PD98059

For research use only.

Catalog No.S1177

299 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 299 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 MVnGeY5kfGmxbjDBd5NigQ>? NHXKdHAzPSEQvF2= MlfJNUBp NH\JfZRjdHWwdIOgeIhmKEKdYW3QMYlv\HWlZXSgbY5kemWjc3WgbY4heGixc4Doc{1EcGtzIHHu[EBxcG:|cHjvMWVTUyCneIDy[ZN{cW:w MlrxNlU4PjlzOEG=
MCF-7  Mly1SpVv[3Srb36gRZN{[Xl? M4j2WFExKM7:TR?= M2exelEhcA>? MVvpcohq[mm2czDJUE0yQC2nbnjhcoNm\CClZXzsJI1q\3KjdHnvci=> NYLLWldIOjV5MkewNVE>
HepG2  NGOz[25HfW6ldHnvckBCe3OjeR?= M{Wwb|ExKM7:TR?= MoTBOUBp M3vEbYJtd2OtczDwbI9{eGixconsZZRm\CCPQWDLd{BqdmS3Y3XkJIJ6KGW6b3flco92eyCWR1[t{tIy NYHMN3B{OjV3NkC0PFg>
HepG2  MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHDNlAh|ryP NUW5ZYNzOjRiaB?= M1i2fJN2eHC{ZYPz[ZMhXEeILd8yNU1qdmS3Y3XkJINmdGxicILvcIln\XKjdHnvckBidmRiaX72ZZNqd25? NVjTS5VDOjV3NkC0PFg>
MDA-MB-231 NHnZUZVHfW6ldHnvckBCe3OjeR?= NFzFTVAzPSEQvF2= NIDKOG4zNTNiaB?= NHvkVINl\WO{ZXHz[ZMheC2HUluxM|Ih[W6mIGOxNFBCPCCneIDy[ZN{cW:w NV\mTmpoOjV3NUW4O|U>
SW480 M1zOemZ2dmO2aX;uJGF{e2G7 M2rXVVIxyqEQvF2= NFnHfowyyqCq NWXSeZhkemWmdXPld{B1cGViZYjwdoV{e2mxbjDv[kBCXEZ|IIDyc5RmcW5? NVjSRoc{OjV2NEe4NVY>
HCT-15 M4jWfGZ2dmO2aX;uJGF{e2G7 NHTs[o4yKGh? NUXpSXZS[XS2ZX71ZZRmeyCSR1WyMYlv\HWlZXSgdIhwe3Cqb4L5cIF1cW:wIH;mJGVzc8Li NW\WR5k6OjV2M{G0NlU>
HCT-15 M3\5bGFxd3C2b4Ppd{BCe3OjeR?= NX21UGxCOSCq MYPhZo9tcXOqZYOgeIhmKHC{b4TlZ5RqfmViZX\m[YN1eyCxZjDQS2UzyqCjZ3HpcpN1KGO3cnP1cYlvNWmwZIXj[YQh[XCxcITvd4l{ MXSyOVQ{OTR{NR?=
786-O MkXoRZBweHSxc3nzJGF{e2G7 M3HrS|UxyqEQvF2= NHXU[VczPCCq MknMdI91\W62aXH0[ZPDqHSqZTDwdo8u[XCxcITveIlkKGWoZnXjeJMhd2ZiTlO= MlnTNlQ2ODh2N{[=
A498 MlzCRZBweHSxc3nzJGF{e2G7 MXW1NOKh|ryP NXTQ[mZvOjRiaB?= NXnBWXZYeG:2ZX70bYF1\XQEoITo[UBxem9vYYDvdJRwfGmlIHXm[oVkfHNib3[gUmM> NV\KTZJDOjR3MEi0O|Y>
NHBE NWLVUIw3TnWwY4Tpc44hSXO|YYm= MnfENk8zOCEQvF2= NEnPRm4zKGh? NFP3SotifHSnboXheIV{KEmOLUOzJJN1cW23bHH0[YQhS1iFTEivTWwuQCC|ZXPy[ZRqd25? M1TOblI1PDd7NUK2
A375 M3v6NGNmdGxiSX72ZZNqd25iQYPzZZk> MVOxNQKBmzJyINM1US=> M33DSVI1KGh? Moj3doVlfWOnczDt[Yxidm:vYTDj[YxtKGmwdnHzbY9v NU\sN3h4OjR2Nk[wN|Y>
