PD98059

Catalog No.S1177

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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Cited by 49 Publications

10 Customer Reviews

  • a-c, Inhibitors of BRAFV600E (PLX4032) and MEK1/2 (PD98059 or AZD6244) increase PGC1α and ID2 expression (a, b) and repress integrin expression and signalling (b, c). Cells were treated with indicated concentration of inhibitors for 6 h (a, b) or 24 h (c). d, e, PLX4032 increases the interaction between ID2 and TCF4 (d) and decreases the occupancy of TCF4 at the promoters of integrin genes (e). f–g, PGC1α and ID2 are partially required for PLX4032-mediated inhibition of invasion and metastasis. For in vitro assays (f), A375 cells were incubated with 1 μM PLX4032 for 10 h. Images represent one picture captured per membrane with the scale bar representing 200 μm. Values in a, b, e and f represent mean±s.d. of independent biological triplicates; *P<0.05 and **P<0.01 by Student's t-test  in a, b, e, f.

    Nature, 2016, 537(7620):422-427.. PD98059 purchased from Selleck.

     

    Melanoma cell viability and in vivo growth by cyclindependent kinase 2/4 inhibition. Western blot analysis for c-Jun, phosphorylated-ERK1/2 (Thr202/Tyr204) (p-ERK1/2), and total ERK1/2 protein levels was done for human melanoma cell lines treated with the BRAFV600E inhibitor GDC-0879 (1 μM), or MEK inhibitors CI-1040 (1 μM), U0126 (1 μM), and PD98059 (10 μM) for 18 hours.

    J Natl Cancer Inst 2012 104(21), 1673-9. PD98059 purchased from Selleck.

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    Melanoma cell viability and in vivo growth by cyclindependent kinase 2/4 inhibition. In vivo growth of LOXIMVI xenografts in athymic nude Foxn1nu mice is shown. Tumors were allowed to grow to a maximum volume of 250 mm3, and the mice were subsequently treated daily at the indicated dose levels with CDK2/4 inhibitors by intraperitoneal injection in combination with a BRAFV600E- or MEK-inhibitor. CDK2/4 inhibitor (CVT-313/indolocarbazole CDK4-I) treatment sensitizes tumors to GDC-0879 and CI1040.

    J Natl Cancer Inst 2012 104(21), 1673-9. PD98059 purchased from Selleck.

    effect of ERK1/2 inhibitor PD98059 (1, 5, and 10 μM) on SRP72 protein expression was evaluated on Jurkat cells stimulated with rhIL-1. The cells were harvested at 0,120, and 240 min, and the protein expression was verified by WB using antibodies against human SRP72, human SRP54 (nonphosphorylated SRP protein), and humanGAPDHas constitutive protein.Adecreased SRP72 expression at 10 μM and 240 min was found.

     

     

    J Biol Chem 2010 285, 32824-32833. PD98059 purchased from Selleck.

  • C, effect of ERK1/2 inhibitor PD98059 (1, 5, and 10 μM) was evaluated in SRP72-immunoprecipitated cell lysates. WB using anti-phosphoserine antibody showed a decreased SRP72 band when used as the inhibitor at concentrations of 1 μM at 240 min, 5 μM at 120 min, and 10 μM at 120 and 240 min (lanes 3, 5, 8, and 9). D, results were analyzed and RUA illustrated, finding significant results at 1 μM at 240 versus 0, 5 μM at 120 versus 0, and 10 μM at 120 versus 0 min.

     

     

    J Biol Chem 2010 285, 32824-32833. PD98059 purchased from Selleck.

    We used real time RT-PCR to investigate the effects of PD98059 on SRP72 mRNA expression. All the samples were treated under the same experimental conditions used in protein tests done by WB, and phosphorylation was measured indirectly by IP-WB. The results did not show significant changes on the mRNA expression of SRP72 after the treatment with these inhibitors.

     

     

    J Biol Chem 2010 285, 32824-32833. PD98059 purchased from Selleck.

  •  

    Activation of a TLR2eERK1/2 pathway in MDDC. (C) MDDC were either untreated or treated with C. pneumoniae alone or in the presence of the ERK1/2 inhibitor PD98059 for 48 h. IL-12p70 and IL-10 release in culture media was assessed by ELISA. (D) MDDC were treated as in panel C for 48 h and then cocultured with purified allogeneic CD3t T cells. On day 12, supernatants were collected, and secreted cytokines were measured by ELISA.

    Microbes Infect 2013 15, 105-14. PD98059 purchased from Selleck.

    HepG2 cells, “Pnt-2” primary HCC cells or THLE-2 normal liver cells were pretreated with PD-98059 (1 mM) or MEK-162 (“MEK”, 1 mM) for 1 h prior toWAY-600 (“WAY”, 100 nM) treatment, after applied period, cell viability and apoptosis were tested by MTT assay (F and H).

    Biochem Biophys Res Commun, 2016, 474(2):330-7.. PD98059 purchased from Selleck.

  • Collagen I and α-SMA are conducive for S. aureus adhesion to and invasion into BMFBs. BMFBs were treated with PD98059 2 h before the addition of 5 ng/ml TGF-β1; 24 h later, the adhesion (A) and invasion (B) assays were performed as previously described. The results are expressed as the mean cfu/ml ± SD from experiments performed in triplicate (*P < 0.05, **P < 0.01).

    Microb Pathog, 2017, 106:25-29. PD98059 purchased from Selleck.

    After starved in serum-free medium for 24h,T47D cells incubated with the indicated concentrations of  PD98059 for 3h,followed by 20-minute  stimolation of 100ng/ml EGF.

     

    2010 Dr. Zhang of Tianjin Medical University. PD98059 purchased from Selleck.

Purity & Quality Control

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.
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 MX3GeY5kfGmxbjDBd5NigQ>? NFLKWWwzPSEQvF2= NWHzboZGOSCq NEe0OI5jdHWwdIOgeIhmKEKdYW3QMYlv\HWlZXSgbY5kemWjc3WgbY4heGixc4Doc{1EcGtzIHHu[EBxcG:|cHjvMWVTUyCneIDy[ZN{cW:w NX3td|lvOjV5NkmxPFE>
MCF-7  MVnGeY5kfGmxbjDBd5NigQ>? NHLte5oyOCEQvF2= MoH0NUBp M2HqOIlvcGmkaYTzJGlNNTF6LXXubIFv[2WmIHPlcIwhdWmpcnH0bY9v NXT4U3loOjV5MkewNVE>
HepG2  M37PSGZ2dmO2aX;uJGF{e2G7 MmGwNVAh|ryP NWLDfpJtPSCq MlrLZoxw[2u|IIDoc5NxcG:{eXzheIVlKE2DUFvzJIlv\HWlZXSgZpkh\XixZ3Xuc5V{KFSJRj5OtlE> M2THcVI2PTZyNEi4
HepG2  MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPN[lkzOCEQvF2= NIn2eYIzPCCq NYTrTldne3WycILld5NmeyCWR1[t{tIyNWmwZIXj[YQh[2WubDDwdo9tcW[ncnH0bY9vKGGwZDDpcpZie2mxbh?= NYi1RmdzOjV3NkC0PFg>
MDA-MB-231 MlLPSpVv[3Srb36gRZN{[Xl? MlT0NlUh|ryP NXnScnAzOi1|IHi= M1nwOIRm[3KnYYPld{BxNUWUS{GvNkBidmRiU{GwNGE1KGW6cILld5Nqd25? NX3RfphNOjV3NUW4O|U>
SW480 NFz4T2dHfW6ldHnvckBCe3OjeR?= NUTaTlRLOjEEoN88US=> NYSzPGFnOcLiaB?= M1;5Z5Jm\HWlZYOgeIhmKGW6cILld5Nqd25ib3[gRXRHOyCycn;0[Ylv MkXONlU1PDd6MU[=
HCT-15 NUXkOIx4TnWwY4Tpc44hSXO|YYm= NHPXN4oyKGh? MlLWZZR1\W63YYTld{BRT0V{LXnu[JVk\WRicHjvd5Bpd3K7bHH0bY9vKG:oIFXyb:Kh MV2yOVQ{OTR{NR?=
HCT-15 M{jp[2Fxd3C2b4Ppd{BCe3OjeR?= NHXOUGUyKGh? NVTr[YVm[WKxbHnzbIV{KHSqZTDwdo91\WO2aY\lJIVn\mWldIOgc4YhWEeHMtMgZYdicW6|dDDjeZJkfW2rbj3pcoR2[2WmIHHwc5B1d3Orcx?= M2LZXFI2PDNzNEK1
786-O M1LXWWFxd3C2b4Ppd{BCe3OjeR?= MlvLOVDDqM7:TR?= MVyyOEBp NWHzTIo6eG:2ZX70bYF1\XQEoITo[UBxem9vYYDvdJRwfGmlIHXm[oVkfHNib3[gUmM> M1fHVFI1PTB6NEe2
A498 M4PGN2Fxd3C2b4Ppd{BCe3OjeR?= Mk\wOVDDqM7:TR?= MnjmNlQhcA>? NELaW49xd3SnboTpZZRme8LidHjlJJBzdy2jcH;weI91cWNiZX\m[YN1eyCxZjDORy=> NYHaNnJGOjR3MEi0O|Y>
NHBE MmT2SpVv[3Srb36gRZN{[Xl? MWiyM|IxKM7:TR?= MkTlNkBp MlfFZZR1\W63YYTld{BKVC1|MzDzeIlufWyjdHXkJGNZS0x6L1nMMVghe2WlcnX0bY9v NEHrRZczPDR5OUWyOi=>
A375 MnvER4VtdCCLbo\hd4lwdiCDc4PhfS=> M1HWOlEx6oDVMkCgxtVO M3;wUVI1KGh? MmW1doVlfWOnczDt[Yxidm:vYTDj[YxtKGmwdnHzbY9v NYrBbnpOOjR2Nk[wN|Y>
HBMEC NF7O[XFHfW6ldHnvckBCe3OjeR?= M{iwZVExKM7:TR?= M1vhNVEhcA>? M4SzTYJtd2OtczDWSWdHNWmwZIXj[YQhTXCqQUKg[ZhxemW|c3nvci=> MVqyOFQ2QDl6Mh?=
