NXPWS4R[TnWwY4Tpc44hSXO|YYm= MWixNEDPxE1? M13JRlEhcA>? MYdCpIF1fGWwdXH0[ZMhXE6ILd8xMZN1cW23bHH0[YQhUUODTT2xJIFv\CCYQ1HNMVEh\XiycnXzd4lwdg>? NGfxXZozPDF|NE[1Oy=>
Ca9-22 M2LleWZ2dmO2aX;uJGF{e2G7 NFGxUpk{KM7:TR?= MYOxJIg> NWrXNY92[WKxbHnzbIV{KHSqZTDhZoltcXS7IH;mJGhjWiC2bzDpcoR2[2ViSVytPEBxem:mdXP0bY9v Mn;1NlQyOjZ3M{K=
Ca9-22 MW\GeY5kfGmxbjDBd5NigQ>? MorYN{DPxE1? NFHOW3QyNzJiaB?= M1O4UZJm\HWlZYOgTIJTNWmwZIXj[YQhSVSILUKgdIhwe3Cqb4L5cIF1cW:w MX2yOFEzPjV|Mh?=
AGS MVTGeY5kfGmxbjDBd5NigQ>? M3rEclExKM7:TdMg NEnpfmwxNjViaB?= NI\QN2FqdmirYnn0d{B1cGVidYDy[Yd2dGG2aX;uJI9nKHSqZTDJUE05KGenbnW= MnvTNlQyODZzNk[=
Caco-2  MWXBdI9xfG:|aYOgRZN{[Xl? NGfXOpkyOMLizszN M{T3dVI1yqCq NFziUIxl\WO{ZXHz[ZMh[2WubDDhdI9xfG:|aYOgbY5lfWOnZDDifUA2NU[X MWKyOFA6PTh4Mx?=
HCT-8 NYizT5Q1SXCxcITvd4l{KEG|c3H5 M3LKUFExyqEQvF2= MUOyOOKhcA>? M4\WTYRm[3KnYYPld{Bk\WyuIHHwc5B1d3OrczDpcoR2[2WmIHL5JFUuTlV? MVqyOFA6PTh4Mx?=
A549 M4XyUGZ2dmO2aX;uJGF{e2G7 M{fIXVUxyqEQvF2= MlPjNkBp M1HCT4Jtd2OtczDFVmsheGixc4Doc5J6dGG2aX;uJI1m\GmjdHXkJIJ6KDFuMj3OVS=> M1TsW|I1ODZ5N{K3
HPMC NETTRVBHfW6ldHnvckBCe3OjeR?= M1LEeFExyqEQvF2= NW\wOph2PDhiaB?= NWLGUGRwemW4ZYLz[ZMhfGinIHPoZY5o\XNiaX6gZ4VtdCCvb4LwbI9td2e7IHnu[JVk\WRiYomgTGdRTFN? NFL5cokzPDB2MkizPC=>
HPMC M2P3NmFxd3C2b4Ppd{BCe3OjeR?= M4L2NVExyqEQvF2= MWiyOOKhcA>? MmfJdoV3\XK|ZYOg[IVkemWjc3WgbY4h[2WubDD2bYFjcWyrdImgbY5lfWOnZDDifUBJT1CGUx?= MWOyOFA1Ojh|OB?=
MGC803  M4H3PWFxd3C2b4Ppd{BCe3OjeR?= NVfH[Zg5OjEEoN88US=> NX:5Z2lDOSCq NF73bpZqdmirYnn0d{BieG:ydH;zbZMhcW6mdXPl[EBjgSCLRl6t{tHDqGGwZDC15qCzNUSIVWK= NHuyRWkzPDB{N{e1NC=>
SGC7901 M2HRNWFxd3C2b4Ppd{BCe3OjeR?= MkLLNlDDqM7:TR?= NHmySJIyKGh? MkiybY5pcWKrdIOgZZBweHSxc3nzJIlv\HWlZXSgZpkhUU[QLd8xxsBidmRiNfMAtk1FTlWU NXHVdWl3OjRyMke3OVA>
COLO205 NGnvc49CeG:ydH;zbZMhSXO|YYm= Mne1NVAwOjBxNECg{txO MkTqNlQhcA>? NWfwZ2VpcW6mdXPld{BFVkFibHHk[IVzKG[xcn3heIlwdg>? M{jkXVI1ODF7MUC4
G292  NHXTRpdCeG:ydH;zbZMhSXO|YYm= NWLGV4QyOzEEoN88US=> M37zW|IhcA>? M1v1UpJme3SxcnXzJINieHOjaXPpck1qdmS3Y3XkJINmdGxiZHXheIg> NH\weWwzPDBzMkmzNC=>
BxPC-3 M{T6dWZ2dmO2aX;uJGF{e2G7 NIL4[I0yOCEQvF5CpC=> MYe2JIg> M4CySolv[3KnYYPlJI1qWi1zNEOg[ZhxemW|c3nvci=> MkfuNlM6PzN5MUC=