HBMEC NVv5fIZkTnWwY4Tpc44hSXO|YYm= MXGxNEDPxE1? MmDnNUBp M{jQboJtd2OtczDWSWdHNWmwZIXj[YQhTXCqQUKg[ZhxemW|c3nvci=> NWDjbW5sOjR2NUi5PFI>
HPAEpiCs  M4GwSWZ2dmO2aX;uJGF{e2G7 MlrKN|Ah|ryP M1vkeFEhcA>? MVrpcohq[mm2czDUUmYu|rFic4TpcZVt[XSnZDDwOFIweDR2IF3BVGsheGixc4Doc5J6dGG2aX;u Mn7tNlQ1PDF6N{C=
BeWo M1j3S2Z2dmO2aX;uJGF{e2G7 MlPyNVDDqM7:TR?= M3rBdVIhcA>? M3r0PYlvcGmkaYTzJGVTUzFxMh?= NGfZeXkzPDR|M{i0Oi=>
PC3  MUHBdI9xfG:|aYOgRZN{[Xl? NFnkNmQ2OCEQvF2= NEXMdZcxNjViaB?= NGXKenBqdmirYnn0d{BOUFlvNES5MYlv\HWlZXSgZZBweHSxc3nzxsA> MmjiNlQ1OjR6OEm=
HGC-27 MnrLRZBweHSxc3nzJGF{e2G7 MWixJOK2VQ>? MV2xJIg> MlHzd5VxeHKnc4Pld{BTSURyMEGgdIx2eyCPSz2yNlA3NWmwZIXj[YQh[2WubDD2bYFjcWyrdImgcI9{ew>? NYm3dIdUOjR2MU[zOFk>
MCF-7 MYnGeY5kfGmxbjDBd5NigQ>? M2PGTlExyqEQvF2= MmHBNVAwOzBibXnu Mnn1doVlfWOnczD0bIUhXVSSLXTldIVv\GWwdDDFVmsheGixc4Doc5J6dGG2aX;u M3nJZlI1OzlyOEG5
HUVECs NXr6T3dWTnWwY4Tpc44hSXO|YYm= NEHQVJkyOMLizszN M3TTflEhcA>? Ml\nbY5pcWKrdIOgeIhmKEiGTDDy[YR2[2WmIFPPXE0zKGW6cILld5Nqd25iYX7kJHBIUS1{IILlcIVie2V? NX;uXoFxOjR|OEWxNFk>
HeLa MYrGeY5kfGmxbjDBd5NigQ>? MkHiOVAh|ryP MonNNE42KGh? MkK5Zoxw[2u|IGTSXE0yKG63Y3zlZZIhdWmpcnH0bY9vKGGwZDDUXG5KWCCmb4fuMZJm\3WuYYTpc44> NF3kWmszPDN5NkiyOy=>
HL-60  NWDPNWpZTnWwY4Tpc44hSXO|YYm= MYKxNE8zOCEQvF2= M1;QRlEhcA>? M3XuXolvcGmkaYTzJJRp\cLiTj6gZ4hqdmWwc3nz[Zh1emGldNMgbY5lfWOnZDDkbYZn\XKnboTpZZRqd25iaX70c{BoemGwdXzvZ5l1\XN? NWPpfFllOjR|NUewNlA>
HL-60 NILQOFZHfW6ldHnvckBCe3OjeR?= M3K0fFIhyrWP Ml;zNVYhcA>? NH;VNpNFVVOR Ml[1bY5pcWKrdIOgeIhmKGG|c3;jbYF1cW:wIH;mJJBUPjJzIGLh[k0yKGGwZDDOSmFV[zNuIHHu[EB1cGViUlGtbY5lfWOnZDDwbI9{eGixconsZZRqd25ib3[gcpVkdGWjcjDOSmFV[zN? M4HnUVI1OzNyME[4
HEK 293 M1Tlb2Z2dmO2aX;uJGF{e2G7 MlfVNVAh|ryP MV61JIg> NFm2NFZFVVOR NYPmT|dncW6qaXLpeJMhX262LXnu[JVk\WRizsKtZ4F1\W6rbj;UR2Y1KGGldHn2bZR6KGGwZDDueYNt\WG{IN8yMYNifGWwaX6gZYNkfW23bHH0bY9v NEHiTYIzPDN{NEO2Oi=>
HEK 293 NF;lPYlHfW6ldHnvckBCe3OjeR?= M{TEPVExKM7:TR?= MojnOUBp Mk\TSG1UVw>? M3XYOpN2eHC{ZYPz[ZMhfGinIFPSWEBi[3Srdnn0fS=> M2L6XFI1OzJ2M{[2
SW480 MXnGeY5kfGmxbjDBd5NigQ>? NVf5[nFROTBizszN MVqyNEBp M3m5[GROW09? M{TDPZN2eHC{ZYPz[ZMhfGinIFPSWEBi[3Srdnn0fS=> NGPS[5AzPDN{NEO2Oi=>
HCSMCs M2j2Rmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nWUFExKM7:TR?= MUeyOEBp Mo\EZoxw[2u|IF\BRnA1NWmwZIXj[YQhUEODU13DJJBzd2yrZnXyZZRqd25? M1zLfVI1OzF{M{ix
PANC-1 M37XV2Z2dmO2aX;uJGF{e2G7 MmjVNlAh|ryP NYfnZW5jPDhiaB?= NH:2UVBqdmirYnn0d{B1cGViZYjwdoV{e2mxbjDv[kDPnD[GIHnuJJJme3CxboPlJJRwKHSqZTDQVGFT|rUEoHHnc45qe3UEoB?= NVv4ZoE5OjR{OUSxN|M>
A549 M3ixXGZ2dmO2aX;uJGF{e2G7 MXKzNEDPxE1? NVm2Z45FOC53IHi= MmfFSG1UVw>? NXGyWYE6cW6qaXLpeJMhfGinIITodo9u[mmwLXnu[JVk\WRiSVytPE9EYEOOOD3MeYMh[WO2aY\peJk> MVyyOFI4PzZ7Nh?=
A549 NEP1dIRHfW6ldHnvckBCe3OjeR?= NILkZ5g{OCEQvF2= NYKyWoJIOC53IHi= NH[xZ2lFVVOR M4\qdYlvcGmkaYTzJJRpem:vYnnuMYlv\HWlZXSgR{9GSlEQsjDUbJIzOzYEoIDoc5NxcG:{eXzheIlwdg>? M1K3UVI1Ojd5Nkm2
MC-3 NHrvUYRCeG:ydH;zbZMhSXO|YYm= M{LFOFExKM7:TR?= MYeyOEBp NXvmVIVoeG:2ZX70bYF1\WRiTVXTR{1qdmS3Y3XkJIFxd3C2b4Ppd{BqdiBiY3XscJM> NFTkNoEzPDJ5MEWyNy=>
Raji  M{nZ[mZ2dmO2aX;uJGF{e2G7 NFHMWmQyOCEQvF2= MYOxJIg> M1XacoJtd2OtczDod2JCTkZiaX7keYNm\CCHcnuxM|IheGixc4Doc5J6dGG2aX;u NYC2TXRTOjR{Nkm2N|A>
Raji  NXPlRlVuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fKSFExKM7:TR?= M3rjT|EhcA>? MkDCbY5pcWKrdIOgeIhmKGKjc3HsJI9zKGi|QlHGSk1{fGmvdXzheIVlKGOnbHygdJJwdGmoZYLheIlwdiCjbnSgeoli[mmuaYT5 MmrjNlQzPjl4M{C=
HT29 NXn4emFzTnWwY4Tpc44hSXO|YYm= NFfS[WwyOCEQvF2= NHnZNIozKGh? NYXsUGdIcW6qaXLpeJMhd2ZiSlHLNkwhTVKNMT:yJIFv\CCVVFHUN{BxcG:|cHjvdplt[XSrb36= MUGyOFI3PTJ7Mx?=
HepG2 MXXBdI9xfG:|aYOgRZN{[Xl? NHXhWoYzOCEQvF2= NYP4TpA2OjRiaB?= M3jFPYlvcGmkaYTzJGVTUzFxMjDwbI9{eGixconsZZRqd25iYX7kJIVvcGGwY3XzJHZDOS2rbnT1Z4VlKGGyb4D0c5Nqew>? NWDHV|NbOjR{NEe5NFk>
HepG2 NIHSdHlHfW6ldHnvckBCe3OjeR?= M{XsTVIxKM7:TR?= NHTLfI8zKGh? NFfRT2pmdmijbnPld{BXSjFvaX7keYNm\CCIT2jPN4EhfHKjboPjdolxfGmxbnHsJIFkfGm4aYT5 M3HUZ|I1OjR5OUC5
TE4 MXvGeY5kfGmxbjDBd5NigQ>? MkDTNlAwPTBxMUCwJO69VQ>? NWfPTlFPPDhiaB?= NW[1OIx5TE2VTx?= NYX6SFZTcW6qaXLpeJMheC2HcnugZY5lKHexcoTtZY5vcW5iZH;3cpJm\3WuYYTl[EBxNUGtdDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= M1e4NFI1OjR2MEKz
TE1 M2\YU2Z2dmO2aX;uJGF{e2G7 NV;CeIV2OjBxNUCvNVAxKM7:TR?= NEjlTGE1QCCq M1PnV2ROW09? NGXLbm1qdmirYnn0d{BxNUW{azDhcoQhf2:{dH3hco5qdiCmb4fudoVofWyjdHXkJJAuSWu2IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NYT3So5iOjR{NESwNlM>
KYSE30 NGCwOnFHfW6ldHnvckBCe3OjeR?= M1KzOVIxNzVyL{GwNEDPxE1? M3X4SlQ5KGh? NInvTo9FVVOR NFnMXXJqdmirYnn0d{BxNUW{azDhcoQhf2:{dH3hco5qdiCmb4fudoVofWyjdHXkJJAuSWu2IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ M3;nNFI1OjR2MEKz
TE1 NYrIbIxKTnWwY4Tpc44hSXO|YYm= NXjTSmp{PTBizszN NVi0SGx4PDhiaB?= NH;TN|FFVVOR NWPJdoxGfXC{ZXf1cIF1\XNidHjlJIV5eHKnc4Ppc44hd2ZiSFzBJINt[XO|IFm= MlWyNlQzPDRyMkO=
TE3 Mo\vSpVv[3Srb36gRZN{[Xl? MV61NEDPxE1? M3;tbFQ5KGh? M3TSOGROW09? M2\KO5VxemWpdXzheIV{KHSqZTDlfJBz\XO|aX;uJI9nKEiOQTDjcIF{eyCL MYWyOFI1PDB{Mx?=
TE4 Mo\BSpVv[3Srb36gRZN{[Xl? NGXw[YI2OCEQvF2= M3vjb|Q5KGh? Mlz1SG1UVw>? MmfNeZBz\We3bHH0[ZMhfGinIHX4dJJme3Orb36gc4YhUEyDIHPsZZN{KEl? M2DkSVI1OjR2MEKz
TE5 NXL5e4dCTnWwY4Tpc44hSXO|YYm= MVm1NEDPxE1? MnLrOFghcA>? M4nWdWROW09? MW\1dJJm\3WuYYTld{B1cGViZYjwdoV{e2mxbjDv[kBJVEFiY3zhd5MhUQ>? NFvMbGwzPDJ2NECyNy=>
KYSE30 M4LKe2Z2dmO2aX;uJGF{e2G7 MmrPOVAh|ryP NIHCVJA1QCCq MV7EUXNQ NYn1TnBFfXC{ZXf1cIF1\XNidHjlJIV5eHKnc4Ppc44hd2ZiSFzBJINt[XO|IFm= MYOyOFI1PDB{Mx?=
MKN7 M{\SPWZ2dmO2aX;uJGF{e2G7 MorvOVAh|ryP NGL2XZM1QCCq NUf3RY5qTE2VTx?= NInUfGxqdmO{ZXHz[ZMh\XiycnXzd4lwdiCxZjDIUGEuSTB{IH;yJGhNSS2DMkSgcY9t\WO3bHXz M3zxXFI1OjR2MEKz
OE19 Ml\LSpVv[3Srb36gRZN{[Xl? M3rnU|UxKM7:TR?= M1rSTFQ5KGh? NV\YUW1FTE2VTx?= MWnpcoNz\WG|ZYOg[ZhxemW|c3nvckBw\iCKTFGtRVAzKG:{IFjMRU1COjRibX;s[YN2dGW| MUSyOFI1PDB{Mx?=
KATOIII  NW\Uflh1TnWwY4Tpc44hSXO|YYm= NInTVGg2OCEQvF2= M13hdVQ5KGh? MVrEUXNQ NUjEVlQ6cW6lcnXhd4V{KGW6cILld5Nqd25ib3[gTGxCNUFyMjDvdkBJVEFvQUK0JI1wdGWldXzldy=> NELHW4wzPDJ2NECyNy=>
NCI-N87  NFPXd|hHfW6ldHnvckBCe3OjeR?= M3\mTVUxKM7:TR?= NF[2UYw1QCCq NFLqO|hFVVOR Ml;5bY5kemWjc3XzJIV5eHKnc4Ppc44hd2ZiSFzBMWExOiCxcjDIUGEuSTJ2IH3vcIVkfWyncx?= MWOyOFI1PDB{Mx?=
NUGC3 NEjHdpRHfW6ldHnvckBCe3OjeR?= NEXsR4o2OCEQvF2= NEDrXVc1QCCq MmDvSG1UVw>? MVTpcoNz\WG|ZYOg[ZhxemW|c3nvckBw\iCKTFGtRVAzKG:{IFjMRU1COjRibX;s[YN2dGW| NGf3dXAzPDJ2NECyNy=>
NUGC2 M1[yNmZ2dmO2aX;uJGF{e2G7 NYjNS|RMPTBizszN M4HpSFQ5KGh? NGLEXZhFVVOR MUHpcoNz\WG|ZYOg[ZhxemW|c3nvckBw\iCKTFGtRVAzKG:{IFjMRU1COjRibX;s[YN2dGW| M2rtcFI1OjR2MEKz
SGC-7901  NVzsN2JKSXCxcITvd4l{KEG|c3H5 M3;NflIxKM7:TR?= M{nC[lI1KGh? MoHWbY5pcWKrdIOgR3AudWWmaXH0[YQh[XCxcITvd4l{ MVSyOFI1OTN3MR?=
MG-63 MXfGeY5kfGmxbjDBd5NigQ>? M{jaclIxKM7:TR?= NGjNOm0xNjViaB?= NE\ZV25jdG:la4OgeIhmKEOKLXnu[JVk\WRicHjvd5Bpd3K7bHH0[YQhTUyNMTDwdo91\WmwIHX4dJJme3Orb36= NV74fJM4OjR{M{m2OFA>
ARPE-19 MmfXSpVv[3Srb36gRZN{[Xl? M1q1cFIxKM7:TR?= M2[w[FAvPSCq MknabY5pcWKrdIOgRZBmdGmwLXnu[JVk\WRicHjvd5Bpd3K7bHH0bY9vKG:oIFXyb{BidmRiQXv0 Mk[wNlQzOjd7MUi=
CRL-2302 NFTZV|FHfW6ldHnvckBCe3OjeR?= NIrFfY4zOCEQvF2= MVGwMlUhcA>? MljYbY5pcWKrdIOgRZBmdGmwLXnu[JVk\WRicHjvd5Bpd3K7bHH0bY9vKG:oIFXyb{BidmRiQXv0 M4PWNVI1OjJ5OUG4
MCF-7 NWnkN4F{TnWwY4Tpc44hSXO|YYm= MoL5NlAh|ryP NULUNIdyOSCq NIPBfVNi[m:uaYPo[ZMh\XiycnXzd4lwdiCxZjDwbI9{eGixconsZZRm\CCHUlugZ48ufHKnYYTt[Y51KHerdHigZ49vcnWpYYTl M4noOFI1OjF4Mki5
MCF-7 MWnBdI9xfG:|aYOgRZN{[Xl? MUWyNEDPxE1? M2fteFEhcA>? MVjpcoNz\WG|ZYOgZ4F{eGG|ZT25JIVvgnmvZTDhZ5Rqfmm2eR?= NYXteoRIOjR{MU[yPFk>
DLD-1  M2njeWZ2dmO2aX;uJGF{e2G7 MVeyNOKh|ryP M1fVPVQ5KGh? MXfy[YR2[2W|IITo[UBDVkmSMzDlfJBz\XO|aX;uJJBz\S22cnXheIVlKHerdHigOU1igmFvZFO= MnHjNlQzOTF3OEG=
HT-29 Mo\JSpVv[3Srb36gRZN{[Xl? M4HSclIxyqEQvF2= MkfLOFghcA>? MoDJdoVlfWOnczD0bIUhSk6LUEOg[ZhxemW|c3nvckBxemVvdILlZZRm\CC5aYToJFUu[XqjLXTD MYSyOFIyOTV6MR?=
7402 MVzBdI9xfG:|aYOgRZN{[Xl? Mme2N|Ah|ryP NXPCPGlRPSCm NFX2XHhl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9v NVnGSHBkOjR{MUGyOVM>
7721 M{nwdWFxd3C2b4Ppd{BCe3OjeR?= M4K1UVMxKM7:TR?= MofUOUBl MUTk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;u M1PpdFI1OjFzMkWz
SGC7901  MV\BdI9xfG:|aYOgRZN{[Xl? M{jhc|UxyqEQvF2= MV:yOE81QC95MjDo NHfKRnBFVVOR M4KxXYlv\HWlZYOgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiSlHLNkB{cFKQQR?= Mnj2NlQyPzh{NEC=
SMMC7721 MlHySpVv[3Srb36gRZN{[Xl? NFu4eFAzPS93MDFOwG0> NEXPNGszPCCq NEn6TYF{fXCycnXzd4V{KHSqZTDlfJBz\XO|aX;uJI9nKHBvQXv0JI9zKHBvRWLLNU8zyqB? NWPqfXBNOjRzNkiwOVY>
MCF-7 MoPqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG[0eWYyOCEQvF2= NWnSblVzPDiq NITQSIRFVVOR MoSydoV3\XK|ZYOgRm5HNWmwZIXj[YQh[2WubDDjfYNt\SCjcoLld5Q> M3TyXVI1OTZ|NEC0
Caco-2 MVjGeY5kfGmxbjDBd5NigQ>? MmDGOVDDqM7:TR?= NFfFWlQ1QGh? M{XjSmROW09? M1;DToVvcGGwY3XzJJRp\SCvUl7BJIxmfmWuczDv[uKhW0OQTkHBMGZZYUR|LNMgUGNVNMLiTF;YMOKhUEmIM1GsxsBbTzF4LNMgVGRGPkIEoHHu[OKhVEeDTGOxOuKh\2WwZYRCpINwNXS{ZXH0[YQhf2m2aDDE[Zg> NYnx[|h4OjRzNkG2PVU>
HAECs M{HaZWZ2dmO2aX;uJGF{e2G7 Mn;TNVAh|ryP MWmxJIg> Mn;VxsBifHSnboXheIV{KFSQRj5OtU1{fGmvdXzheIVlKEmFQV2tNUBidmRiVlPBUU0yKGW6cILld5Nqd25? NHrzbHAzPDF|NE[1Oy=>
Ca9-22 MXnGeY5kfGmxbjDBd5NigQ>? M376cVMh|ryP NIrkeFkyKGh? MmWyZYJwdGm|aHXzJJRp\SCjYnnsbZR6KG:oIFjiVkB1dyCrbnT1Z4UhUUxvODDwdo9lfWO2aX;u MUCyOFEzPjV|Mh?=
Ca9-22 MYLGeY5kfGmxbjDBd5NigQ>? NFXaRmo{KM7:TR?= M3rHNVEwOiCq NEXHNZBz\WS3Y3XzJGhjWi2rbnT1Z4VlKEGWRj2yJJBpd3OyaH;yfYxifGmxbh?= MXuyOFEzPjV|Mh?=
AGS MnvaSpVv[3Srb36gRZN{[Xl? M{\zS|ExKM7:TdMg M4L6[|AvPSCq NVv0TGxGcW6qaXLpeJMhfGinIIXwdoVofWyjdHnvckBw\iC2aHWgTWwuQCCpZX7l MkPjNlQyODZzNk[=
Caco-2  NFHUZmNCeG:ydH;zbZMhSXO|YYm= NVXsUWxKOTEEoN88US=> NEXrZmszPMLiaB?= MoW3[IVkemWjc3XzJINmdGxiYYDvdJRwe2m|IHnu[JVk\WRiYomgOU1HXQ>? M37ZZVI1ODl3OE[z
HCT-8 NWG0eIplSXCxcITvd4l{KEG|c3H5 Mn\2NVDDqM7:TR?= MWSyOOKhcA>? MmLv[IVkemWjc3XzJINmdGxiYYDvdJRwe2m|IHnu[JVk\WRiYomgOU1HXQ>? MnrHNlQxQTV6NkO=
A549 MV\GeY5kfGmxbjDBd5NigQ>? NVm0SXJVPTEEoN88US=> M2DIfFIhcA>? M2rsWYJtd2OtczDFVmsheGixc4Doc5J6dGG2aX;uJI1m\GmjdHXkJIJ6KDFuMj3OVS=> MV2yOFA3Pzd{Nx?=
HPMC M3LMWWZ2dmO2aX;uJGF{e2G7 M3PiT|ExyqEQvF2= NGHRPHM1QCCq NHT1dmdz\X[ncoPld{B1cGViY3jhcodmeyCrbjDj[YxtKG2xcoDoc4xw\3liaX7keYNm\CCkeTDIS3BFWw>? M3Pw[lI1ODR{OEO4
HPMC M3vHXmFxd3C2b4Ppd{BCe3OjeR?= M4TBR|ExyqEQvF2= MnHMNlTDqGh? Mn\pdoV3\XK|ZYOg[IVkemWjc3WgbY4h[2WubDD2bYFjcWyrdImgbY5lfWOnZDDifUBJT1CGUx?= NI\ZRWczPDB2MkizPC=>
MGC803  NYC1dIM{SXCxcITvd4l{KEG|c3H5 NFi1W2EzOMLizszN NUGxPI5NOSCq MkTLbY5pcWKrdIOgZZBweHSxc3nzJIlv\HWlZXSgZpkhUU[QLd8xxsBidmRiNfMAtk1FTlWU NF:5dXUzPDB{N{e1NC=>
SGC7901 MofuRZBweHSxc3nzJGF{e2G7 NHfxfXAzOMLizszN MWqxJIg> NIP3U45qdmirYnn0d{BieG:ydH;zbZMhcW6mdXPl[EBjgSCLRl6t{tHDqGGwZDC15qCzNUSIVWK= MnjDNlQxOjd5NUC=
COLO205 NFO5W49CeG:ydH;zbZMhSXO|YYm= NGHNcHkyOC9{MD:0NEDPxE1? M1qyN|I1KGh? M{DSXIlv\HWlZYOgSG5CKGyjZHTldkBnd3KvYYTpc44> NFP2boczPDBzOUGwPC=>
G292  MWPBdI9xfG:|aYOgRZN{[Xl? NFLDbmE{OMLizszN NVPsdZp3OiCq M{TZNZJme3SxcnXzJINieHOjaXPpck1qdmS3Y3XkJINmdGxiZHXheIg> M{LsWFI1ODF{OUOw
BxPC-3 MkLnSpVv[3Srb36gRZN{[Xl? M1\1NFExKM7:TdMg MV62JIg> MYXpcoNz\WG|ZTDtbXIuOTR|IHX4dJJme3Orb36= M{HFOVI{QTd|N{Gw
HPAF-II NU\BbnhsTnWwY4Tpc44hSXO|YYm= MU[xNEDPxE4EoB?= NFu4[XI3KGh? NWrCdHE3cW6lcnXhd4UhdWmULUG0N{BmgHC{ZYPzbY9v MV:yN|k4OzdzMB?=
HL-60 Mn;FRZBweHSxc3nzJGF{e2G7 NE\nWIE2OMLizszN M{THeVEhcA>? NGDNTG9z\XOldXXzJGJCOTR3IH3l[IlifGWmIHHwc5B1d3Orcx?= MX6yN|k1QDd3MR?=
HepG2 MXTGeY5kfGmxbjDBd5NigQ>? NEjiclI1OCEQvF2= MWO2M|EzKGh? MXjpcohq[mm2czD0bIUhcW6lcnXhd4Uhd2ZicD3FVmsyKGGwZDDwMYMuUnWwIIDyc5RmcW5iZYjwdoV{e2mxbjDifUBRVA>? M2nBcFI{QTR{OEWx
HUVECs M{S1[GZ2dmO2aX;uJGF{e2G7 MUeyOUDPxE1? M2PiR|EhcA>? M1XlXIlv[3KnYYPlJG5HNc78QjDwOlUhdnWlbHXhdkB1emGwc3zvZ4F1cW:w MV6yN|kxOTByOB?=
LNCaP  Mk[2SpVv[3Srb36gRZN{[Xl? MkXSNVAh|ryPwrC= NVzGOZRSOSCq NW\BV4N6\GWlcnXhd4V{KHSqZTDFS2YhfXC{ZXf1cIF1\WRicD3ZRk0y NHL3bGgzOzh|OEOxPC=>
HL60  MYPGeY5kfGmxbjDBd5NigQ>? NEjw[|EzOMLizszN NVX2WWRPPzJiaB?= M4DmVGROW09? NGK2VHZqdmirYnn0d{Bl[XOjdHnubYIucW6mdXPl[EBETDFzYjDlfJBz\XO|aX;u NECyeVAzOzh{NUW4OS=>
NB4  MnzDSpVv[3Srb36gRZN{[Xl? NGKyd|cyOCEQvF5CpC=> M1\NblczKGh? MnnJSG1UVw>? MWfpcohq[mm2czDkZZNifGmwaXKtbY5lfWOnZDDDSFEy[iCneIDy[ZN{cW:w NH7WT3EzOzh{NUW4OS=>
EPOR/CR3 M37PVWZ2dmO2aX;uJGF{e2G7 NXT0XFBmPTEEoN88US=> MVizJIg> NVH1PGpkemWmdXPld{BGWE9iYX7kM49zKEmOLUOtbY5lfWOnZDD0bIUhfHm{b4PpcoUheGixc4Doc5J6dGG2aX;uxsA> MnrFNlM5OjB5M{G=
HUASMCs MVrGeY5kfGmxbjDBd5NigQ>? MofFNVAh|ryPwrC= MoPnNlQhcA>? M{\vdYRqdWmwaYPo[ZMhSW6pIFnJMYNifXOnZDDTU2NUOyCvUl7BJIFv\CCycn;0[YlvKGW6cILld5Nqd28EoB?= Ml:1NlM5OTZ2Nki=
HUASMCs NVvnelR3TnWwY4Tpc44hSXO|YYm= NUHsU|ZqOTBizszNxsA> Mn7iNlQhcA>? NUKzfWR{cW6qaXLpeJMhSW6pIFnJMYlv\HWlZXSgSXJMOS9{IIDoc5NxcG:{eXzheIlwdiCuZY\lcC=> NIq2XlAzOzhzNkS2PC=>
SGC7901 M4jQd2Z2dmO2aX;uJGF{e2G7 M1PzTlExKM7:TdMg NIew[|gzPCCq Ml7WbY5pcWKrdIOgeIhmKGW6cILld5Nqd25ib3[gdIhwe3Cqb4L5cIF1\WRiRWLLNU8z NVzsUHZHOjN5OUK1PFg>
MKN45 NEjubmxHfW6ldHnvckBCe3OjeR?= NW\we2VVOTBizszNxsA> NGrqcJUzPCCq NUmyfmU{cW6qaXLpeJMhfGinIHX4dJJme3Orb36gc4YheGixc4Doc5J6dGG2ZXSgSXJMOS9{ NV7iN3ZzOjN5OUK1PFg>
SGC7901 NX20dII4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVqxNEDPxE4EoB?= Ml\HNlQwPDhxN{KgbC=> NXrZNmdScW6qaXLpeJMh[2WubDDndo94fGhiY3:teJJm[XSnZDD3bZRpKESDUGS= MVOyN|c6OjV6OB?=
MKN45 NYjxbGhKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{G0RVExKM7:TdMg NHXJfoUzPC92OD:3NkBp MYfpcohq[mm2czDj[YxtKGe{b4f0bEBkdy22cnXheIVlKHerdHigSGFRXA>? MnOxNlM4QTJ3OEi=
SGC7901 NH\SPZJCeG:ydH;zbZMhSXO|YYm= NUjDXIdCOTBizszNxsA> M2TkdVI1KGh? NETN[ZZqdmO{ZXHz[ZMhfGinIFTBVHQucW6mdXPl[EBk\WyuIHHwc5B1d3Orcx?= NI\jZ5EzOzd7MkW4PC=>
MKN45 MoH6RZBweHSxc3nzJGF{e2G7 M4e0d|ExKM7:TdMg MV[yOEBp MVTpcoNz\WG|ZYOgeIhmKESDUGStbY5lfWOnZDDj[YxtKGGyb4D0c5Nqew>? NWf5SG9nOjN5OUK1PFg>
BxPC-3 cells M4jTZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDKNVgzOMLizszN NUTUT|FxOC53IHi= NULBZWg1cW6qaXLpeJMhXkWJRj3BMZJm\3WuYYTl[EBJXV[HQzDndo94fGhiYX7kJJR2[mViZn;ycYF1cW:wIHnu[JVk\WRiYomgVGFTNTJiQWC= MlvkNlM4PjRyNE[=
NB4  MWHBdI9xfG:|aYOgRZN{[Xl? MWexNE8zOC94MDFOwG0> NWjDTYpGOS53IHi= Mof2SG1UVw>? NInESW5l\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgZ48ufHKnYYTl[EB4cXSqIGDhZ4xqfGG6ZXy= MV[yN|c{PTV2MR?=
HepG2  M4PsfmZ2dmO2aX;uJGF{e2G7 Mk\QNlDDqM7:TR?= MmPzNlQhcA>? MkH1bY5pcWKrdIOgeIhmKEiRLUGgdJJwfGWrbjDlfJBz\XO|aX;uJINwNXS{ZXH0[YQhf2m2aDDt[ZRnd3KvaX6= NWLHUWlQOjN5MEe2NFk>
HUVECs NIraNZJCeG:ydH;zbZMhSXO|YYm= NWXpTnVQOi92IN88US=> MVeyOE81QCCq Mn\ZbY5lfWOnczDj[YxtKGSnYYTo NX\uemZsOjN5MEe1NlA>
KG-1  NXTORphQSXCxcITvd4l{KEG|c3H5 NFvySI0zOMLizszN MV:xNkBp M2ryXYVvcGGwY3XzJINmdGxiYYDvdJRwe2m|IHnu[JVk\WRiYomgV|E> MV2yN|cxPjZ7MR?=
AML 1# MYDBdI9xfG:|aYOgRZN{[Xl? MVOyNOKh|ryP NUHVeoZlOTJiaB?= NUTmTJlr\W6qYX7j[ZMh[2WubDDhdI9xfG:|aYOgbY5lfWOnZDDifUBUOQ>? MV:yN|cxPjZ7MR?=
A2780  M{XPWGZ2dmO2aX;uJGF{e2G7 NWe3VmJ3OjEEoN88US=> NGPqNGMyKGh? NUDBZ2hU[myxY3vzJGRVS0RvaX7keYNm\CCGUkWg[ZhxemW|c3nvci=> NETGO4MzOzZ7Nki2Ni=>

... 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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    C2
    V2

* 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.

Molarity Calculator

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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