HPAEpiCs  MWXGeY5kfGmxbjDBd5NigQ>? MUGzNEDPxE1? NYjXdXA6OSCq NUHvOoZocW6qaXLpeJMhXE6ILd8xJJN1cW23bHH0[YQheDR{L4C0OEBOSVCNIIDoc5NxcG:{eXzheIlwdg>? MV2yOFQ1OTh5MB?=
BeWo Mni2SpVv[3Srb36gRZN{[Xl? NIP0PGsyOMLizszN MXeyJIg> NHuxcmtqdmirYnn0d{BGWktzL{K= MWGyOFQ{Ozh2Nh?=
PC3  MXfBdI9xfG:|aYOgRZN{[Xl? M2SwNVUxKM7:TR?= MYGwMlUhcA>? NH7qU4xqdmirYnn0d{BOUFlvNES5MYlv\HWlZXSgZZBweHSxc3nzxsA> M3rjeFI1PDJ2OEi5
HGC-27 NUTrbHYySXCxcITvd4l{KEG|c3H5 MYCxJOK2VQ>? MkXHNUBp NH\kbJJ{fXCycnXzd4V{KFKDRECwNUBxdHW|IF3LMVIzODZvaX7keYNm\CClZXzsJJZq[WKrbHn0fUBtd3O| NUS4co1JOjR2MU[zOFk>
MCF-7 MkDrSpVv[3Srb36gRZN{[Xl? MnXqNVDDqM7:TR?= MnjJNVAwOzBibXnu M3HOTpJm\HWlZYOgeIhmKFWWUD3k[ZBmdmSnboSgSXJMKHCqb4PwbI9zgWyjdHnvci=> Mmm3NlQ{QTB6MUm=
HUVECs M1HL[2Z2dmO2aX;uJGF{e2G7 NFTkWG4yOMLizszN NGG2cHcyKGh? M1zvbIlvcGmkaYTzJJRp\SCKRFygdoVlfWOnZDDDU3guOiCneIDy[ZN{cW:wIHHu[EBRT0lvMjDy[Yxm[XOn NWLiOZM3OjR|OEWxNFk>
HeLa MWDGeY5kfGmxbjDBd5NigQ>? NXLxcJY5PTBizszN MVmwMlUhcA>? NFTBeZpjdG:la4OgWHJZNTFiboXjcIVieiCvaXfyZZRqd25iYX7kJHRZVkmSIHTve44uemWpdXzheIlwdg>? MmLLNlQ{PzZ6Mke=
HL-60  M3u2XGZ2dmO2aX;uJGF{e2G7 NWfybGR2OTBxMkCg{txO MWCxJIg> NYT6TYt3cW6qaXLpeJMhfGinwrDOMkBkcGmwZX7zbZNmgHS{YXP0xsBqdmS3Y3XkJIRq\m[ncnXueIlifGmxbjDpcpRwKGe{YX71cI9kgXSncx?= M2Du[|I1OzV5MEKw
HL-60 NHXnXFVHfW6ldHnvckBCe3OjeR?= NVvvUZBQOiEEtV2= MUOxOkBp MX7EUXNQ MX\pcohq[mm2czD0bIUh[XO|b3PpZZRqd25ib3[gdHM3OjFiUnHmMVEh[W6mIF7GRXRkOyxiYX7kJJRp\SCUQT3pcoR2[2WmIIDoc5NxcG:{eXzheIlwdiCxZjDueYNt\WG{IF7GRXRkOw>? NG\ZTmEzPDN|MEC2PC=>
HEK 293 MYLGeY5kfGmxbjDBd5NigQ>? MUOxNEDPxE1? NWOzbmdMPSCq MlrHSG1UVw>? MYPpcohq[mm2czDXcpQucW6mdXPl[EDPui2lYYTlcolvN1SFRkSgZYN1cX[rdImgZY5lKG63Y3zlZZIh|rJvY3H0[Y5qdiCjY3P1cZVt[XSrb36= NW[xWXB{OjR|MkSzOlY>
HEK 293 NVnOVVczTnWwY4Tpc44hSXO|YYm= M17t[VExKM7:TR?= NWfCRVYzPSCq MkfqSG1UVw>? NWrwZ4FXe3WycILld5NmeyC2aHWgR3JVKGGldHn2bZR6 NVHzSXBJOjR|MkSzOlY>
SW480 NH3oUWFHfW6ldHnvckBCe3OjeR?= NW\kcXBsOTBizszN MXqyNEBp MmnpSG1UVw>? NYPIfGZxe3WycILld5NmeyC2aHWgR3JVKGGldHn2bZR6 NE\LeG0zPDN{NEO2Oi=>
HCSMCs M2GxPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnqVHFVOTBizszN MlHGNlQhcA>? M1fhRoJtd2OtczDGRWJRPC2rbnT1Z4VlKEiFQWPNR{Bxem:uaX\ldoF1cW:w MnSzNlQ{OTJ|OEG=
PANC-1 NWXEbXpqTnWwY4Tpc44hSXO|YYm= MVuyNEDPxE1? MnHwOFghcA>? MoezbY5pcWKrdIOgeIhmKGW6cILld5Nqd25ib3[g{rQ3TCCrbjDy[ZNxd26|ZTD0c{B1cGViUGDBVu61yqCjZ3;ubZN1yqB? M2r4PFI1Ojl2MUOz
A549 M2TseWZ2dmO2aX;uJGF{e2G7 NHK4bYU{OCEQvF2= M{PlRlAvPSCq NE\HfoNFVVOR M2fKUolvcGmkaYTzJJRp\SC2aILvcYJqdi2rbnT1Z4VlKEmOLUivR3hEVDhvTIXjJIFkfGm4aYT5 MVOyOFI4PzZ7Nh?=
A549 M{DMVmZ2dmO2aX;uJGF{e2G7 NXjyco52OzBizszN NV;uNWJxOC53IHi= MljxSG1UVw>? MYfpcohq[mm2czD0bJJwdWKrbj3pcoR2[2WmIFOvSWJR|rJiVHjyNlM2yqCyaH;zdIhwenmuYYTpc44> MXGyOFI4PzZ7Nh?=
MC-3 M4LucGFxd3C2b4Ppd{BCe3OjeR?= NVj1fFRtOTBizszN NGPQUHYzPCCq MXPwc5RmdnSrYYTl[EBOTVOFLXnu[JVk\WRiYYDvdJRwe2m|IHnuJEBk\Wyucx?= MlrqNlQzPzB3MkO=
Raji  M4K2fGZ2dmO2aX;uJGF{e2G7 MojENVAh|ryP M1zueFEhcA>? NELTWIRjdG:la4OgbJNDSU[IIHnu[JVk\WRiRYLrNU8zKHCqb4PwbI9zgWyjdHnvci=> NXTJbVlNOjR{Nkm2N|A>
Raji  MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLpU5JmOTBizszN MnPuNUBp M4LEfIlvcGmkaYTzJJRp\SCkYYPhcEBweiCqc1LBSmYue3SrbYXsZZRm\CClZXzsJJBzd2yrZnXyZZRqd25iYX7kJJZq[WKrbHn0fS=> MWOyOFI3QTZ|MB?=
HT29 NWfFTpc1TnWwY4Tpc44hSXO|YYm= MV:xNEDPxE1? MWWyJIg> Mkf3bY5pcWKrdIOgc4YhUkGNMjygSXJMOS9{IHHu[EBUXEGWMzDwbI9{eGixconsZZRqd25? Ml7vNlQzPjV{OUO=
HepG2 NFXIOmxCeG:ydH;zbZMhSXO|YYm= NX\SU5JSOjBizszN MoHxNlQhcA>? NEfuVoRqdmirYnn0d{BGWktzL{KgdIhwe3Cqb4L5cIF1cW:wIHHu[EBmdmijbnPld{BXSjFvaX7keYNm\CCjcH;weI9{cXN? MoPGNlQzPDd7MEm=
HepG2 NWXjN|FKTnWwY4Tpc44hSXO|YYm= MXGyNEDPxE1? MX:yJIg> MV;lcohidmOnczDWRlEucW6mdXPl[EBHV1iRM3GgeJJidnOlcnnweIlwdmGuIHHjeIl3cXS7 NH74RoczPDJ2N{mwPS=>
TE4 MV\GeY5kfGmxbjDBd5NigQ>? M4HGN|IxNzVyL{GwNEDPxE1? MUe0PEBp NHfJS45FVVOR NIHnN5pqdmirYnn0d{BxNUW{azDhcoQhf2:{dH3hco5qdiCmb4fudoVofWyjdHXkJJAuSWu2IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ Mn\MNlQzPDRyMkO=
TE1 M2THS2Z2dmO2aX;uJGF{e2G7 Mo\wNlAwPTBxMUCwJO69VQ>? Mm\aOFghcA>? MVzEUXNQ MY\pcohq[mm2czDwMWVzcyCjbnSge49zfG2jbn7pckBld3ewcnXneYxifGWmIICtRYt1KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NYnsXZM6OjR{NESwNlM>
KYSE30 NGjaO4JHfW6ldHnvckBCe3OjeR?= MYGyNE82OC9zMECg{txO NVj4cpVYPDhiaB?= MnvVSG1UVw>? Mn\ibY5pcWKrdIOgdE1GemtiYX7kJJdwenSvYX7ubY4h\G:5boLl[5Vt[XSnZDDwMWFsfCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MWqyOFI1PDB{Mx?=
TE1 MVnGeY5kfGmxbjDBd5NigQ>? Mme3OVAh|ryP NGHxTlY1QCCq MkH1SG1UVw>? NIiwboR2eHKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCKTFGgZ4xie3NiSR?= MYSyOFI1PDB{Mx?=
TE3 M2LkZ2Z2dmO2aX;uJGF{e2G7 MY[1NEDPxE1? M2\EUlQ5KGh? NXnmZnFOTE2VTx?= MUf1dJJm\3WuYYTld{B1cGViZYjwdoV{e2mxbjDv[kBJVEFiY3zhd5MhUQ>? M{PL[|I1OjR2MEKz
TE4 M4n3OWZ2dmO2aX;uJGF{e2G7 MliwOVAh|ryP MnXMOFghcA>? M4e1UmROW09? MYP1dJJm\3WuYYTld{B1cGViZYjwdoV{e2mxbjDv[kBJVEFiY3zhd5MhUQ>? M{OxflI1OjR2MEKz