HPAF-II MnHRSpVv[3Srb36gRZN{[Xl? M3\iUFExKM7:TdMg Mnf1OkBp MX\pcoNz\WG|ZTDtbXIuOTR|IHX4dJJme3Orb36= MonmNlM6PzN5MUC=
HL-60 NUXLd3BmSXCxcITvd4l{KEG|c3H5 NUfk[YpyPTEEoN88US=> M{LBXVEhcA>? M1OydpJme2O3ZYOgRmEyPDVibXXkbYF1\WRiYYDvdJRwe2m| NYnkfIh1OjN7NEi3OVE>
HepG2 MUXGeY5kfGmxbjDBd5NigQ>? NVezRWVjPDBizszN NVX3WnI3Pi9zMjDo MUXpcohq[mm2czD0bIUhcW6lcnXhd4Uhd2ZicD3FVmsyKGGwZDDwMYMuUnWwIIDyc5RmcW5iZYjwdoV{e2mxbjDifUBRVA>? NVXjRWpzOjN7NEK4OVE>
HUVECs MmHmSpVv[3Srb36gRZN{[Xl? M3faPFI2KM7:TR?= M1Pud|EhcA>? NHXGNYdqdmO{ZXHz[UBPTi4QulKgdFY2KG63Y3zlZZIhfHKjboPsc4NifGmxbh?= NIPpXmMzOzlyMUCwPC=>
LNCaP  NFHyflhHfW6ldHnvckBCe3OjeR?= MVuxNEDPxE4EoB?= MlTaNUBp M2S1PIRm[3KnYYPld{B1cGViRVfGJJVxemWpdXzheIVlKHBvWVKtNS=> NVf3d3RVOjN6M{izNVg>
HL60  Ml\nSpVv[3Srb36gRZN{[Xl? MYKyNOKh|ryP MUK3NkBp Mn\tSG1UVw>? Moj3bY5pcWKrdIOg[IF{[XSrbnniMYlv\HWlZXSgR2QyOWJiZYjwdoV{e2mxbh?= MkHUNlM5OjV3OEW=
NB4  NWr6THc2TnWwY4Tpc44hSXO|YYm= NYDyW5BUOTBizszNxsA> NWH1VpI4PzJiaB?= NHvi[45FVVOR MWXpcohq[mm2czDkZZNifGmwaXKtbY5lfWOnZDDDSFEy[iCneIDy[ZN{cW:w M{DVd|I{QDJ3NUi1
EPOR/CR3 NGjDUFhHfW6ldHnvckBCe3OjeR?= MWq1NOKh|ryP NGLxVVM{KGh? Mn33doVlfWOnczDFVG8h[W6mL3;yJGlNNTNvaX7keYNm\CC2aHWgeJlzd3OrbnWgdIhwe3Cqb4L5cIF1cW:wwrC= NVmydmRKOjN6MkC3N|E>
HUASMCs NYCzeYVbTnWwY4Tpc44hSXO|YYm= MWexNEDPxE4EoB?= MXyyOEBp M3fmOYRqdWmwaYPo[ZMhSW6pIFnJMYNifXOnZDDTU2NUOyCvUl7BJIFv\CCycn;0[YlvKGW6cILld5Nqd28EoB?= Mly1NlM5OTZ2Nki=
HUASMCs M3;zR2Z2dmO2aX;uJGF{e2G7 NHLUcokyOCEQvF5CpC=> NYL5eGZsOjRiaB?= MYHpcohq[mm2czDBcochUUlvaX7keYNm\CCHUluxM|IheGixc4Doc5J6dGG2aX;uJIxmfmWu NIjzSmYzOzhzNkS2PC=>
SGC7901 MWXGeY5kfGmxbjDBd5NigQ>? MXixNEDPxE4EoB?= MlT0NlQhcA>? NHrzcmZqdmirYnn0d{B1cGViZYjwdoV{e2mxbjDv[kBxcG:|cHjvdplt[XSnZDDFVmsyNzJ? NEH1dW4zOzd7MkW4PC=>
MKN45 NYTrSlVrTnWwY4Tpc44hSXO|YYm= NW\WPZVbOTBizszNxsA> NFy1WlEzPCCq M1fjOIlvcGmkaYTzJJRp\SCneIDy[ZN{cW:wIH;mJJBpd3OyaH;yfYxifGWmIFXST|EwOg>? NGLYVoUzOzd7MkW4PC=>
SGC7901 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{C1VlExKM7:TdMg NGewZ|EzPC92OD:3NkBp NFjM[4xqdmirYnn0d{Bk\WyuIHfyc5d1cCClbz30doVifGWmIIfpeIghTEGSVB?= M{LxS|I{Pzl{NUi4
MKN45 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELF[lgyOCEQvF5CpC=> MVmyOE81QC95MjDo M3qxdYlvcGmkaYTzJINmdGxiZ4Lve5RpKGOxLYTy[YF1\WRid3n0bEBFSVCW MU[yN|c6OjV6OB?=
SGC7901 MlPtRZBweHSxc3nzJGF{e2G7 NV3FN3ZGOTBizszNxsA> NVLmSFhOOjRiaB?= MljBbY5kemWjc3XzJJRp\SCGQWDUMYlv\HWlZXSgZ4VtdCCjcH;weI9{cXN? NULteHZOOjN5OUK1PFg>
MKN45 NXPXbmFVSXCxcITvd4l{KEG|c3H5 MkXPNVAh|ryPwrC= NEj3SY0zPCCq NHTRN2JqdmO{ZXHz[ZMhfGinIFTBVHQucW6mdXPl[EBk\WyuIHHwc5B1d3Orcx?= MkDsNlM4QTJ3OEi=
BxPC-3 cells MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1f4SlIxyqEQvF2= NUS5bG1xOC53IHi= M1jnNYlvcGmkaYTzJHZGT0ZvQT3y[Yd2dGG2ZXSgTHVXTUNiZ4Lve5RpKGGwZDD0eYJmKG[xcn3heIlwdiCrbnT1Z4VlKGK7IGDBVk0zKEGS NHLLU40zOzd4NEC0Oi=>
NB4  MlvuRZBweHSxc3nzJGF{e2G7 NUXMepltOTBxMkCvOlAh|ryP NITkU2YyNjViaB?= MWHEUXNQ MYrk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliY3:teJJm[XSnZDD3bZRpKFCjY3zpeIF5\Wx? NHHDdo4zOzd|NUW0NS=>
HepG2  M3nBXGZ2dmO2aX;uJGF{e2G7 MkjmNlDDqM7:TR?= NU\tcI8{OjRiaB?= NH2zPVdqdmirYnn0d{B1cGViSF:tNUBxem:2ZXnuJIV5eHKnc4Ppc44h[29vdILlZZRm\CC5aYToJI1mfG[xcn3pci=> M2LoPVI{PzB5NkC5
HUVECs M3LaXWFxd3C2b4Ppd{BCe3OjeR?= MUSyM|Qh|ryP NWTkfGNuOjRxNEigbC=> MXLpcoR2[2W|IHPlcIwh\GWjdHi= NX3nc|duOjN5MEe1NlA>
KG-1  MXnBdI9xfG:|aYOgRZN{[Xl? MVeyNOKh|ryP M1nqZ|EzKGh? NInsfoNmdmijbnPld{Bk\WyuIHHwc5B1d3OrczDpcoR2[2WmIHL5JHMy NH\3ZWwzOzdyNk[5NS=>
AML 1# MXPBdI9xfG:|aYOgRZN{[Xl? MmLkNlDDqM7:TR?= M4i4b|EzKGh? M3jTboVvcGGwY3XzJINmdGxiYYDvdJRwe2m|IHnu[JVk\WRiYomgV|E> NI\jdFYzOzdyNk[5NS=>
A2780  M3TNOWZ2dmO2aX;uJGF{e2G7 NH7rVW4zOMLizszN NX\xcVZROSCq NVjXcGhi[myxY3vzJGRVS0RvaX7keYNm\CCGUkWg[ZhxemW|c3nvci=> M1[2VFI{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
In vivo Treatment of mice 30 minutes before focal cerebral ischemia with PD98059 protects against damage, resulting in a decrease in infarct volume. [5] Pretreated with PD98059 (10 mg/kg per i.v. injection) 30 minutes before and then together with hourly cerulein injections for 3 hours significantly ameliorates cerulein-induced acute pancreatitis ipancreatitis on the basis of pancreatic wet weight and histology. [6] Administration of PD98059 (10 mg/kg) in mice 1 hour after carrageenan causes a reduction in all the parameters of inflammation measured. [7]

Protocol

Kinase Assay:

[1]

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In vitro MEK-inhibitory activity:

Incorporation of 32P into myelin basic protein (MBP) is assayed in the presence of glutathione S-transferase (GST) fusion proteins containing the 44-kDa MAPK (GST-MAPK) or the 45-kDa MEK (GST-MEK1). Assays are conducted in 50 μL of 50 mM Tris, pH 7.4/10 mM MgCl2/2 mM EGTA/10 μM [γ-32P]ATP containing 10 μg of GST-MEK1, 0.5 μg of GST-MAPK, and 40 μg of MBP. After incubation at 30°C for 15 minutes, reactions are stopped by addition of Laemmli SDS sample buffer. Phosphorylated MBP is resolved by SDS/10% PAGE.
Cell Research:

[1]

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  • Cell lines: K-Balb, KNRK, v-raf-3Y1, SRA/3Y1, EGFR/3T3, and K562
  • Concentrations: Dissolved in DMSO, final concentrations ~100 μM
  • Incubation Time: 3 dyas, or 7-10 days
  • Method:

    For monolayer growth, cells are plated into multi-well plates at 10,000-20,000/mL. Forty-eight hours later, various concentrations of PD98059 are added to the cell growth medium and incubation is continued for an additional 3 days. Cells are then removed from the wells by incubation with trypsin and enumerated with a Coulter Counter. For growth in soft agar, cells are seeded into 35-mm dishes at 5,000-10,000 cells per dish with growth medium containing 0.3% agar and desired concentrations of PD98059. After 7-10 days of growth, visible colonies are manually enumerated with the aid of a dissecting microscope.


    (Only for Reference)
Animal Research:

[7]

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  • Animal Models: Male Sprague–Dawley rats with acute pancreatitis
  • Formulation: Dissolved in DMSO, and diluted in saline
  • Dosages: 10 mg/kg
  • Administration: Injection i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 14 mg/mL warmed (52.37 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
1mg/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 267.28
Formula

C16H13NO3

CAS No. 167869-21-8
Storage powder
in solvent
Synonyms N/A
Smiles COC1=C(N)C(=CC=C1)C2=CC(=O)C3=CC=CC=C3O2

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

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

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
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Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

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

  • Answer:

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID