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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In DMSO USD 134 In stock
USD 147 In stock
USD 470 In stock
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Cited by 48 Publications

9 Customer Reviews

  • 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.

  • 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

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 NUjmUWIyTnWwY4Tpc44hSXO|YYm= Ml7mNlUh|ryP MUGxJIg> M1PhV4JtfW62czD0bIUhSlujXWCtbY5lfWOnZDDpcoNz\WG|ZTDpckBxcG:|cHjvMWNpczFiYX7kJJBpd3OyaH:tSXJMKGW6cILld5Nqd25? NFLBcFYzPTd4OUG4NS=>
MCF-7  NY\4O5VqTnWwY4Tpc44hSXO|YYm= NVjqOZFWOTBizszN MkjSNUBp NIrTeGxqdmirYnn0d{BKVC1zOD3lcohidmOnZDDj[YxtKG2rZ4LheIlwdg>? NXH3cFFkOjV5MkewNVE>
HepG2  MXvGeY5kfGmxbjDBd5NigQ>? MUmxNEDPxE1? MWO1JIg> MmTrZoxw[2u|IIDoc5NxcG:{eXzheIVlKE2DUFvzJIlv\HWlZXSgZpkh\XixZ3Xuc5V{KFSJRj5OtlE> M3WzZ|I2PTZyNEi4
HepG2  M2n2e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\x[FIxKM7:TR?= M3XBPFI1KGh? NU\SUGlqe3WycILld5NmeyCWR1[t{tIyNWmwZIXj[YQh[2WubDDwdo9tcW[ncnH0bY9vKGGwZDDpcpZie2mxbh?= NWLZOotTOjV3NkC0PFg>
MDA-MB-231 MYfGeY5kfGmxbjDBd5NigQ>? NVq4SG9uOjVizszN MWqyMVMhcA>? NX6xZZMy\GWlcnXhd4V{KHBvRWLLNU8zKGGwZDDTNVAxSTRiZYjwdoV{e2mxbh?= NVHLZWNUOjV3NUW4O|U>
SW480 MXzGeY5kfGmxbjDBd5NigQ>? M2PGTFIxyqEQvF2= M4LTPVHDqGh? Mm\FdoVlfWOnczD0bIUh\XiycnXzd4lwdiCxZjDBWGY{KHC{b4TlbY4> NH\aWWczPTR2N{ixOi=>
HCT-15 NEPJemJHfW6ldHnvckBCe3OjeR?= M{XscVEhcA>? NY\vbWhS[XS2ZX71ZZRmeyCSR1WyMYlv\HWlZXSgdIhwe3Cqb4L5cIF1cW:wIH;mJGVzc8Li NVr3SZY4OjV2M{G0NlU>
HCT-15 M1T2XmFxd3C2b4Ppd{BCe3OjeR?= NV7sbFE{OSCq NFrkbGZi[m:uaYPo[ZMhfGinIIDyc5Rm[3SrdnWg[YZn\WO2czDv[kBRT0V{wrDh[4FqdnO2IHP1doN2dWmwLXnu[JVk\WRiYYDvdJRwe2m| NHf2boszPTR|MUSyOS=>
786-O NXT1UW4ySXCxcITvd4l{KEG|c3H5 NUPiWJVVPTEEoN88US=> MWeyOEBp MWHwc5RmdnSrYYTld:KhfGinIIDyc{1ieG:ydH;0bYMh\W[oZXP0d{Bw\iCQQx?= MV:yOFUxQDR5Nh?=
A498 NFzsTopCeG:ydH;zbZMhSXO|YYm= NIPac2E2OMLizszN NWf1b5hNOjRiaB?= MlH5dI91\W62aXH0[ZPDqHSqZTDwdo8u[XCxcITveIlkKGWoZnXjeJMhd2ZiTlO= NUfIfWtmOjR3MEi0O|Y>
NHBE MVTGeY5kfGmxbjDBd5NigQ>? NH7UepkzNzJyIN88US=> MkTyNkBp Mn;2ZZR1\W63YYTld{BKVC1|MzDzeIlufWyjdHXkJGNZS0x6L1nMMVghe2WlcnX0bY9v Ml6yNlQ1Pzl3Mk[=
A375 M4LacGNmdGxiSX72ZZNqd25iQYPzZZk> MU[xNQKBmzJyINM1US=> MlnYNlQhcA>? MlTydoVlfWOnczDt[Yxidm:vYTDj[YxtKGmwdnHzbY9v NVPVelQ6OjR2Nk[wN|Y>
HBMEC Mmm4SpVv[3Srb36gRZN{[Xl? MUCxNEDPxE1? MYmxJIg> MVHicI9kc3NiVlXHSk1qdmS3Y3XkJGVxcEF{IHX4dJJme3Orb36= M4nMRVI1PDV6OUiy
HPAEpiCs  MXPGeY5kfGmxbjDBd5NigQ>? MUWzNEDPxE1? MnrNNUBp NUfie3VbcW6qaXLpeJMhXE6ILd8xJJN1cW23bHH0[YQheDR{L4C0OEBOSVCNIIDoc5NxcG:{eXzheIlwdg>? NYHOPGtMOjR2NEG4O|A>
BeWo NInTdmRHfW6ldHnvckBCe3OjeR?= Mnz0NVDDqM7:TR?= NELQfVczKGh? NYHY[2drcW6qaXLpeJMhTVKNMT:y MXeyOFQ{Ozh2Nh?=
PC3  M{\5TmFxd3C2b4Ppd{BCe3OjeR?= MWS1NEDPxE1? MnjkNE42KGh? M4LmVYlvcGmkaYTzJG1JYS12NEmtbY5lfWOnZDDhdI9xfG:|aYRCpC=> M4HxflI1PDJ2OEi5
HGC-27 Mo[yRZBweHSxc3nzJGF{e2G7 NWTvcoRROSEEtV2= Mkn3NUBp NITWb4p{fXCycnXzd4V{KFKDRECwNUBxdHW|IF3LMVIzODZvaX7keYNm\CClZXzsJJZq[WKrbHn0fUBtd3O| NXH0V2tiOjR2MU[zOFk>
MCF-7 M{j0fmZ2dmO2aX;uJGF{e2G7 MVGxNOKh|ryP MnTmNVAwOzBibXnu MmH0doVlfWOnczD0bIUhXVSSLXTldIVv\GWwdDDFVmsheGixc4Doc5J6dGG2aX;u NWHrdo5KOjR|OUC4NVk>
HUVECs NXrG[XZNTnWwY4Tpc44hSXO|YYm= NIjWU2cyOMLizszN NHP2eYYyKGh? NHHXXVZqdmirYnn0d{B1cGViSFTMJJJm\HWlZXSgR29ZNTJiZYjwdoV{e2mxbjDhcoQhWEeLLUKgdoVt\WG|ZR?= NInufYMzPDN6NUGwPS=>
HeLa M2fxXWZ2dmO2aX;uJGF{e2G7 M1H0SVUxKM7:TR?= NGq1cpoxNjViaB?= NWLmVlN{[myxY3vzJHRTYC1zIH71Z4xm[XJibXnndoF1cW:wIHHu[EBVYE6LUDDkc5dvNXKnZ4XsZZRqd25? M3fHT|I1Ozd4OEK3
HL-60  MkTJSpVv[3Srb36gRZN{[Xl? NHnCXpUyOC9{MDFOwG0> NFq0PGEyKGh? M3jIPIlvcGmkaYTzJJRp\cLiTj6gZ4hqdmWwc3nz[Zh1emGldNMgbY5lfWOnZDDkbYZn\XKnboTpZZRqd25iaX70c{BoemGwdXzvZ5l1\XN? NIGzZmszPDN3N{CyNC=>
HL-60 M4DmVGZ2dmO2aX;uJGF{e2G7 Mo[5NkDDvU1? NUTNR2VwOTZiaB?= MnrISG1UVw>? NHjrOW9qdmirYnn0d{B1cGViYYPzc4Nq[XSrb36gc4YheFN4MkGgVoFnNTFiYX7kJG5HSVSlMzygZY5lKHSqZTDSRU1qdmS3Y3XkJJBpd3OyaH;yfYxifGmxbjDv[kBvfWOuZXHyJG5HSVSlMx?= NHywUZkzPDN|MEC2PC=>