TE5 MorMSpVv[3Srb36gRZN{[Xl? MV[1NEDPxE1? M33lSVQ5KGh? Mn7qSG1UVw>? NIHpZnh2eHKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCKTFGgZ4xie3NiSR?= NGrLdVAzPDJ2NECyNy=>
KYSE30 MXzGeY5kfGmxbjDBd5NigQ>? M{HjZVUxKM7:TR?= M{\uOFQ5KGh? MkjmSG1UVw>? MmjSeZBz\We3bHH0[ZMhfGinIHX4dJJme3Orb36gc4YhUEyDIHPsZZN{KEl? MoK5NlQzPDRyMkO=
MKN7 NHr0cZRHfW6ldHnvckBCe3OjeR?= NGSyT4M2OCEQvF2= M{TGR|Q5KGh? M17jWmROW09? M2e5Nolv[3KnYYPld{BmgHC{ZYPzbY9vKG:oIFjMRU1CODJib4KgTGxCNUF{NDDtc4xm[3WuZYO= MkjMNlQzPDRyMkO=
OE19 NX7SSlNzTnWwY4Tpc44hSXO|YYm= Mnu1OVAh|ryP NX7KTIluPDhiaB?= NXfTTFh6TE2VTx?= Ml7KbY5kemWjc3XzJIV5eHKnc4Ppc44hd2ZiSFzBMWExOiCxcjDIUGEuSTJ2IH3vcIVkfWyncx?= NX\yc5hQOjR{NESwNlM>
KATOIII  NFXLUVFHfW6ldHnvckBCe3OjeR?= MUO1NEDPxE1? Ml\kOFghcA>? MmrmSG1UVw>? MXzpcoNz\WG|ZYOg[ZhxemW|c3nvckBw\iCKTFGtRVAzKG:{IFjMRU1COjRibX;s[YN2dGW| MUOyOFI1PDB{Mx?=
NCI-N87  NVXoe21bTnWwY4Tpc44hSXO|YYm= MYq1NEDPxE1? MYi0PEBp NWLZVnhETE2VTx?= NYP1SIpycW6lcnXhd4V{KGW6cILld5Nqd25ib3[gTGxCNUFyMjDvdkBJVEFvQUK0JI1wdGWldXzldy=> M3nk[|I1OjR2MEKz
NUGC3 M4LGdGZ2dmO2aX;uJGF{e2G7 NWnNTXdCPTBizszN MXy0PEBp M3XTS2ROW09? MXnpcoNz\WG|ZYOg[ZhxemW|c3nvckBw\iCKTFGtRVAzKG:{IFjMRU1COjRibX;s[YN2dGW| M4LWeVI1OjR2MEKz
NUGC2 NXfsUIxkTnWwY4Tpc44hSXO|YYm= Mnz3OVAh|ryP NWqzVppXPDhiaB?= NX70OZlVTE2VTx?= NXjsW4REcW6lcnXhd4V{KGW6cILld5Nqd25ib3[gTGxCNUFyMjDvdkBJVEFvQUK0JI1wdGWldXzldy=> NIrlZVgzPDJ2NECyNy=>
SGC-7901  NX;WPZk5SXCxcITvd4l{KEG|c3H5 NGH0fIwzOCEQvF2= M{GxUVI1KGh? MYfpcohq[mm2czDDVE1u\WSrYYTl[EBieG:ydH;zbZM> MXqyOFI1OTN3MR?=
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ARPE-19 MV7GeY5kfGmxbjDBd5NigQ>? NUT6WllxOjBizszN NWDQSmp5OC53IHi= NY[2fGhlcW6qaXLpeJMhSXCnbHnuMYlv\HWlZXSgdIhwe3Cqb4L5cIF1cW:wIH;mJGVzcyCjbnSgRYt1 NGTOemgzPDJ{N{mxPC=>
CRL-2302 NFjxTW5HfW6ldHnvckBCe3OjeR?= M4TOTFIxKM7:TR?= MX:wMlUhcA>? NF23N3FqdmirYnn0d{BCeGWuaX6tbY5lfWOnZDDwbI9{eGixconsZZRqd25ib3[gSZJsKGGwZDDBb5Q> NVHKeHVmOjR{Mke5NVg>
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MCF-7 NI\SXIdCeG:ydH;zbZMhSXO|YYm= MkGyNlAh|ryP M2i4N|EhcA>? NWPkZ4hjcW6lcnXhd4V{KGOjc4Dhd4UuQSCnbor5cYUh[WO2aY\peJk> Ml3SNlQzOTZ{OEm=
DLD-1  NGPsTXVHfW6ldHnvckBCe3OjeR?= MVGyNOKh|ryP M2\zb|Q5KGh? MlTqdoVlfWOnczD0bIUhSk6LUEOg[ZhxemW|c3nvckBxemVvdILlZZRm\CC5aYToJFUu[XqjLXTD NVXrfocyOjR{MUG1PFE>
HT-29 MU\GeY5kfGmxbjDBd5NigQ>? MYOyNOKh|ryP NFfWVW41QCCq MknxdoVlfWOnczD0bIUhSk6LUEOg[ZhxemW|c3nvckBxemVvdILlZZRm\CC5aYToJFUu[XqjLXTD Mlm5NlQzOTF3OEG=
7402 NVrIZVlqSXCxcITvd4l{KEG|c3H5 NIq0[|M{OCEQvF2= NUn4TZNOPSCm MYnk[YNz\WG|ZYOgZ4VtdCCycn;sbYZmemG2aX;u MXOyOFIyOTJ3Mx?=
