PD98059

For research use only.

Catalog No.S1177

272 publications

PD98059 Chemical Structure

CAS No. 167869-21-8

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. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR) and functions as an AHR antagonist.

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Selleck's PD98059 has been cited by 272 publications

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Choose Selective MEK Inhibitors

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. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR) and functions as an AHR antagonist.
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 Mk\ESpVv[3Srb36gRZN{[Xl? M{S0TFI2KM7:TR?= MnjjNUBp NGXJNHZjdHWwdIOgeIhmKEKdYW3QMYlv\HWlZXSgbY5kemWjc3WgbY4heGixc4Doc{1EcGtzIHHu[EBxcG:|cHjvMWVTUyCneIDy[ZN{cW:w M1LleVI2PzZ7MUix
MCF-7  NYS5VmZDTnWwY4Tpc44hSXO|YYm= M3\hW|ExKM7:TR?= MUKxJIg> Mm\NbY5pcWKrdIOgTWwuOThvZX7oZY5k\WRiY3XscEBucWe{YYTpc44> M1rBSFI2PzJ5MEGx
HepG2  NHewe3BHfW6ldHnvckBCe3OjeR?= NVvMWWk3OTBizszN MWO1JIg> NEHoRVhjdG:la4OgdIhwe3Cqb4L5cIF1\WRiTVHQT5MhcW6mdXPl[EBjgSCneH;n[Y5wfXNiVFfGMe6zOQ>? NYLkZXozOjV3NkC0PFg>
HepG2  NVXNOFBCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnCZlZbOjBizszN NXTNVGt4OjRiaB?= Mknud5VxeHKnc4Pld{BVT0ZvzsKxMYlv\HWlZXSgZ4VtdCCycn;sbYZmemG2aX;uJIFv\CCrbo\hd4lwdg>? NGnMTpkzPTV4MES4PC=>
MDA-MB-231 NV\Fe|RNTnWwY4Tpc44hSXO|YYm= MmjrNlUh|ryP MoToNk0{KGh? MlPn[IVkemWjc3XzJJAuTVKNMT:yJIFv\CCVMUCwRVQh\XiycnXzd4lwdg>? M1LM[lI2PTV3OEe1
SW480 MkDKSpVv[3Srb36gRZN{[Xl? MWeyNOKh|ryP MmX3NeKhcA>? MUDy[YR2[2W|IITo[UBmgHC{ZYPzbY9vKG:oIFHUSlMheHKxdHXpci=> NU\oXlllOjV2NEe4NVY>
HCT-15 M3jZcmZ2dmO2aX;uJGF{e2G7 NEmzVWMyKGh? M3;EWoF1fGWwdXH0[ZMhWEeHMj3pcoR2[2WmIIDoc5NxcG:{eXzheIlwdiCxZjDFdovDqA>? MXmyOVQ{OTR{NR?=
HCT-15 M3Xs[mFxd3C2b4Ppd{BCe3OjeR?= MXmxJIg> MW\hZo9tcXOqZYOgeIhmKHC{b4TlZ5RqfmViZX\m[YN1eyCxZjDQS2UzyqCjZ3HpcpN1KGO3cnP1cYlvNWmwZIXj[YQh[XCxcITvd4l{ M2P3UlI2PDNzNEK1
786-O NWq2XIo6SXCxcITvd4l{KEG|c3H5 MnO4OVDDqM7:TR?= NFLiT3ozPCCq M4K4UpBwfGWwdHnheIV{yqC2aHWgdJJwNWGyb4D0c5Rq[yCnZn\lZ5R{KG:oIF7D NV7ybXBJOjR3MEi0O|Y>
A498 NITkUHhCeG:ydH;zbZMhSXO|YYm= MU[1NOKh|ryP Mn;4NlQhcA>? M3Ps[JBwfGWwdHnheIV{yqC2aHWgdJJwNWGyb4D0c5Rq[yCnZn\lZ5R{KG:oIF7D MnLzNlQ2ODh2N{[=