HEK 293 M2DCeGZ2dmO2aX;uJGF{e2G7 MnKyNVAh|ryP NEH0VGs2KGh? NXy2R3ZTTE2VTx?= MmLCbY5pcWKrdIOgW451NWmwZIXj[YQh|rJvY3H0[Y5qdi:WQ1[0JIFkfGm4aYT5JIFv\CCwdXPs[YFzKM7{LXPheIVvcW5iYXPjeY12dGG2aX;u Mmf1NlQ{OjR|Nk[=
HEK 293 NWCxN2w1TnWwY4Tpc44hSXO|YYm= NH3vRoMyOCEQvF2= NGPyZpQ2KGh? NUD0VGZqTE2VTx?= MkL2d5VxeHKnc4Pld{B1cGViQ2LUJIFkfGm4aYT5 MlXlNlQ{OjR|Nk[=
SW480 M4HEO2Z2dmO2aX;uJGF{e2G7 NFLZT2wyOCEQvF2= MnvHNlAhcA>? MXzEUXNQ NXyzOZhYe3WycILld5NmeyC2aHWgR3JVKGGldHn2bZR6 MnLTNlQ{OjR|Nk[=
HCSMCs M4\VU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2ToeVExKM7:TR?= MnGwNlQhcA>? MXTicI9kc3NiRlHCVFQucW6mdXPl[EBJS0GVTVOgdJJwdGmoZYLheIlwdg>? NVfVXnh[OjR|MUKzPFE>
PANC-1 M1LpSWZ2dmO2aX;uJGF{e2G7 Mor1NlAh|ryP MUK0PEBp NULZW4g6cW6qaXLpeJMhfGinIHX4dJJme3Orb36gc4Yh|pR4RDDpckBz\XOyb37z[UB1dyC2aHWgVHBCWs72wrDh[49vcXO2wrC= M{fESFI1Ojl2MUOz
A549 MnGySpVv[3Srb36gRZN{[Xl? MVyzNEDPxE1? NICxfXQxNjViaB?= NHvIeFRFVVOR NIe4d3dqdmirYnn0d{B1cGVidHjyc41jcW5vaX7keYNm\CCLTD24M2NZS0x6LVz1Z{Bi[3Srdnn0fS=> M2\I[|I1Ojd5Nkm2
A549 M4nGbmZ2dmO2aX;uJGF{e2G7 NEDsc|c{OCEQvF2= NGruOIsxNjViaB?= NHPrc|FFVVOR M3L0bIlvcGmkaYTzJJRpem:vYnnuMYlv\HWlZXSgR{9GSlEQsjDUbJIzOzYEoIDoc5NxcG:{eXzheIlwdg>? MXeyOFI4PzZ7Nh?=
MC-3 MmO3RZBweHSxc3nzJGF{e2G7 Mly4NVAh|ryP MVSyOEBp MULwc5RmdnSrYYTl[EBOTVOFLXnu[JVk\WRiYYDvdJRwe2m|IHnuJEBk\Wyucx?= NWj6[XdxOjR{N{C1NlM>
Raji  MUHGeY5kfGmxbjDBd5NigQ>? NH7kfXcyOCEQvF2= MmnyNUBp MXnicI9kc3NiaIPCRWZHKGmwZIXj[YQhTXKtMT:yJJBpd3OyaH;yfYxifGmxbh?= MkXjNlQzPjl4M{C=
Raji  NUnhcZNyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWexNEDPxE1? NVr2OVR1OSCq NIPNeGJqdmirYnn0d{B1cGViYnHzZYwhd3JiaIPCRWZHNXO2aX31cIF1\WRiY3XscEBxem:uaX\ldoF1cW:wIHHu[EB3cWGkaXzpeJk> MmXGNlQzPjl4M{C=
HT29 MUTGeY5kfGmxbjDBd5NigQ>? NFnFOGIyOCEQvF2= NXXuRpl[OiCq MW\pcohq[mm2czDv[kBLSUt{LDDFVmsyNzJiYX7kJHNVSVR|IIDoc5NxcG:{eXzheIlwdg>? MYKyOFI3PTJ7Mx?=
HepG2 MkT1RZBweHSxc3nzJGF{e2G7 MnH0NlAh|ryP MmLxNlQhcA>? M3X1fYlvcGmkaYTzJGVTUzFxMjDwbI9{eGixconsZZRqd25iYX7kJIVvcGGwY3XzJHZDOS2rbnT1Z4VlKGGyb4D0c5Nqew>? M2HMWlI1OjR5OUC5