7721 MUTBdI9xfG:|aYOgRZN{[Xl? M{PUXVMxKM7:TR?= MXu1JIQ> NFXtOIFl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9v NGG2c3UzPDJzMUK1Ny=>
SGC7901  MljPRZBweHSxc3nzJGF{e2G7 MVK1NOKh|ryP NGLFWFUzPC92OD:3NkBp M4niPWROW09? NUjiblN1cW6mdXPld{BieG:ydH;zbZMh[2:vYnnu[YQhf2m2aDDKRWszKHOqUl7B M{n6XFI1OTd6MkSw
SMMC7721 M1mySWZ2dmO2aX;uJGF{e2G7 NFqxW5EzPS93MDFOwG0> NELUR4IzPCCq MUfzeZBxemW|c3XzJJRp\SCneIDy[ZN{cW:wIH;mJJAuSWu2IH;yJJAuTVKNMT:yxsA> MWWyOFE3QDB3Nh?=
MCF-7 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fkN|ExKM7:TR?= NVrRVI9nPDiq M3m1bGROW09? MUfy[ZZmenOnczDCUmYucW6mdXPl[EBk\WyuIHP5Z4xmKGG{cnXzeC=> NX;ORYNxOjRzNkO0NFQ>
Caco-2 M4rJcGZ2dmO2aX;uJGF{e2G7 NFrmXZc2OMLizszN MYO0PIg> MlrYSG1UVw>? NUm4WmxM\W6qYX7j[ZMhfGinIH3SUmEhdGW4ZXzzJI9nyqCVQ17ONWEtTli\REOsxsBNS1RuwrDMU3gtyqCKSV[zRUzDqFqJMU[sxsBRTEV4QdMgZY5lyqCOR1HMV|E3yqCpZX7ld:Kh[29vdILlZZRm\CC5aYToJGRmgA>? NF;TfG8zPDF4MU[5OS=>
HAECs MYjGeY5kfGmxbjDBd5NigQ>? NF\5TYEyOCEQvF2= NF\P[2MyKGh? NHrWUmLDqGG2dHXueYF1\XNiVF7GMe6yNXO2aX31cIF1\WRiSVPBUU0yKGGwZDDWR2FONTFiZYjwdoV{e2mxbh?= NV;vbXNKOjRzM{S2OVc>
Ca9-22 Mlj0SpVv[3Srb36gRZN{[Xl? MVOzJO69VQ>? M3vscVEhcA>? NUPOdVdH[WKxbHnzbIV{KHSqZTDhZoltcXS7IH;mJGhjWiC2bzDpcoR2[2ViSVytPEBxem:mdXP0bY9v MV6yOFEzPjV|Mh?=
Ca9-22 MXvGeY5kfGmxbjDBd5NigQ>? M3XxeFMh|ryP MXuxM|IhcA>? MXny[YR2[2W|IFjiVk1qdmS3Y3XkJGFVTi1{IIDoc5NxcG:{eXzheIlwdg>? NHiweoUzPDF{NkWzNi=>
AGS NHqzXGhHfW6ldHnvckBCe3OjeR?= NVLxZ|NZOTBizszNxsA> M2\R[FAvPSCq MnrEbY5pcWKrdIOgeIhmKHWycnXneYxifGmxbjDv[kB1cGViSVytPEBo\W6n MnvsNlQyODZzNk[=
Caco-2  MYfBdI9xfG:|aYOgRZN{[Xl? NHLLelIyOMLizszN MV[yOOKhcA>? MoL4[IVkemWjc3XzJINmdGxiYYDvdJRwe2m|IHnu[JVk\WRiYomgOU1HXQ>? MkLkNlQxQTV6NkO=
HCT-8 NFjLOYpCeG:ydH;zbZMhSXO|YYm= NX7DeXFmOTEEoN88US=> Mn3uNlTDqGh? M3LEXoRm[3KnYYPld{Bk\WyuIHHwc5B1d3OrczDpcoR2[2WmIHL5JFUuTlV? MVOyOFA6PTh4Mx?=
A549 NUWy[lJYTnWwY4Tpc44hSXO|YYm= NHXuOZY2OMLizszN MkL4NkBp MYXicI9kc3NiRWLLJJBpd3OyaH;yfYxifGmxbjDt[YRq[XSnZDDifUAyNDJvTmG= NGnF[nIzPDB4N{eyOy=>
HPMC NES4TYVHfW6ldHnvckBCe3OjeR?= NInCdlcyOMLizszN MYW0PEBp M3fIRZJmfmW{c3XzJJRp\SClaHHu[4V{KGmwIHPlcIwhdW:{cHjvcI9ogSCrbnT1Z4VlKGK7IFjHVGRU NHHUOIIzPDB2MkizPC=>
HPMC MX;BdI9xfG:|aYOgRZN{[Xl? M4CyOlExyqEQvF2= NFWwTXUzPMLiaB?= NHm1[ZJz\X[ncoPld{Bl\WO{ZXHz[UBqdiClZXzsJJZq[WKrbHn0fUBqdmS3Y3XkJIJ6KEiJUFTT MmDiNlQxPDJ6M{i=
MGC803  NFTsdIJCeG:ydH;zbZMhSXO|YYm= NWfGdXdLOjEEoN88US=> NU[4ZYp2OSCq M1LH[olvcGmkaYTzJIFxd3C2b4Ppd{BqdmS3Y3XkJIJ6KEmITj5OteKh[W6mIEZihNIuTE[XUh?= MnfoNlQxOjd5NUC=
SGC7901 MknWRZBweHSxc3nzJGF{e2G7 MWeyNOKh|ryP MljmNUBp NYPFV2J1cW6qaXLpeJMh[XCxcITvd4l{KGmwZIXj[YQh[nliSV\OMe6yyqCjbnSgOgKBui2GRmXS M4DNbFI1ODJ5N{Ww
COLO205 NGrJOlRCeG:ydH;zbZMhSXO|YYm= MVixNE8zOC92MDFOwG0> MXGyOEBp M4ridIlv\HWlZYOgSG5CKGyjZHTldkBnd3KvYYTpc44> MYmyOFAyQTFyOB?=
G292  NFLhWG9CeG:ydH;zbZMhSXO|YYm= NEDU[5E{OMLizszN NVrENWRtOiCq NUnIVYVHemW|dH;y[ZMh[2Gyc3HpZ4lvNWmwZIXj[YQh[2WubDDk[YF1cA>? NGXGXWgzPDBzMkmzNC=>
BxPC-3 MkTBSpVv[3Srb36gRZN{[Xl? NFfLPXcyOCEQvF5CpC=> NYPqSpAyPiCq M{\rfYlv[3KnYYPlJI1qWi1zNEOg[ZhxemW|c3nvci=> MoXQNlM6PzN5MUC=
HPAF-II MoDRSpVv[3Srb36gRZN{[Xl? MkWwNVAh|ryPwrC= NFLCOZA3KGh? MlPlbY5kemWjc3WgcYlTNTF2MzDlfJBz\XO|aX;u M2qy[FI{QTd|N{Gw
HL-60 MVnBdI9xfG:|aYOgRZN{[Xl? Mkm5OVDDqM7:TR?= NWC0TWo{OSCq MnS5doV{[3WnczDCRVE1PSCvZXTpZZRm\CCjcH;weI9{cXN? NHzL[40zOzl2OEe1NS=>
HepG2 NGfVeYNHfW6ldHnvckBCe3OjeR?= NHTGfHg1OCEQvF2= M1vqV|YwOTJiaB?= NWfEcZJGcW6qaXLpeJMhfGinIHnuZ5Jm[XOnIH;mJJAuTVKNMTDhcoQheC2lLVr1ckBxem:2ZXnuJIV5eHKnc4Ppc44h[nliUFy= NUi1b2F3OjN7NEK4OVE>
HUVECs Mo\qSpVv[3Srb36gRZN{[Xl? MWiyOUDPxE1? NVe5NW9xOSCq NGnqe|JqdmO{ZXHz[UBPTi4QulKgdFY2KG63Y3zlZZIhfHKjboPsc4NifGmxbh?= MV6yN|kxOTByOB?=
LNCaP  Mni1SpVv[3Srb36gRZN{[Xl? MVuxNEDPxE4EoB?= NECzTm8yKGh? Mn7W[IVkemWjc3XzJJRp\SCHR1[geZBz\We3bHH0[YQheC2\Qj2x M336fVI{QDN6M{G4
HL60  MkS3SpVv[3Srb36gRZN{[Xl? MXSyNOKh|ryP MV63NkBp NXvqRWF5TE2VTx?= MknUbY5pcWKrdIOg[IF{[XSrbnniMYlv\HWlZXSgR2QyOWJiZYjwdoV{e2mxbh?= MV[yN|gzPTV6NR?=
NB4  MXjGeY5kfGmxbjDBd5NigQ>? MWixNEDPxE4EoB?= NEPyUnk4OiCq NVfjVZdRTE2VTx?= M324cYlvcGmkaYTzJIRie2G2aX7pZk1qdmS3Y3XkJGNFOTGkIHX4dJJme3Orb36= Mm\5NlM5OjV3OEW=
EPOR/CR3 MmXsSpVv[3Srb36gRZN{[Xl? NIjGXng2OMLizszN M1n4TVMhcA>? NUD3RVQ3emWmdXPld{BGWE9iYX7kM49zKEmOLUOtbY5lfWOnZDD0bIUhfHm{b4PpcoUheGixc4Doc5J6dGG2aX;uxsA> NWHrTnpDOjN6MkC3N|E>
HUASMCs MWHGeY5kfGmxbjDBd5NigQ>? MkXjNVAh|ryPwrC= NEPxc2QzPCCq MXvkbY1qdmm|aHXzJGFv\yCLST3jZZV{\WRiU1;DV|MhdVKQQTDhcoQheHKxdHXpckBmgHC{ZYPzbY9vyqB? M2\mblI{QDF4NE[4
HUASMCs NX2w[nh1TnWwY4Tpc44hSXO|YYm= MkPlNVAh|ryPwrC= MY[yOEBp M2TIV4lvcGmkaYTzJGFv\yCLST3pcoR2[2WmIFXST|EwOiCyaH;zdIhwenmuYYTpc44hdGW4ZXy= MmHXNlM5OTZ2Nki=
SGC7901 MUPGeY5kfGmxbjDBd5NigQ>? M2fIelExKM7:TdMg MVOyOEBp MV3pcohq[mm2czD0bIUh\XiycnXzd4lwdiCxZjDwbI9{eGixconsZZRm\CCHUluxM|I> NFvoVWgzOzd7MkW4PC=>
MKN45 NHLK[|BHfW6ldHnvckBCe3OjeR?= NVXQeo5VOTBizszNxsA> MVuyOEBp NFy0Vo1qdmirYnn0d{B1cGViZYjwdoV{e2mxbjDv[kBxcG:|cHjvdplt[XSnZDDFVmsyNzJ? MlztNlM4QTJ3OEi=
SGC7901 NFHwZ3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{K2WlExKM7:TdMg MWqyOE81QC95MjDo Mo\obY5pcWKrdIOgZ4VtdCCpcn;3eIgh[29vdILlZZRm\CC5aYToJGRCWFR? NITGZlgzOzd7MkW4PC=>
MKN45 M4jaPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHPUJlUOTBizszNxsA> NVvCVodHOjRxNEivO|IhcA>? M17sfolvcGmkaYTzJINmdGxiZ4Lve5RpKGOxLYTy[YF1\WRid3n0bEBFSVCW M3nkWFI{Pzl{NUi4
SGC7901 MX;BdI9xfG:|aYOgRZN{[Xl? M3;ZUlExKM7:TdMg M13xRVI1KGh? M4PKUolv[3KnYYPld{B1cGViRFHQWE1qdmS3Y3XkJINmdGxiYYDvdJRwe2m| MUGyN|c6OjV6OB?=
MKN45 MYDBdI9xfG:|aYOgRZN{[Xl? NUfkTG9kOTBizszNxsA> NFn5VFgzPCCq NUK0V|h5cW6lcnXhd4V{KHSqZTDERXBVNWmwZIXj[YQh[2WubDDhdI9xfG:|aYO= M3SxRlI{Pzl{NUi4
BxPC-3 cells NUD4U|hpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPMU4czOMLizszN MoHiNE42KGh? Mnv3bY5pcWKrdIOgWmVITi2DLYLl[5Vt[XSnZDDIWXZGSyCpcn;3eIgh[W6mIIT1ZoUh\m:{bXH0bY9vKGmwZIXj[YQh[nliUFHSMVIhSVB? NYm1eoNSOjN5NkSwOFY>
NB4  MXPBdI9xfG:|aYOgRZN{[Xl? NUTxemh4OTBxMkCvOlAh|ryP M2LhXFEvPSCq NHTzWoRFVVOR MmW3[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHPvMZRz\WG2ZXSge4l1cCCSYXPsbZRigGWu MXqyN|c{PTV2MR?=
HepG2  NXm5dW57TnWwY4Tpc44hSXO|YYm= M4i0d|IxyqEQvF2= NYnrU4F5OjRiaB?= NGHBbWJqdmirYnn0d{B1cGViSF:tNUBxem:2ZXnuJIV5eHKnc4Ppc44h[29vdILlZZRm\CC5aYToJI1mfG[xcn3pci=> MXqyN|cxPzZyOR?=
HUVECs M13VZWFxd3C2b4Ppd{BCe3OjeR?= NETNNGQzNzRizszN M4PNPVI1NzR6IHi= NW\YOWx7cW6mdXPld{Bk\WyuIHTlZZRp MWiyN|cxPzV{MB?=
KG-1  M1;0TGFxd3C2b4Ppd{BCe3OjeR?= NG\qSG4zOMLizszN MlraNVIhcA>? MWflcohidmOnczDj[YxtKGGyb4D0c5NqeyCrbnT1Z4VlKGK7IGOx MWqyN|cxPjZ7MR?=
AML 1# MWHBdI9xfG:|aYOgRZN{[Xl? M2\hdVIxyqEQvF2= MmfxNVIhcA>? MVrlcohidmOnczDj[YxtKGGyb4D0c5NqeyCrbnT1Z4VlKGK7IGOx M4fET|I{PzB4Nkmx
A2780  NYrpe2JlTnWwY4Tpc44hSXO|YYm= NUXRXYdoOjEEoN88US=> MXKxJIg> MnzHZoxw[2u|IFTUR2QucW6mdXPl[EBFWjViZYjwdoV{e2mxbh?= M3GzUVI{Pjl4OE[y

... Click to View More Cell Line Experimental Data

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]

+ Expand

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]

+ Expand
  • 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]

+ Expand
  • 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

Bio Calculators

Molarity Calculator

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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).

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

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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