NHBE MoLVSpVv[3Srb36gRZN{[Xl? M3LsUVIwOjBizszN NX;mb4RuOiCq MXHheJRmdnWjdHXzJGlNNTN|IIP0bY12dGG2ZXSgR3hEVDhxSVytPEB{\WO{ZYTpc44> NVT2OFdTOjR2N{m1NlY>
A375 M{DpSWNmdGxiSX72ZZNqd25iQYPzZZk> NWTrfohzOTEkgKOyNEDDvU1? MX:yOEBp M3n3U5Jm\HWlZYOgcYVt[W6xbXGgZ4VtdCCrbo\hd4lwdg>? NX\teFBqOjR2Nk[wN|Y>
HBMEC M3\oXGZ2dmO2aX;uJGF{e2G7 M172WlExKM7:TR?= M1\SWVEhcA>? MoPYZoxw[2u|IG\FS2YucW6mdXPl[EBGeGiDMjDlfJBz\XO|aX;u NFTFUlIzPDR3OEm4Ni=>
HPAEpiCs  NG\HNmdHfW6ldHnvckBCe3OjeR?= MXSzNEDPxE1? NYP0d2dYOSCq MWjpcohq[mm2czDUUmYu|rFic4TpcZVt[XSnZDDwOFIweDR2IF3BVGsheGixc4Doc5J6dGG2aX;u MWGyOFQ1OTh5MB?=
BeWo NGjwPXBHfW6ldHnvckBCe3OjeR?= MVWxNOKh|ryP NUjIfWNlOiCq MnrwbY5pcWKrdIOgSXJMOS9{ MojUNlQ1OzN6NE[=
PC3  NWrSVo1USXCxcITvd4l{KEG|c3H5 NF3HWZE2OCEQvF2= NUHQZnBjOC53IHi= NGnib2xqdmirYnn0d{BOUFlvNES5MYlv\HWlZXSgZZBweHSxc3nzxsA> MVKyOFQzPDh6OR?=
HGC-27 MlfORZBweHSxc3nzJGF{e2G7 NIS1cGMyKML3TR?= NX\pTXcyOSCq NXTa[JZme3WycILld5NmeyCUQVSwNFEheGy3czDNT{0zOjB4LXnu[JVk\WRiY3XscEB3cWGkaXzpeJkhdG:|cx?= NVvp[Yg1OjR2MU[zOFk>
MCF-7 NIfYV4FHfW6ldHnvckBCe3OjeR?= MX:xNOKh|ryP MVWxNE8{OCCvaX6= NF7YWVBz\WS3Y3XzJJRp\SCXVGCt[IVx\W6mZX70JGVTUyCyaH;zdIhwenmuYYTpc44> NGGzbmIzPDN7MEixPS=>
HUVECs M{TQbmZ2dmO2aX;uJGF{e2G7 NYntXVhUOTEEoN88US=> M4W0R|EhcA>? MmHlbY5pcWKrdIOgeIhmKEiGTDDy[YR2[2WmIFPPXE0zKGW6cILld5Nqd25iYX7kJHBIUS1{IILlcIVie2V? NUXPcGwyOjR|OEWxNFk>
HeLa NHK4RW9HfW6ldHnvckBCe3OjeR?= MlHkOVAh|ryP NVy2SmJEOC53IHi= MV3icI9kc3NiVGLYMVEhdnWlbHXhdkBucWe{YYTpc44h[W6mIGTYUmlRKGSxd36tdoVofWyjdHnvci=> NYK0cJRSOjR|N{[4Nlc>
HL-60  NXjtRlY{TnWwY4Tpc44hSXO|YYm= M1PlO|ExNzJyIN88US=> MVmxJIg> NGSyWndqdmirYnn0d{B1cGYEoF6uJINpcW6nboPpd4V5fHKjY4VCpIlv\HWlZXSg[Iln\mW{ZX70bYF1cW:wIHnueI8h\3KjboXsc4N6fGW| MkDlNlQ{PTdyMkC=
HL-60 NH\aXIpHfW6ldHnvckBCe3OjeR?= MkHRNkDDvU1? NH;lcI4yPiCq NG[zO3pFVVOR NUDiXItHcW6qaXLpeJMhfGinIHHzd49kcWG2aX;uJI9nKHCVNkKxJHJi\i1zIHHu[EBPTkGWY{OsJIFv\CC2aHWgVmEucW6mdXPl[EBxcG:|cHjvdplt[XSrb36gc4YhdnWlbHXhdkBPTkGWY{O= NFvDdZAzPDN|MEC2PC=>
HEK 293 MnvHSpVv[3Srb36gRZN{[Xl? M2f0eVExKM7:TR?= M1G0RVUhcA>? NV7kbmZ5TE2VTx?= NX\LZXNScW6qaXLpeJMhX262LXnu[JVk\WRizsKtZ4F1\W6rbj;UR2Y1KGGldHn2bZR6KGGwZDDueYNt\WG{IN8yMYNifGWwaX6gZYNkfW23bHH0bY9v MkDwNlQ{OjR|Nk[=
HEK 293 M1LvT2Z2dmO2aX;uJGF{e2G7 NH\kWFEyOCEQvF2= NWjUPIViPSCq NWLsN4ptTE2VTx?= NIfuZ21{fXCycnXzd4V{KHSqZTDDVnQh[WO2aY\peJk> MWGyOFMzPDN4Nh?=
SW480 NIe0SGxHfW6ldHnvckBCe3OjeR?= M1zwNFExKM7:TR?= NVLsVWd3OjBiaB?= NEDMW5VFVVOR MWrzeZBxemW|c3XzJJRp\SCFUmSgZYN1cX[rdIm= Mk\RNlQ{OjR|Nk[=
HCSMCs M4D5SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrvZ4ZTOTBizszN M3nC[FI1KGh? M2\nPYJtd2OtczDGRWJRPC2rbnT1Z4VlKEiFQWPNR{Bxem:uaX\ldoF1cW:w MonqNlQ{OTJ|OEG=
PANC-1 MW\GeY5kfGmxbjDBd5NigQ>? NI[yb4kzOCEQvF2= MX[0PEBp MlGxbY5pcWKrdIOgeIhmKGW6cILld5Nqd25ib3[g{rQ3TCCrbjDy[ZNxd26|ZTD0c{B1cGViUGDBVu61yqCjZ3;ubZN1yqB? NXr0dWEyOjR{OUSxN|M>
A549 MomySpVv[3Srb36gRZN{[Xl? NYD5WGZUOzBizszN NIG1UlYxNjViaB?= NHHxepdFVVOR MY\pcohq[mm2czD0bIUhfGi{b33ibY4ucW6mdXPl[EBKVC16L1PYR2w5NUy3YzDhZ5Rqfmm2eR?= MYeyOFI4PzZ7Nh?=
A549 NXe1VGQ3TnWwY4Tpc44hSXO|YYm= MnXjN|Ah|ryP M17xOFAvPSCq MYfEUXNQ NEjSfZdqdmirYnn0d{B1cHKxbXLpck1qdmS3Y3XkJGMwTUKSzsKgWIhzOjN3wrDwbI9{eGixconsZZRqd25? NF7QbJMzPDJ5N{[5Oi=>
MC-3 M2jPNmFxd3C2b4Ppd{BCe3OjeR?= NV3GeGc3OTBizszN MlH3NlQhcA>? NX7nRXN2eG:2ZX70bYF1\WRiTVXTR{1qdmS3Y3XkJIFxd3C2b4Ppd{BqdiBiY3XscJM> MlnJNlQzPzB3MkO=
Raji  NWTXVXI{TnWwY4Tpc44hSXO|YYm= NVXySlRtOTBizszN NF:2VIcyKGh? MlXnZoxw[2u|IHjzRmFHTiCrbnT1Z4VlKEW{a{GvNkBxcG:|cHjvdplt[XSrb36= NFKyPJIzPDJ4OU[zNC=>
Raji  MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LDdVExKM7:TR?= M1\EflEhcA>? NUS5SJZCcW6qaXLpeJMhfGinIHLhd4FtKG:{IHjzRmFHTi2|dHnteYxifGWmIHPlcIwheHKxbHnm[ZJifGmxbjDhcoQhfmmjYnnsbZR6 NX\0W2lHOjR{Nkm2N|A>
HT29 NF2y[VNHfW6ldHnvckBCe3OjeR?= MXqxNEDPxE1? NFHGbnUzKGh? MX;pcohq[mm2czDv[kBLSUt{LDDFVmsyNzJiYX7kJHNVSVR|IIDoc5NxcG:{eXzheIlwdg>? MorLNlQzPjV{OUO=
HepG2 NWXSeG95SXCxcITvd4l{KEG|c3H5 NHr5UZkzOCEQvF2= NF;VVYkzPCCq NFy3XHJqdmirYnn0d{BGWktzL{KgdIhwe3Cqb4L5cIF1cW:wIHHu[EBmdmijbnPld{BXSjFvaX7keYNm\CCjcH;weI9{cXN? Ml[xNlQzPDd7MEm=
HepG2 MljZSpVv[3Srb36gRZN{[Xl? MYGyNEDPxE1? MUKyJIg> M3vkN4VvcGGwY3XzJHZDOS2rbnT1Z4VlKE[RWF:zZUB1emGwc3PybZB1cW:wYXygZYN1cX[rdIm= Mn;pNlQzPDd7MEm=
TE4 MUXGeY5kfGmxbjDBd5NigQ>? MWGyNE82OC9zMECg{txO MXq0PEBp NIC3eppFVVOR Mn;JbY5pcWKrdIOgdE1GemtiYX7kJJdwenSvYX7ubY4h\G:5boLl[5Vt[XSnZDDwMWFsfCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M13jUFI1OjR2MEKz
TE1 MlfJSpVv[3Srb36gRZN{[Xl? MVWyNE82OC9zMECg{txO NWHB[IE5PDhiaB?= MlrmSG1UVw>? Mne3bY5pcWKrdIOgdE1GemtiYX7kJJdwenSvYX7ubY4h\G:5boLl[5Vt[XSnZDDwMWFsfCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? Ml\qNlQzPDRyMkO=
KYSE30 M{fmU2Z2dmO2aX;uJGF{e2G7 M1q3cVIxNzVyL{GwNEDPxE1? NI\6SIU1QCCq NIHDVJRFVVOR M{nROIlvcGmkaYTzJJAuTXKtIHHu[EB4d3K2bXHucolvKGSxd37y[Yd2dGG2ZXSgdE1Cc3RiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MYCyOFI1PDB{Mx?=
TE1 MWHGeY5kfGmxbjDBd5NigQ>? NF;vTlM2OCEQvF2= NIDnN5k1QCCq NEP0SlRFVVOR NF3OS4V2eHKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCKTFGgZ4xie3NiSR?= NEW4SmgzPDJ2NECyNy=>
TE3 NUL6NoVsTnWwY4Tpc44hSXO|YYm= NUfLSoRTPTBizszN NWG4No9kPDhiaB?= MmS3SG1UVw>? MYD1dJJm\3WuYYTld{B1cGViZYjwdoV{e2mxbjDv[kBJVEFiY3zhd5MhUQ>? MmPpNlQzPDRyMkO=
TE4 M4jaWGZ2dmO2aX;uJGF{e2G7 MVq1NEDPxE1? NFvtdlY1QCCq MUXEUXNQ MlXMeZBz\We3bHH0[ZMhfGinIHX4dJJme3Orb36gc4YhUEyDIHPsZZN{KEl? M33TNlI1OjR2MEKz
TE5 M1nteGZ2dmO2aX;uJGF{e2G7 Mn7sOVAh|ryP M4T3RlQ5KGh? NHXnZm5FVVOR MlrYeZBz\We3bHH0[ZMhfGinIHX4dJJme3Orb36gc4YhUEyDIHPsZZN{KEl? M{\XNFI1OjR2MEKz
KYSE30 MlfYSpVv[3Srb36gRZN{[Xl? NVezU2h7PTBizszN MnTROFghcA>? NGraTHZFVVOR NEfzdm92eHKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCKTFGgZ4xie3NiSR?= NEDJXYwzPDJ2NECyNy=>
MKN7 NXXUSnhVTnWwY4Tpc44hSXO|YYm= MWK1NEDPxE1? MofJOFghcA>? NWThZVBnTE2VTx?= NGDRZ3FqdmO{ZXHz[ZMh\XiycnXzd4lwdiCxZjDIUGEuSTB{IH;yJGhNSS2DMkSgcY9t\WO3bHXz M1fLdlI1OjR2MEKz
OE19 NULTTGVOTnWwY4Tpc44hSXO|YYm= NFrGNlU2OCEQvF2= NWC4bItUPDhiaB?= M3jaS2ROW09? NWXrXFVCcW6lcnXhd4V{KGW6cILld5Nqd25ib3[gTGxCNUFyMjDvdkBJVEFvQUK0JI1wdGWldXzldy=> NWrpTHdoOjR{NESwNlM>
KATOIII  NXjPVlhjTnWwY4Tpc44hSXO|YYm= NXn6N29LPTBizszN M1rR[lQ5KGh? NUPadXUxTE2VTx?= M{\1dIlv[3KnYYPld{BmgHC{ZYPzbY9vKG:oIFjMRU1CODJib4KgTGxCNUF{NDDtc4xm[3WuZYO= MWGyOFI1PDB{Mx?=
NCI-N87  NH7DTHFHfW6ldHnvckBCe3OjeR?= M4r4b|UxKM7:TR?= NFn3PVg1QCCq MWXEUXNQ MWnpcoNz\WG|ZYOg[ZhxemW|c3nvckBw\iCKTFGtRVAzKG:{IFjMRU1COjRibX;s[YN2dGW| M2nPb|I1OjR2MEKz
NUGC3 M1rpPGZ2dmO2aX;uJGF{e2G7 MlrqOVAh|ryP NV2xd|NDPDhiaB?= MWnEUXNQ M2DKRYlv[3KnYYPld{BmgHC{ZYPzbY9vKG:oIFjMRU1CODJib4KgTGxCNUF{NDDtc4xm[3WuZYO= NHrVV3EzPDJ2NECyNy=>
NUGC2 NX\5W2FbTnWwY4Tpc44hSXO|YYm= Ml[2OVAh|ryP NV3CdWdXPDhiaB?= MnvVSG1UVw>? NXTPNYY{cW6lcnXhd4V{KGW6cILld5Nqd25ib3[gTGxCNUFyMjDvdkBJVEFvQUK0JI1wdGWldXzldy=> MX6yOFI1PDB{Mx?=
SGC-7901  M1TkUmFxd3C2b4Ppd{BCe3OjeR?= M1vqW|IxKM7:TR?= MX2yOEBp M1vQZYlvcGmkaYTzJGNRNW2nZHnheIVlKGGyb4D0c5Nqew>? NUfEfGN[OjR{NEGzOVE>
MG-63 NH;rfZNHfW6ldHnvckBCe3OjeR?= MWSyNEDPxE1? NX3xZXBVOC53IHi= NYP4[VMz[myxY3vzJJRp\SCFSD3pcoR2[2WmIIDoc5NxcG:{eXzheIVlKEWOS{GgdJJwfGWrbjDlfJBz\XO|aX;u M1rTe|I1OjN7NkSw
ARPE-19 NYnYdYZ[TnWwY4Tpc44hSXO|YYm= M2HReVIxKM7:TR?= MYqwMlUhcA>? MlLYbY5pcWKrdIOgRZBmdGmwLXnu[JVk\WRicHjvd5Bpd3K7bHH0bY9vKG:oIFXyb{BidmRiQXv0 MYOyOFIzPzlzOB?=
CRL-2302 MYDGeY5kfGmxbjDBd5NigQ>? M4CyT|IxKM7:TR?= NGjjb2IxNjViaB?= MnLwbY5pcWKrdIOgRZBmdGmwLXnu[JVk\WRicHjvd5Bpd3K7bHH0bY9vKG:oIFXyb{BidmRiQXv0 NYK5V403OjR{Mke5NVg>
MCF-7 MXXGeY5kfGmxbjDBd5NigQ>? NYnNW2JtOjBizszN M1m3T|EhcA>? NWHSSVBy[WKxbHnzbIV{KGW6cILld5Nqd25ib3[gdIhwe3Cqb4L5cIF1\WRiRWLLJINwNXS{ZXH0cYVvfCC5aYToJINwdmq3Z3H0[S=> NWC5OmFQOjR{MU[yPFk>
MCF-7 NGfGeGtCeG:ydH;zbZMhSXO|YYm= M{PaNVIxKM7:TR?= NV:1VYVEOSCq M2HUU4lv[3KnYYPld{Bk[XOyYYPlMVkh\W68eX3lJIFkfGm4aYT5 NVnXOZhVOjR{MU[yPFk>
DLD-1  M2n2[mZ2dmO2aX;uJGF{e2G7 NXTxUJJ1OjEEoN88US=> Mk\XOFghcA>? MYTy[YR2[2W|IITo[UBDVkmSMzDlfJBz\XO|aX;uJJBz\S22cnXheIVlKHerdHigOU1igmFvZFO= MmC2NlQzOTF3OEG=
HT-29 NX;F[HlqTnWwY4Tpc44hSXO|YYm= MlTxNlDDqM7:TR?= M3GzbVQ5KGh? M2DTWZJm\HWlZYOgeIhmKEKQSWCzJIV5eHKnc4Ppc44heHKnLYTy[YF1\WRid3n0bEA2NWG8YT3kRy=> NVK5bG5JOjR{MUG1PFE>
7402 M3W0NmFxd3C2b4Ppd{BCe3OjeR?= MUCzNEDPxE1? NXLqUIg4PSCm NWP6NGxC\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdg>? NGDmPVYzPDJzMUK1Ny=>
7721 NGfmNGhCeG:ydH;zbZMhSXO|YYm= MYCzNEDPxE1? NV7Gcm93PSCm NUnLVWNP\GWlcnXhd4V{KGOnbHygdJJwdGmoZYLheIlwdg>? MYOyOFIyOTJ3Mx?=
SGC7901  NXTsdINjSXCxcITvd4l{KEG|c3H5 M{Tse|UxyqEQvF2= NWjRblhoOjRxNEivO|IhcA>? NXfZVIFtTE2VTx?= M2Cx[4lv\HWlZYOgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiSlHLNkB{cFKQQR?= NXTMS3VjOjRzN{iyOFA>
SMMC7721 NV33e45bTnWwY4Tpc44hSXO|YYm= NHzZTlAzPS93MDFOwG0> NWLveIJCOjRiaB?= MnHMd5VxeHKnc4Pld{B1cGViZYjwdoV{e2mxbjDv[kBxNUGtdDDvdkBxNUWUS{GvNuKh NFj1NIwzPDF4OEC1Oi=>
MCF-7 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnCNVAh|ryP MX60PIg> Mn\TSG1UVw>? NWLObFhVemW4ZYLz[ZMhSk6ILXnu[JVk\WRiY3XscEBkgWOuZTDhdpJme3R? MWCyOFE3OzRyNB?=
Caco-2 MVfGeY5kfGmxbjDBd5NigQ>? MU[1NOKh|ryP NH7UOVc1QGh? MVfEUXNQ MVflcohidmOnczD0bIUhdVKQQTDs[ZZmdHNib3dCpHNEVk5zQTzGXHlFOy{EoFzDWEzDqEyRWD|CpGhKTjODLNMgXmcyPi{EoGDESVZCyqCjbnVCpGxISUyVMUdCpIdmdmW|wrDjc{11emWjdHXkJJdqfGhiRHX4 NVHyPJFWOjRzNkG2PVU>
HAECs M1\aT2Z2dmO2aX;uJGF{e2G7 MmLLNVAh|ryP M1L0TlEhcA>? MX9CpIF1fGWwdXH0[ZMhXE6ILd8xMZN1cW23bHH0[YQhUUODTT2xJIFv\CCYQ1HNMVEh\XiycnXzd4lwdg>? MViyOFE{PDZ3Nx?=
Ca9-22 M3Ts[GZ2dmO2aX;uJGF{e2G7 M4nUNVMh|ryP NXS4VYJGOSCq MmPZZYJwdGm|aHXzJJRp\SCjYnnsbZR6KG:oIFjiVkB1dyCrbnT1Z4UhUUxvODDwdo9lfWO2aX;u MXKyOFEzPjV|Mh?=
Ca9-22 NVr6SXA2TnWwY4Tpc44hSXO|YYm= MWqzJO69VQ>? MojaNU8zKGh? M3LkWJJm\HWlZYOgTIJTNWmwZIXj[YQhSVSILUKgdIhwe3Cqb4L5cIF1cW:w MWeyOFEzPjV|Mh?=
AGS M{PF[mZ2dmO2aX;uJGF{e2G7 MXGxNEDPxE4EoB?= Mk\1NE42KGh? M4G4cYlvcGmkaYTzJJRp\SC3cILl[5Vt[XSrb36gc4YhfGinIFnMMVgh\2WwZR?= NHzUSmszPDFyNkG2Oi=>
Caco-2  NIDoPYVCeG:ydH;zbZMhSXO|YYm= MkKyNVDDqM7:TR?= MlrFNlTDqGh? NUnHfJVO\GWlcnXhd4V{KGOnbHygZZBweHSxc3nzJIlv\HWlZXSgZpkhPS2IVR?= NEO4OGIzPDB7NUi2Ny=>
HCT-8 M4rsfGFxd3C2b4Ppd{BCe3OjeR?= M4PVflExyqEQvF2= MUWyOOKhcA>? Mkfk[IVkemWjc3XzJINmdGxiYYDvdJRwe2m|IHnu[JVk\WRiYomgOU1HXQ>? NVO4fY14OjRyOUW4OlM>
A549 NEjs[GtHfW6ldHnvckBCe3OjeR?= MUK1NOKh|ryP M{LGPVIhcA>? M2C2ToJtd2OtczDFVmsheGixc4Doc5J6dGG2aX;uJI1m\GmjdHXkJIJ6KDFuMj3OVS=> MojINlQxPjd5Mke=
HPMC MXPGeY5kfGmxbjDBd5NigQ>? MV[xNOKh|ryP MVW0PEBp MmTGdoV3\XK|ZYOgeIhmKGOqYX7n[ZMhcW5iY3XscEBud3KyaH;sc4d6KGmwZIXj[YQh[nliSFfQSHM> MWeyOFA1Ojh|OB?=
HPMC MnH1RZBweHSxc3nzJGF{e2G7 NXXLNnlOOTEEoN88US=> MV[yOOKhcA>? NW\zZ3VPemW4ZYLz[ZMh\GWlcnXhd4UhcW5iY3XscEB3cWGkaXzpeJkhcW6mdXPl[EBjgSCKR2DEVy=> NXXYVIpNOjRyNEK4N|g>
MGC803  Mn7iRZBweHSxc3nzJGF{e2G7 MojFNlDDqM7:TR?= MYqxJIg> NVT1cmd6cW6qaXLpeJMh[XCxcITvd4l{KGmwZIXj[YQh[nliSV\OMe6yyqCjbnSgOgKBui2GRmXS MYOyOFAzPzd3MB?=
SGC7901 NFvVZWhCeG:ydH;zbZMhSXO|YYm= NYPkdXk3OjEEoN88US=> MlLQNUBp NX3YUGR{cW6qaXLpeJMh[XCxcITvd4l{KGmwZIXj[YQh[nliSV\OMe6yyqCjbnSgOgKBui2GRmXS Mnq4NlQxOjd5NUC=
COLO205 NI\lNlVCeG:ydH;zbZMhSXO|YYm= MkLyNVAwOjBxNECg{txO MYKyOEBp M{nEPIlv\HWlZYOgSG5CKGyjZHTldkBnd3KvYYTpc44> M1voTFI1ODF7MUC4
G292  NVfIRZBQSXCxcITvd4l{KEG|c3H5 MUmzNOKh|ryP NWHnSmJ5OiCq M3PrWZJme3SxcnXzJINieHOjaXPpck1qdmS3Y3XkJINmdGxiZHXheIg> Mm\1NlQxOTJ7M{C=
BxPC-3 Mo\WSpVv[3Srb36gRZN{[Xl? NYOzb4I4OTBizszNxsA> MoPQOkBp M2G3cYlv[3KnYYPlJI1qWi1zNEOg[ZhxemW|c3nvci=> MmHjNlM6PzN5MUC=
HPAF-II NFjUdYxHfW6ldHnvckBCe3OjeR?= NED3W|gyOCEQvF5CpC=> Mor2OkBp MX\pcoNz\WG|ZTDtbXIuOTR|IHX4dJJme3Orb36= NFPnW5YzOzl5M{exNC=>
HL-60 M3jkNGFxd3C2b4Ppd{BCe3OjeR?= NF7ZZZM2OMLizszN Ml7RNUBp NFrxTHFz\XOldXXzJGJCOTR3IH3l[IlifGWmIHHwc5B1d3Orcx?= M1PkclI{QTR6N{Wx
HepG2 Mor0SpVv[3Srb36gRZN{[Xl? NEfuNIY1OCEQvF2= NHrSd|U3NzF{IHi= MnjUbY5pcWKrdIOgeIhmKGmwY4LlZZNmKG:oIICtSXJMOSCjbnSgdE1kNUq3bjDwdo91\WmwIHX4dJJme3Orb36gZpkhWEx? NYj2WFV{OjN7NEK4OVE>
HUVECs NGr1SWdHfW6ldHnvckBCe3OjeR?= MmK2NlUh|ryP NEn5fnYyKGh? NGTLN2JqdmO{ZXHz[UBPTi4QulKgdFY2KG63Y3zlZZIhfHKjboPsc4NifGmxbh?= M{fN[|I{QTBzMEC4
LNCaP  NHXtT4FHfW6ldHnvckBCe3OjeR?= MmLZNVAh|ryPwrC= Ml3xNUBp M4q4b4Rm[3KnYYPld{B1cGViRVfGJJVxemWpdXzheIVlKHBvWVKtNS=> MlrLNlM5Ozh|MUi=
HL60  M{i0cWZ2dmO2aX;uJGF{e2G7 NFOzV5EzOMLizszN NEDmSJY4OiCq M3rIfWROW09? Mo\DbY5pcWKrdIOg[IF{[XSrbnniMYlv\HWlZXSgR2QyOWJiZYjwdoV{e2mxbh?= NF3hZXkzOzh{NUW4OS=>
NB4  MX;GeY5kfGmxbjDBd5NigQ>? M4jP[|ExKM7:TdMg NW\0ToU1PzJiaB?= NFrpcW1FVVOR NHrZSFZqdmirYnn0d{Bl[XOjdHnubYIucW6mdXPl[EBETDFzYjDlfJBz\XO|aX;u NH65Z2ozOzh{NUW4OS=>
EPOR/CR3 NUnYVogzTnWwY4Tpc44hSXO|YYm= Ml25OVDDqM7:TR?= MUSzJIg> NVqyRpJRemWmdXPld{BGWE9iYX7kM49zKEmOLUOtbY5lfWOnZDD0bIUhfHm{b4PpcoUheGixc4Doc5J6dGG2aX;uxsA> NUjF[ppJOjN6MkC3N|E>
HUASMCs NV\ZSJltTnWwY4Tpc44hSXO|YYm= Ml\HNVAh|ryPwrC= NHnzfGQzPCCq M1j6U4RqdWmwaYPo[ZMhSW6pIFnJMYNifXOnZDDTU2NUOyCvUl7BJIFv\CCycn;0[YlvKGW6cILld5Nqd28EoB?= MVWyN|gyPjR4OB?=
HUASMCs M3q2VmZ2dmO2aX;uJGF{e2G7 NVPSZnB2OTBizszNxsA> M4nOdFI1KGh? MVLpcohq[mm2czDBcochUUlvaX7keYNm\CCHUluxM|IheGixc4Doc5J6dGG2aX;uJIxmfmWu NEDxcVgzOzhzNkS2PC=>
SGC7901 MULGeY5kfGmxbjDBd5NigQ>? MUmxNEDPxE4EoB?= MUCyOEBp NX7wdFFwcW6qaXLpeJMhfGinIHX4dJJme3Orb36gc4YheGixc4Doc5J6dGG2ZXSgSXJMOS9{ NHPYNYEzOzd7MkW4PC=>
MKN45 MnroSpVv[3Srb36gRZN{[Xl? MVixNEDPxE4EoB?= Mn\VNlQhcA>? M4OxTYlvcGmkaYTzJJRp\SCneIDy[ZN{cW:wIH;mJJBpd3OyaH;yfYxifGWmIFXST|EwOg>? MlnONlM4QTJ3OEi=
SGC7901 MkTmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVKxNEDPxE4EoB?= NWn1cWFJOjRxNEivO|IhcA>? M2jBWYlvcGmkaYTzJINmdGxiZ4Lve5RpKGOxLYTy[YF1\WRid3n0bEBFSVCW NF3Mdm4zOzd7MkW4PC=>