HepG2 M2HQZ2Z2dmO2aX;uJGF{e2G7 MVSyNEDPxE1? MkXrNkBp NV31WlRF\W6qYX7j[ZMhXkJzLXnu[JVk\WRiRl;YU|NiKHS{YX7zZ5JqeHSrb37hcEBi[3Srdnn0fS=> NFLldXEzPDJ2N{mwPS=>
TE4 M2f5O2Z2dmO2aX;uJGF{e2G7 MmjoNlAwPTBxMUCwJO69VQ>? NUfJNYc3PDhiaB?= NWTt[WU{TE2VTx?= NH62R3VqdmirYnn0d{BxNUW{azDhcoQhf2:{dH3hco5qdiCmb4fudoVofWyjdHXkJJAuSWu2IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ Mn31NlQzPDRyMkO=
TE1 NWLwbmI1TnWwY4Tpc44hSXO|YYm= NYHWZoNxOjBxNUCvNVAxKM7:TR?= MY[0PEBp MmrhSG1UVw>? M2HPWolvcGmkaYTzJJAuTXKtIHHu[EB4d3K2bXHucolvKGSxd37y[Yd2dGG2ZXSgdE1Cc3RiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MYmyOFI1PDB{Mx?=
KYSE30 NVO5Ro8yTnWwY4Tpc44hSXO|YYm= Mn7xNlAwPTBxMUCwJO69VQ>? M4P3cVQ5KGh? M4T5bmROW09? Moi2bY5pcWKrdIOgdE1GemtiYX7kJJdwenSvYX7ubY4h\G:5boLl[5Vt[XSnZDDwMWFsfCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NV\MRpJ4OjR{NESwNlM>
TE1 NHH4Z4JHfW6ldHnvckBCe3OjeR?= NYHhV3hwPTBizszN NUXWZpd3PDhiaB?= MWLEUXNQ MV\1dJJm\3WuYYTld{B1cGViZYjwdoV{e2mxbjDv[kBJVEFiY3zhd5MhUQ>? M2[1UVI1OjR2MEKz
TE3 MWDGeY5kfGmxbjDBd5NigQ>? M3nIN|UxKM7:TR?= MWG0PEBp M1XDSWROW09? M2HxRZVxemWpdXzheIV{KHSqZTDlfJBz\XO|aX;uJI9nKEiOQTDjcIF{eyCL MlXTNlQzPDRyMkO=
TE4 M17aXGZ2dmO2aX;uJGF{e2G7 Mlj2OVAh|ryP MkPIOFghcA>? MUfEUXNQ MVX1dJJm\3WuYYTld{B1cGViZYjwdoV{e2mxbjDv[kBJVEFiY3zhd5MhUQ>? MWCyOFI1PDB{Mx?=
TE5 M4\nU2Z2dmO2aX;uJGF{e2G7 M1HZOlUxKM7:TR?= MYW0PEBp NEXY[YFFVVOR NUjVV29TfXC{ZXf1cIF1\XNidHjlJIV5eHKnc4Ppc44hd2ZiSFzBJINt[XO|IFm= Ml3UNlQzPDRyMkO=
KYSE30 MY\GeY5kfGmxbjDBd5NigQ>? NIS1dmk2OCEQvF2= Mn7hOFghcA>? NFfHXlRFVVOR MonmeZBz\We3bHH0[ZMhfGinIHX4dJJme3Orb36gc4YhUEyDIHPsZZN{KEl? Mn3vNlQzPDRyMkO=
MKN7 MmfDSpVv[3Srb36gRZN{[Xl? MXS1NEDPxE1? NYq4R4F4PDhiaB?= MYHEUXNQ NXTnZ21rcW6lcnXhd4V{KGW6cILld5Nqd25ib3[gTGxCNUFyMjDvdkBJVEFvQUK0JI1wdGWldXzldy=> NEixVYgzPDJ2NECyNy=>
OE19 NUnN[VU5TnWwY4Tpc44hSXO|YYm= MVS1NEDPxE1? Mme1OFghcA>? NVXVTVk{TE2VTx?= MlLpbY5kemWjc3XzJIV5eHKnc4Ppc44hd2ZiSFzBMWExOiCxcjDIUGEuSTJ2IH3vcIVkfWyncx?= MXuyOFI1PDB{Mx?=
KATOIII  NXLTSJA{TnWwY4Tpc44hSXO|YYm= MVS1NEDPxE1? MVG0PEBp NH;2fYlFVVOR MXPpcoNz\WG|ZYOg[ZhxemW|c3nvckBw\iCKTFGtRVAzKG:{IFjMRU1COjRibX;s[YN2dGW| NHrVNpAzPDJ2NECyNy=>
NCI-N87  NUWxe5pyTnWwY4Tpc44hSXO|YYm= MnqwOVAh|ryP M1XxNVQ5KGh? MmLqSG1UVw>? M4\0NIlv[3KnYYPld{BmgHC{ZYPzbY9vKG:oIFjMRU1CODJib4KgTGxCNUF{NDDtc4xm[3WuZYO= MVGyOFI1PDB{Mx?=
NUGC3 MUHGeY5kfGmxbjDBd5NigQ>? NFHEV4g2OCEQvF2= Mmq2OFghcA>? NUHJVWx4TE2VTx?= NHTZdFRqdmO{ZXHz[ZMh\XiycnXzd4lwdiCxZjDIUGEuSTB{IH;yJGhNSS2DMkSgcY9t\WO3bHXz NIrlb5QzPDJ2NECyNy=>
NUGC2 NY\abHk6TnWwY4Tpc44hSXO|YYm= MY[1NEDPxE1? MnXZOFghcA>? MWLEUXNQ NH20PW1qdmO{ZXHz[ZMh\XiycnXzd4lwdiCxZjDIUGEuSTB{IH;yJGhNSS2DMkSgcY9t\WO3bHXz MUKyOFI1PDB{Mx?=
SGC-7901  M2TNV2Fxd3C2b4Ppd{BCe3OjeR?= MXmyNEDPxE1? M1LCNlI1KGh? NWrYVGlicW6qaXLpeJMhS1BvbXXkbYF1\WRiYYDvdJRwe2m| M1PGdlI1OjRzM{Wx
MG-63 MoLVSpVv[3Srb36gRZN{[Xl? NV7Ed5ZbOjBizszN NHH4OowxNjViaB?= NHXSdJJjdG:la4OgeIhmKEOKLXnu[JVk\WRicHjvd5Bpd3K7bHH0[YQhTUyNMTDwdo91\WmwIHX4dJJme3Orb36= M1KxdVI1OjN7NkSw
ARPE-19 NVTSblltTnWwY4Tpc44hSXO|YYm= NF61V4QzOCEQvF2= NVi1VmRpOC53IHi= MULpcohq[mm2czDBdIVtcW5vaX7keYNm\CCyaH;zdIhwenmuYYTpc44hd2ZiRYLrJIFv\CCDa4S= M{PLe|I1OjJ5OUG4
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SMMC7721 MnfLSpVv[3Srb36gRZN{[Xl? Ml61NlUwPTBizszN MUCyOEBp NGjkV|Z{fXCycnXzd4V{KHSqZTDlfJBz\XO|aX;uJI9nKHBvQXv0JI9zKHBvRWLLNU8zyqB? MUeyOFE3QDB3Nh?=
MCF-7 NHXNVGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV6xNEDPxE1? M4Luc|Q5cA>? NITsRnRFVVOR MlnEdoV3\XK|ZYOgRm5HNWmwZIXj[YQh[2WubDDjfYNt\SCjcoLld5Q> MmjmNlQyPjN2MES=
Caco-2 NFj1S2FHfW6ldHnvckBCe3OjeR?= NIrQeIQ2OMLizszN M{\JUVQ5cA>? NX3FcoIyTE2VTx?= NV7qUmhR\W6qYX7j[ZMhfGinIH3SUmEhdGW4ZXzzJI9nyqCVQ17ONWEtTli\REOsxsBNS1RuwrDMU3gtyqCKSV[zRUzDqFqJMU[sxsBRTEV4QdMgZY5lyqCOR1HMV|E3yqCpZX7ld:Kh[29vdILlZZRm\CC5aYToJGRmgA>? MlHZNlQyPjF4OUW=
HAECs NXj4PHNPTnWwY4Tpc44hSXO|YYm= MYmxNEDPxE1? MU[xJIg> M{m0UOKh[XS2ZX71ZZRmeyCWTl[t{tEue3SrbYXsZZRm\CCLQ1HNMVEh[W6mIG\DRW0uOSCneIDy[ZN{cW:w NYfUXlRjOjRzM{S2OVc>