MKN45 NFfRbo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGC0eVQyOCEQvF5CpC=> NX\oeoo5OjRxNEivO|IhcA>? M4TEdolvcGmkaYTzJINmdGxiZ4Lve5RpKGOxLYTy[YF1\WRid3n0bEBFSVCW NHrOd|kzOzd7MkW4PC=>
SGC7901 MX7BdI9xfG:|aYOgRZN{[Xl? NYTKfG5EOTBizszNxsA> MVGyOEBp M1f2Z4lv[3KnYYPld{B1cGViRFHQWE1qdmS3Y3XkJINmdGxiYYDvdJRwe2m| MoTHNlM4QTJ3OEi=
MKN45 MWTBdI9xfG:|aYOgRZN{[Xl? NXzXfYVyOTBizszNxsA> M1jn[VI1KGh? MoP6bY5kemWjc3XzJJRp\SCGQWDUMYlv\HWlZXSgZ4VtdCCjcH;weI9{cXN? NEjNSo0zOzd7MkW4PC=>
BxPC-3 cells M2fsPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLWNlDDqM7:TR?= M3ex[FAvPSCq Mn\sbY5pcWKrdIOgWmVITi2DLYLl[5Vt[XSnZDDIWXZGSyCpcn;3eIgh[W6mIIT1ZoUh\m:{bXH0bY9vKGmwZIXj[YQh[nliUFHSMVIhSVB? NUjVW3p{OjN5NkSwOFY>
NB4  NYjqbWlMSXCxcITvd4l{KEG|c3H5 M2q0VFExNzJyL{[wJO69VQ>? MnzYNU42KGh? NULoTJBDTE2VTx?= M1T4eIRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDjc{11emWjdHXkJJdqfGhiUHHjcIl1[XinbB?= M2LhOFI{PzN3NUSx
HepG2  MVrGeY5kfGmxbjDBd5NigQ>? M3W2WVIxyqEQvF2= MljtNlQhcA>? MlPGbY5pcWKrdIOgeIhmKEiRLUGgdJJwfGWrbjDlfJBz\XO|aX;uJINwNXS{ZXH0[YQhf2m2aDDt[ZRnd3KvaX6= NYqzOZNGOjN5MEe2NFk>
HUVECs NXzUU4tqSXCxcITvd4l{KEG|c3H5 Mo\jNk81KM7:TR?= MkfYNlQwPDhiaB?= MnTxbY5lfWOnczDj[YxtKGSnYYTo NYP5RndXOjN5MEe1NlA>
KG-1  M2LM[2Fxd3C2b4Ppd{BCe3OjeR?= MnfKNlDDqM7:TR?= MnTBNVIhcA>? M2DadoVvcGGwY3XzJINmdGxiYYDvdJRwe2m|IHnu[JVk\WRiYomgV|E> MXiyN|cxPjZ7MR?=
AML 1# NEm5c2FCeG:ydH;zbZMhSXO|YYm= MXeyNOKh|ryP MUmxNkBp MnrB[Y5p[W6lZYOgZ4VtdCCjcH;weI9{cXNiaX7keYNm\CCkeTDTNS=> NH;TcWMzOzdyNk[5NS=>
A2780  M3L5PWZ2dmO2aX;uJGF{e2G7 MX2yNOKh|ryP NVm0PZg6OSCq NH7nW2NjdG:la4OgSHRETC2rbnT1Z4VlKESUNTDlfJBz\XO|aX;u MV:yN|Y6Pjh4Mh?=

... 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
  • 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=CC=CC(=C1N)C2=CC(=O)C3=CC=CC=C3O2

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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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

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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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