Ca9-22 NIjWUINHfW6ldHnvckBCe3OjeR?= MUezJO69VQ>? MVixJIg> M1X4bIFjd2yrc3jld{B1cGViYXLpcIl1gSCxZjDIZnIhfG9iaX7keYNmKEmOLUigdJJw\HWldHnvci=> NWn0cXRjOjRzMk[1N|I>
Ca9-22 NYPON41vTnWwY4Tpc44hSXO|YYm= MlHRN{DPxE1? NFXzXJUyNzJiaB?= M37m[JJm\HWlZYOgTIJTNWmwZIXj[YQhSVSILUKgdIhwe3Cqb4L5cIF1cW:w MmTSNlQyOjZ3M{K=
AGS NWLZSlNbTnWwY4Tpc44hSXO|YYm= NV7zbpV3OTBizszNxsA> MXGwMlUhcA>? NVOyOGFUcW6qaXLpeJMhfGinIIXwdoVofWyjdHnvckBw\iC2aHWgTWwuQCCpZX7l MXmyOFExPjF4Nh?=
Caco-2  MU\BdI9xfG:|aYOgRZN{[Xl? M4WyfVExyqEQvF2= NYnhUmRQOjUEoHi= NIfuR|Bl\WO{ZXHz[ZMh[2WubDDhdI9xfG:|aYOgbY5lfWOnZDDifUA2NU[X NXu1XI4{OjRyOUW4OlM>
HCT-8 NGX4S5RCeG:ydH;zbZMhSXO|YYm= MkPpNVDDqM7:TR?= MkKxNlTDqGh? M{mwdIRm[3KnYYPld{Bk\WyuIHHwc5B1d3OrczDpcoR2[2WmIHL5JFUuTlV? MlfDNlQxQTV6NkO=
A549 MXLGeY5kfGmxbjDBd5NigQ>? Ml[3OVDDqM7:TR?= Mnf5NkBp MXLicI9kc3NiRWLLJJBpd3OyaH;yfYxifGmxbjDt[YRq[XSnZDDifUAyNDJvTmG= M4Pk[FI1ODZ5N{K3
HPMC NUHNVXRYTnWwY4Tpc44hSXO|YYm= Mk\FNVDDqM7:TR?= MnL2OFghcA>? MYXy[ZZmenOnczD0bIUh[2ijbnfld{BqdiClZXzsJI1wenCqb3zv[5khcW6mdXPl[EBjgSCKR2DEVy=> MofFNlQxPDJ6M{i=
HPMC NFy4bmlCeG:ydH;zbZMhSXO|YYm= MXKxNOKh|ryP M4\JblI1yqCq NImwSZdz\X[ncoPld{Bl\WO{ZXHz[UBqdiClZXzsJJZq[WKrbHn0fUBqdmS3Y3XkJIJ6KEiJUFTT NUfUN3hROjRyNEK4N|g>
MGC803  NXHCZlc2SXCxcITvd4l{KEG|c3H5 MViyNOKh|ryP MnfNNUBp M1zNZolvcGmkaYTzJIFxd3C2b4Ppd{BqdmS3Y3XkJIJ6KEmITj5OteKh[W6mIEZihNIuTE[XUh?= M2Pke|I1ODJ5N{Ww
SGC7901 MlHiRZBweHSxc3nzJGF{e2G7 NX\v[phrOjEEoN88US=> M1;zclEhcA>? MV;pcohq[mm2czDhdI9xfG:|aYOgbY5lfWOnZDDifUBKTk5vzsJCpIFv\CB34pEyMWRHXVJ? M2nxVlI1ODJ5N{Ww
COLO205 M3;IUmFxd3C2b4Ppd{BCe3OjeR?= MmHPNVAwOjBxNECg{txO M4\MVFI1KGh? M3PCZ4lv\HWlZYOgSG5CKGyjZHTldkBnd3KvYYTpc44> MkDoNlQxOTlzMEi=
G292  MXXBdI9xfG:|aYOgRZN{[Xl? M2rHVFMxyqEQvF2= MmjLNkBp MYXy[ZN1d3KnczDjZZB{[WmlaX6tbY5lfWOnZDDj[YxtKGSnYYTo NXixXZBEOjRyMUK5N|A>
BxPC-3 M4XObGZ2dmO2aX;uJGF{e2G7 MlTjNVAh|ryPwrC= MY[2JIg> NG\aNHFqdmO{ZXHz[UBucVJvMUSzJIV5eHKnc4Ppc44> M4nueVI{QTd|N{Gw
HPAF-II MVfGeY5kfGmxbjDBd5NigQ>? NVHDbXpPOTBizszNxsA> Mm\nOkBp MnXybY5kemWjc3WgcYlTNTF2MzDlfJBz\XO|aX;u Mm[2NlM6PzN5MUC=
HL-60 M{fzZWFxd3C2b4Ppd{BCe3OjeR?= MmK2OVDDqM7:TR?= Ml;TNUBp NELNT|lz\XOldXXzJGJCOTR3IH3l[IlifGWmIHHwc5B1d3Orcx?= NUDYNYhXOjN7NEi3OVE>
HepG2 MVrGeY5kfGmxbjDBd5NigQ>? MWq0NEDPxE1? MWm2M|EzKGh? M4i2TIlvcGmkaYTzJJRp\SCrbnPy[YF{\SCxZjDwMWVTUzFiYX7kJJAu[y2MdX6gdJJwfGWrbjDlfJBz\XO|aX;uJIJ6KFCO NYPZUplkOjN7NEK4OVE>
HUVECs MYPGeY5kfGmxbjDBd5NigQ>? Mof3NlUh|ryP MlL5NUBp NXPUXVRHcW6lcnXhd4UhVkZvzsrCJJA3PSCwdXPs[YFzKHS{YX7zcI9k[XSrb36= M4HPelI{QTBzMEC4
LNCaP  M2KxdmZ2dmO2aX;uJGF{e2G7 M2jG[FExKM7:TdMg NVTmcGV[OSCq Mnm5[IVkemWjc3XzJJRp\SCHR1[geZBz\We3bHH0[YQheC2\Qj2x MUKyN|g{QDNzOB?=
HL60  NUXHOmNxTnWwY4Tpc44hSXO|YYm= MWiyNOKh|ryP M{[5SVczKGh? MXjEUXNQ MlPEbY5pcWKrdIOg[IF{[XSrbnniMYlv\HWlZXSgR2QyOWJiZYjwdoV{e2mxbh?= NHfKUYkzOzh{NUW4OS=>
NB4  M1LCdGZ2dmO2aX;uJGF{e2G7 NGTGOI8yOCEQvF5CpC=> NFjk[ZY4OiCq M3n0PGROW09? MniybY5pcWKrdIOg[IF{[XSrbnniMYlv\HWlZXSgR2QyOWJiZYjwdoV{e2mxbh?= NYDmXZJGOjN6MkW1PFU>
EPOR/CR3 NV;ZfWhYTnWwY4Tpc44hSXO|YYm= M2HYR|UxyqEQvF2= NGe2UY8{KGh? MlS5doVlfWOnczDFVG8h[W6mL3;yJGlNNTNvaX7keYNm\CC2aHWgeJlzd3OrbnWgdIhwe3Cqb4L5cIF1cW:wwrC= NGD2XlczOzh{MEezNS=>
HUASMCs NFTrRYlHfW6ldHnvckBCe3OjeR?= NXHKbHhROTBizszNxsA> Mk\CNlQhcA>? NVrpWY9X\GmvaX7pd4hmeyCDbnegTWku[2G3c3XkJHNQS1N|IH3SUmEh[W6mIIDyc5RmcW5iZYjwdoV{e2mxbtMg NH;sSGozOzhzNkS2PC=>
HUASMCs NWrDXHRzTnWwY4Tpc44hSXO|YYm= NHj1UHoyOCEQvF5CpC=> M2\MeVI1KGh? M2rpUYlvcGmkaYTzJGFv\yCLST3pcoR2[2WmIFXST|EwOiCyaH;zdIhwenmuYYTpc44hdGW4ZXy= MV[yN|gyPjR4OB?=
SGC7901 M3v4cGZ2dmO2aX;uJGF{e2G7 MUmxNEDPxE4EoB?= MoK0NlQhcA>? NUnoUnFscW6qaXLpeJMhfGinIHX4dJJme3Orb36gc4YheGixc4Doc5J6dGG2ZXSgSXJMOS9{ MYKyN|c6OjV6OB?=
MKN45 M1PUSmZ2dmO2aX;uJGF{e2G7 NYrOXo9SOTBizszNxsA> M{XHcVI1KGh? MVXpcohq[mm2czD0bIUh\XiycnXzd4lwdiCxZjDwbI9{eGixconsZZRm\CCHUluxM|I> NXL5UGRxOjN5OUK1PFg>
SGC7901 M2j4N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW[ySnNHOTBizszNxsA> MVWyOE81QC95MjDo MV;pcohq[mm2czDj[YxtKGe{b4f0bEBkdy22cnXheIVlKHerdHigSGFRXA>? NVvicGJzOjN5OUK1PFg>
MKN45 M{O3Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjUVJcxOTBizszNxsA> NG\0d44zPC92OD:3NkBp MmO2bY5pcWKrdIOgZ4VtdCCpcn;3eIgh[29vdILlZZRm\CC5aYToJGRCWFR? MXyyN|c6OjV6OB?=
SGC7901 M{XzUGFxd3C2b4Ppd{BCe3OjeR?= NELrTWsyOCEQvF5CpC=> NGDQU|MzPCCq NFXzO2VqdmO{ZXHz[ZMhfGinIFTBVHQucW6mdXPl[EBk\WyuIHHwc5B1d3Orcx?= M3jCUFI{Pzl{NUi4
MKN45 NE\NTIJCeG:ydH;zbZMhSXO|YYm= MoTmNVAh|ryPwrC= NXLrSplqOjRiaB?= Mn3nbY5kemWjc3XzJJRp\SCGQWDUMYlv\HWlZXSgZ4VtdCCjcH;weI9{cXN? Mof3NlM4QTJ3OEi=
BxPC-3 cells MoHTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVuyNOKh|ryP MoP5NE42KGh? M{HpW4lvcGmkaYTzJHZGT0ZvQT3y[Yd2dGG2ZXSgTHVXTUNiZ4Lve5RpKGGwZDD0eYJmKG[xcn3heIlwdiCrbnT1Z4VlKGK7IGDBVk0zKEGS M{XBSVI{PzZ2MES2
NB4  MkSzRZBweHSxc3nzJGF{e2G7 M1\tcFExNzJyL{[wJO69VQ>? MWqxMlUhcA>? Ml;VSG1UVw>? MYnk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliY3:teJJm[XSnZDD3bZRpKFCjY3zpeIF5\Wx? NIHZWWozOzd|NUW0NS=>
HepG2  MXvGeY5kfGmxbjDBd5NigQ>? NXnkVYcyOjEEoN88US=> MUWyOEBp NWXBc4ZUcW6qaXLpeJMhfGinIFjPMVEheHKxdHXpckBmgHC{ZYPzbY9vKGOxLYTy[YF1\WRid3n0bEBu\XSob4LtbY4> M1jNOFI{PzB5NkC5
HUVECs NIfkOlhCeG:ydH;zbZMhSXO|YYm= NG[4ZW0zNzRizszN NX3kbWdyOjRxNEigbC=> MUjpcoR2[2W|IHPlcIwh\GWjdHi= NWrZTVdwOjN5MEe1NlA>
KG-1  NEDRfplCeG:ydH;zbZMhSXO|YYm= MYmyNOKh|ryP NEnQS40yOiCq NHLlNXBmdmijbnPld{Bk\WyuIHHwc5B1d3OrczDpcoR2[2WmIHL5JHMy MV:yN|cxPjZ7MR?=
AML 1# MYHBdI9xfG:|aYOgRZN{[Xl? MmHiNlDDqM7:TR?= NYDkWoVYOTJiaB?= NYO0b4Yz\W6qYX7j[ZMh[2WubDDhdI9xfG:|aYOgbY5lfWOnZDDifUBUOQ>? NUj3UJk1OjN5ME[2PVE>
A2780  MknLSpVv[3Srb36gRZN{[Xl? NHjFT28zOMLizszN Mli3NUBp NVywO3FQ[myxY3vzJGRVS0RvaX7keYNm\CCGUkWg[ZhxemW|c3nvci=> NGiyNoszOzZ7Nki2Ni=>

... 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 (52.37 mM) warming
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 4% DMSO+30% PEG 300+5% Tween 80+ddH2O 1mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID