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
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Cited by 50 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 NVvBeHluTnWwY4Tpc44hSXO|YYm= MVqyOUDPxE1? NYHF[oFUOSCq NUnC[4R4[my3boTzJJRp\SCEW3HdVE1qdmS3Y3XkJIlv[3KnYYPlJIlvKHCqb4PwbI8uS2itMTDhcoQheGixc4Doc{1GWktiZYjwdoV{e2mxbh?= NIflc3MzPTd4OUG4NS=>
MCF-7  MXrGeY5kfGmxbjDBd5NigQ>? MkHsNVAh|ryP NH;GVIkyKGh? NH7jR5dqdmirYnn0d{BKVC1zOD3lcohidmOnZDDj[YxtKG2rZ4LheIlwdg>? NVPzc29[OjV5MkewNVE>
HepG2  NUXqfnplTnWwY4Tpc44hSXO|YYm= NYL3TY93OTBizszN MW[1JIg> MX\icI9kc3NicHjvd5Bpd3K7bHH0[YQhVUGSS4OgbY5lfWOnZDDifUBmgG:pZX7veZMhXEeILd8yNS=> M3;LXlI2PTZyNEi4
HepG2  MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXLqd4lYOjBizszN NGPMTmczPCCq M{DjcZN2eHC{ZYPz[ZMhXEeILd8yNU1qdmS3Y3XkJINmdGxicILvcIln\XKjdHnvckBidmRiaX72ZZNqd25? MnnwNlU2PjB2OEi=
MDA-MB-231 M{PXN2Z2dmO2aX;uJGF{e2G7 NHHQdZUzPSEQvF2= Mn[0Nk0{KGh? NHe5PINl\WO{ZXHz[ZMheC2HUluxM|Ih[W6mIGOxNFBCPCCneIDy[ZN{cW:w M1jjclI2PTV3OEe1
SW480 MlPWSpVv[3Srb36gRZN{[Xl? M2Pu[FIxyqEQvF2= M1PwN|HDqGh? NY\BSm9SemWmdXPld{B1cGViZYjwdoV{e2mxbjDv[kBCXEZ|IIDyc5RmcW5? NXvnVWhEOjV2NEe4NVY>
HCT-15 M{XM[2Z2dmO2aX;uJGF{e2G7 MUOxJIg> Mm\yZZR1\W63YYTld{BRT0V{LXnu[JVk\WRicHjvd5Bpd3K7bHH0bY9vKG:oIFXyb:Kh MlvlNlU1OzF2MkW=
HCT-15 MYjBdI9xfG:|aYOgRZN{[Xl? NVzIW|VuOSCq NWC5dVJw[WKxbHnzbIV{KHSqZTDwdo91\WO2aY\lJIVn\mWldIOgc4YhWEeHMtMgZYdicW6|dDDjeZJkfW2rbj3pcoR2[2WmIHHwc5B1d3Orcx?= NGPWcmgzPTR|MUSyOS=>
786-O MkH4RZBweHSxc3nzJGF{e2G7 MkDBOVDDqM7:TR?= NXq2TnZoOjRiaB?= NH\RNpVxd3SnboTpZZRme8LidHjlJJBzdy2jcH;weI91cWNiZX\m[YN1eyCxZjDORy=> NGGySpAzPDVyOES3Oi=>
A498 NUPvO3lqSXCxcITvd4l{KEG|c3H5 NICxNWg2OMLizszN MVGyOEBp M{P3fpBwfGWwdHnheIV{yqC2aHWgdJJwNWGyb4D0c5Rq[yCnZn\lZ5R{KG:oIF7D NWnWToNtOjR3MEi0O|Y>
NHBE MojsSpVv[3Srb36gRZN{[Xl? M3e0UlIwOjBizszN NHjoOpczKGh? M1nGboF1fGWwdXH0[ZMhUUxvM{Ogd5RqdXWuYYTl[EBEYEOOOD;JUE05KHOnY4LleIlwdg>? MV:yOFQ4QTV{Nh?=
A375 NHi2UJRE\WyuIFnueoF{cW:wIFHzd4F6 Mn3BNVDjiJN{MDFCuW0> NGnTc2MzPCCq NEnifW5z\WS3Y3XzJI1mdGGwb33hJINmdGxiaX72ZZNqd25? NWTCdoc1OjR2Nk[wN|Y>
HBMEC M3:yV2Z2dmO2aX;uJGF{e2G7 MY[xNEDPxE1? M4C1eFEhcA>? MnO3Zoxw[2u|IG\FS2YucW6mdXPl[EBGeGiDMjDlfJBz\XO|aX;u MYWyOFQ2QDl6Mh?=
HPAEpiCs  NFfBVI9HfW6ldHnvckBCe3OjeR?= NGjTbVA{OCEQvF2= NXPNW4V2OSCq NHzhVZhqdmirYnn0d{BVVkZvzsGgd5RqdXWuYYTl[EBxPDJxcES0JG1CWEticHjvd5Bpd3K7bHH0bY9v NVW1NXo3OjR2NEG4O|A>
BeWo M{DqdGZ2dmO2aX;uJGF{e2G7 MYKxNOKh|ryP NEn3fIgzKGh? MkmwbY5pcWKrdIOgSXJMOS9{ M3GwfFI1PDN|OES2
PC3  MWPBdI9xfG:|aYOgRZN{[Xl? NUTLdlB6PTBizszN M4j1dVAvPSCq MVPpcohq[mm2czDNTHkuPDR7LXnu[JVk\WRiYYDvdJRwe2m|wrC= MoTkNlQ1OjR6OEm=
HGC-27 MV\BdI9xfG:|aYOgRZN{[Xl? NWPGfIVXOSEEtV2= NIDVUmoyKGh? NXy4VFM5e3WycILld5NmeyCUQVSwNFEheGy3czDNT{0zOjB4LXnu[JVk\WRiY3XscEB3cWGkaXzpeJkhdG:|cx?= NEPBcnQzPDRzNkO0PS=>
MCF-7 NXXmbFQ2TnWwY4Tpc44hSXO|YYm= NYTNVVI5OTEEoN88US=> NGTVV3YyOC9|MDDtbY4> M4C0eZJm\HWlZYOgeIhmKFWWUD3k[ZBmdmSnboSgSXJMKHCqb4PwbI9zgWyjdHnvci=> NHzYRXEzPDN7MEixPS=>
HUVECs M13OWmZ2dmO2aX;uJGF{e2G7 NV7XN4ExOTEEoN88US=> NHrVXmQyKGh? M1nrWolvcGmkaYTzJJRp\SCKRFygdoVlfWOnZDDDU3guOiCneIDy[ZN{cW:wIHHu[EBRT0lvMjDy[Yxm[XOn NFyzXZAzPDN6NUGwPS=>
HeLa MV;GeY5kfGmxbjDBd5NigQ>? MYC1NEDPxE1? M{ixSVAvPSCq MWjicI9kc3NiVGLYMVEhdnWlbHXhdkBucWe{YYTpc44h[W6mIGTYUmlRKGSxd36tdoVofWyjdHnvci=> NEP1SYgzPDN5NkiyOy=>
HL-60  M{K5cGZ2dmO2aX;uJGF{e2G7 M1\ucVExNzJyIN88US=> MmL3NUBp M3f6[IlvcGmkaYTzJJRp\cLiTj6gZ4hqdmWwc3nz[Zh1emGldNMgbY5lfWOnZDDkbYZn\XKnboTpZZRqd25iaX70c{BoemGwdXzvZ5l1\XN? NGXzdGgzPDN3N{CyNC=>
HL-60 NETFbJVHfW6ldHnvckBCe3OjeR?= NV\0ZZlUOiEEtV2= NF\iV24yPiCq NIfaPYNFVVOR M1zOdYlvcGmkaYTzJJRp\SCjc4PvZ4lifGmxbjDv[kBxWzZ{MTDSZYYuOSCjbnSgUmZCXGN|LDDhcoQhfGinIGLBMYlv\HWlZXSgdIhwe3Cqb4L5cIF1cW:wIH;mJI52[2ynYYKgUmZCXGN| NVe0NYN4OjR|M{CwOlg>
HEK 293 MWTGeY5kfGmxbjDBd5NigQ>? MWWxNEDPxE1? Mki2OUBp MVPEUXNQ NF\GfFNqdmirYnn0d{BYdnRvaX7keYNm\CEQsj3jZZRmdmmwL2TDSlQh[WO2aY\peJkh[W6mIH71Z4xm[XJizsKtZ4F1\W6rbjDhZ4N2dXWuYYTpc44> NX;NcVJjOjR|MkSzOlY>
HEK 293 M2XONmZ2dmO2aX;uJGF{e2G7 MVKxNEDPxE1? M1PLZlUhcA>? NIrMd2dFVVOR M2DEb5N2eHC{ZYPz[ZMhfGinIFPSWEBi[3Srdnn0fS=> M3P6RlI1OzJ2M{[2
SW480 NYjndW5lTnWwY4Tpc44hSXO|YYm= MlzPNVAh|ryP M3nreVIxKGh? MV3EUXNQ MYnzeZBxemW|c3XzJJRp\SCFUmSgZYN1cX[rdIm= NInlZoEzPDN{NEO2Oi=>
HCSMCs M3vaSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWmxNEDPxE1? NI\6[oczPCCq M1rsXYJtd2OtczDGRWJRPC2rbnT1Z4VlKEiFQWPNR{Bxem:uaX\ldoF1cW:w MmHQNlQ{OTJ|OEG=
PANC-1 NELDPHNHfW6ldHnvckBCe3OjeR?= MljlNlAh|ryP MlT4OFghcA>? M{nNRolvcGmkaYTzJJRp\SCneIDy[ZN{cW:wIH;mJO6VPkRiaX6gdoV{eG:wc3WgeI8hfGinIGDQRXLPvMLiYXfvcol{fMLi NVnXZ|M6OjR{OUSxN|M>
A549 NFrwcIRHfW6ldHnvckBCe3OjeR?= NFjEZlQ{OCEQvF2= M2rxR|AvPSCq NWfqRnBVTE2VTx?= MlX2bY5pcWKrdIOgeIhmKHSqcn;tZolvNWmwZIXj[YQhUUxvOD;DXGNNQC2OdXOgZYN1cX[rdIm= NULEZWM4OjR{N{e2PVY>
A549 NUTLZ5VsTnWwY4Tpc44hSXO|YYm= MkPsN|Ah|ryP MlHPNE42KGh? NGPycGRFVVOR NITkRZdqdmirYnn0d{B1cHKxbXLpck1qdmS3Y3XkJGMwTUKSzsKgWIhzOjN3wrDwbI9{eGixconsZZRqd25? MkXENlQzPzd4OU[=
MC-3 MnTaRZBweHSxc3nzJGF{e2G7 M17ENVExKM7:TR?= M4LqflI1KGh? MX\wc5RmdnSrYYTl[EBOTVOFLXnu[JVk\WRiYYDvdJRwe2m|IHnuJEBk\Wyucx?= M2m4bFI1OjdyNUKz
Raji  NEfmT|ZHfW6ldHnvckBCe3OjeR?= MmDGNVAh|ryP NXLuNpRLOSCq MWricI9kc3NiaIPCRWZHKGmwZIXj[YQhTXKtMT:yJJBpd3OyaH;yfYxifGmxbh?= NH7mXVYzPDJ4OU[zNC=>
Raji  M4TKOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVOxNEDPxE1? MlnKNUBp MmTYbY5pcWKrdIOgeIhmKGKjc3HsJI9zKGi|QlHGSk1{fGmvdXzheIVlKGOnbHygdJJwdGmoZYLheIlwdiCjbnSgeoli[mmuaYT5 NGXtUFAzPDJ4OU[zNC=>
HT29 NV7neXJXTnWwY4Tpc44hSXO|YYm= NFvve2gyOCEQvF2= NIjzdlIzKGh? NYjZSW17cW6qaXLpeJMhd2ZiSlHLNkwhTVKNMT:yJIFv\CCVVFHUN{BxcG:|cHjvdplt[XSrb36= MmH3NlQzPjV{OUO=
HepG2 MnjuRZBweHSxc3nzJGF{e2G7 MnTWNlAh|ryP NU\SO3o{OjRiaB?= NIS0eIpqdmirYnn0d{BGWktzL{KgdIhwe3Cqb4L5cIF1cW:wIHHu[EBmdmijbnPld{BXSjFvaX7keYNm\CCjcH;weI9{cXN? MYeyOFI1PzlyOR?=
HepG2 NXe5TFU6TnWwY4Tpc44hSXO|YYm= MXuyNEDPxE1? NGXMepMzKGh? NXW1SHBF\W6qYX7j[ZMhXkJzLXnu[JVk\WRiRl;YU|NiKHS{YX7zZ5JqeHSrb37hcEBi[3Srdnn0fS=> MoP4NlQzPDd7MEm=
TE4 NXHzSFhwTnWwY4Tpc44hSXO|YYm= M1zXdlIxNzVyL{GwNEDPxE1? M32zUFQ5KGh? NHPnXYFFVVOR M3LCc4lvcGmkaYTzJJAuTXKtIHHu[EB4d3K2bXHucolvKGSxd37y[Yd2dGG2ZXSgdE1Cc3RiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NHX5RYkzPDJ2NECyNy=>
TE1 MlnQSpVv[3Srb36gRZN{[Xl? NFT4OWozOC93MD:xNFAh|ryP MlPWOFghcA>? MoXDSG1UVw>? MmnNbY5pcWKrdIOgdE1GemtiYX7kJJdwenSvYX7ubY4h\G:5boLl[5Vt[XSnZDDwMWFsfCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MW[yOFI1PDB{Mx?=
KYSE30 NWHxXXVrTnWwY4Tpc44hSXO|YYm= MU[yNE82OC9zMECg{txO MX20PEBp MmflSG1UVw>? Mmf3bY5pcWKrdIOgdE1GemtiYX7kJJdwenSvYX7ubY4h\G:5boLl[5Vt[XSnZDDwMWFsfCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? Moi2NlQzPDRyMkO=
TE1 MlfRSpVv[3Srb36gRZN{[Xl? MWO1NEDPxE1? NUXOcmZiPDhiaB?= MVHEUXNQ NHvOfIh2eHKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCKTFGgZ4xie3NiSR?= MXyyOFI1PDB{Mx?=
TE3 MmDQSpVv[3Srb36gRZN{[Xl? NFTuR|I2OCEQvF2= M1T5PFQ5KGh? M33jdmROW09? NIGzdld2eHKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCKTFGgZ4xie3NiSR?= MYqyOFI1PDB{Mx?=
TE4 MWXGeY5kfGmxbjDBd5NigQ>? MmH5OVAh|ryP MlfTOFghcA>? MYHEUXNQ MXL1dJJm\3WuYYTld{B1cGViZYjwdoV{e2mxbjDv[kBJVEFiY3zhd5MhUQ>? NF7rSnIzPDJ2NECyNy=>
TE5 NED6OIFHfW6ldHnvckBCe3OjeR?= NHXXTHU2OCEQvF2= Mn;aOFghcA>? NYXQS4hzTE2VTx?= M3WxV5VxemWpdXzheIV{KHSqZTDlfJBz\XO|aX;uJI9nKEiOQTDjcIF{eyCL NXq5UmFvOjR{NESwNlM>
KYSE30 MnG0SpVv[3Srb36gRZN{[Xl? M33VdVUxKM7:TR?= M2ixWVQ5KGh? NIDNeXVFVVOR M{jndZVxemWpdXzheIV{KHSqZTDlfJBz\XO|aX;uJI9nKEiOQTDjcIF{eyCL MmjJNlQzPDRyMkO=
MKN7 MYfGeY5kfGmxbjDBd5NigQ>? NVLUXlFIPTBizszN MnmyOFghcA>? NEPBNmxFVVOR M{f3dolv[3KnYYPld{BmgHC{ZYPzbY9vKG:oIFjMRU1CODJib4KgTGxCNUF{NDDtc4xm[3WuZYO= Mkf1NlQzPDRyMkO=
OE19 NYLPNXVJTnWwY4Tpc44hSXO|YYm= M1juRVUxKM7:TR?= NIPTXmE1QCCq NEPtfVlFVVOR NVvxSY1HcW6lcnXhd4V{KGW6cILld5Nqd25ib3[gTGxCNUFyMjDvdkBJVEFvQUK0JI1wdGWldXzldy=> M{GxVFI1OjR2MEKz
KATOIII  M1u1PWZ2dmO2aX;uJGF{e2G7 MVW1NEDPxE1? NUW1TWd[PDhiaB?= Mnm1SG1UVw>? M2HIT4lv[3KnYYPld{BmgHC{ZYPzbY9vKG:oIFjMRU1CODJib4KgTGxCNUF{NDDtc4xm[3WuZYO= MoT0NlQzPDRyMkO=
NCI-N87  MUTGeY5kfGmxbjDBd5NigQ>? MoL1OVAh|ryP MmXwOFghcA>? NYL4RXFJTE2VTx?= MmPzbY5kemWjc3XzJIV5eHKnc4Ppc44hd2ZiSFzBMWExOiCxcjDIUGEuSTJ2IH3vcIVkfWyncx?= MXGyOFI1PDB{Mx?=
NUGC3 MX;GeY5kfGmxbjDBd5NigQ>? MlzoOVAh|ryP NUHLWFVnPDhiaB?= NEDs[nhFVVOR MYPpcoNz\WG|ZYOg[ZhxemW|c3nvckBw\iCKTFGtRVAzKG:{IFjMRU1COjRibX;s[YN2dGW| M{jzflI1OjR2MEKz
NUGC2 NFHYSIxHfW6ldHnvckBCe3OjeR?= MXW1NEDPxE1? NI\wT241QCCq NYjQZWJ1TE2VTx?= MVPpcoNz\WG|ZYOg[ZhxemW|c3nvckBw\iCKTFGtRVAzKG:{IFjMRU1COjRibX;s[YN2dGW| MXOyOFI1PDB{Mx?=
SGC-7901  NXr4RoEySXCxcITvd4l{KEG|c3H5 NXfrUHNoOjBizszN NGj4bFgzPCCq NFS3eVdqdmirYnn0d{BEWC2vZXTpZZRm\CCjcH;weI9{cXN? MViyOFI1OTN3MR?=
MG-63 M{\mOmZ2dmO2aX;uJGF{e2G7 MWSyNEDPxE1? MkfFNE42KGh? NGjzeJJjdG:la4OgeIhmKEOKLXnu[JVk\WRicHjvd5Bpd3K7bHH0[YQhTUyNMTDwdo91\WmwIHX4dJJme3Orb36= MmP1NlQzOzl4NEC=
ARPE-19 M3zvWmZ2dmO2aX;uJGF{e2G7 NV7CTZVrOjBizszN M33vSVAvPSCq MnHCbY5pcWKrdIOgRZBmdGmwLXnu[JVk\WRicHjvd5Bpd3K7bHH0bY9vKG:oIFXyb{BidmRiQXv0 NWTaXohMOjR{Mke5NVg>
CRL-2302 NHjjSlBHfW6ldHnvckBCe3OjeR?= MmPwNlAh|ryP MoTFNE42KGh? NHXIPZhqdmirYnn0d{BCeGWuaX6tbY5lfWOnZDDwbI9{eGixconsZZRqd25ib3[gSZJsKGGwZDDBb5Q> NF3o[HgzPDJ{N{mxPC=>
MCF-7 MXrGeY5kfGmxbjDBd5NigQ>? Ml;LNlAh|ryP M2nJXFEhcA>? MXrhZo9tcXOqZYOg[ZhxemW|c3nvckBw\iCyaH;zdIhwenmuYYTl[EBGWktiY3:teJJm[XSvZX70JJdqfGhiY3;ubpVo[XSn MV2yOFIyPjJ6OR?=
MCF-7 NHzheIlCeG:ydH;zbZMhSXO|YYm= NYDvUWJKOjBizszN NGr2cXoyKGh? Ml3FbY5kemWjc3XzJINie3Cjc3WtPUBmdnq7bXWgZYN1cX[rdIm= MnXNNlQzOTZ{OEm=
DLD-1  MVPGeY5kfGmxbjDBd5NigQ>? Mn\lNlDDqM7:TR?= M{XvV|Q5KGh? MoPWdoVlfWOnczD0bIUhSk6LUEOg[ZhxemW|c3nvckBxemVvdILlZZRm\CC5aYToJFUu[XqjLXTD M{jGcFI1OjFzNUix
HT-29 NIS3NnBHfW6ldHnvckBCe3OjeR?= MVyyNOKh|ryP Ml;WOFghcA>? MlTOdoVlfWOnczD0bIUhSk6LUEOg[ZhxemW|c3nvckBxemVvdILlZZRm\CC5aYToJFUu[XqjLXTD MYKyOFIyOTV6MR?=
7402 M3HJc2Fxd3C2b4Ppd{BCe3OjeR?= MVGzNEDPxE1? MkPJOUBl NH23b|hl\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9v MUKyOFIyOTJ3Mx?=
7721 NUPaR5c1SXCxcITvd4l{KEG|c3H5 NYTkWm11OzBizszN M1fETFUh\A>? M2L0eoRm[3KnYYPld{Bk\WyuIIDyc4xq\mW{YYTpc44> MYGyOFIyOTJ3Mx?=
SGC7901  M3PnbWFxd3C2b4Ppd{BCe3OjeR?= NEjpcWw2OMLizszN NID5XJMzPC92OD:3NkBp NXrHbWxYTE2VTx?= NFHQU5RqdmS3Y3XzJIFxd3C2b4Ppd{Bkd22kaX7l[EB4cXSqIFrBT|Ihe2iUTlG= NHLEN|UzPDF5OEK0NC=>
SMMC7721 NHTDcmdHfW6ldHnvckBCe3OjeR?= MX6yOU82OCEQvF2= NV3B[mpIOjRiaB?= NGfBWJJ{fXCycnXzd4V{KHSqZTDlfJBz\XO|aX;uJI9nKHBvQXv0JI9zKHBvRWLLNU8zyqB? MWKyOFE3QDB3Nh?=
MCF-7 NFn6eVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGP3bVYyOCEQvF2= MYG0PIg> M{L5RWROW09? MU\y[ZZmenOnczDCUmYucW6mdXPl[EBk\WyuIHP5Z4xmKGG{cnXzeC=> M3\nXlI1OTZ|NEC0
Caco-2 NGGzRllHfW6ldHnvckBCe3OjeR?= NWO3PY5wPTEEoN88US=> MUW0PIg> NVrmV2EyTE2VTx?= M3\kcIVvcGGwY3XzJJRp\SCvUl7BJIxmfmWuczDv[uKhW0OQTkHBMGZZYUR|LNMgUGNVNMLiTF;YMOKhUEmIM1GsxsBbTzF4LNMgVGRGPkIEoHHu[OKhVEeDTGOxOuKh\2WwZYRCpINwNXS{ZXH0[YQhf2m2aDDE[Zg> NVj0ZYtGOjRzNkG2PVU>
HAECs MoP3SpVv[3Srb36gRZN{[Xl? NV3mR|h2OTBizszN Mo\PNUBp MmPSxsBifHSnboXheIV{KFSQRj5OtU1{fGmvdXzheIVlKEmFQV2tNUBidmRiVlPBUU0yKGW6cILld5Nqd25? M1O2[VI1OTN2NkW3
Ca9-22 M1nF[2Z2dmO2aX;uJGF{e2G7 M3rofFMh|ryP M3fBfVEhcA>? NWTPdGxC[WKxbHnzbIV{KHSqZTDhZoltcXS7IH;mJGhjWiC2bzDpcoR2[2ViSVytPEBxem:mdXP0bY9v M{\TNlI1OTJ4NUOy
Ca9-22 Mk\vSpVv[3Srb36gRZN{[Xl? Mkj4N{DPxE1? NXrCR3NROS9{IHi= M{nGTpJm\HWlZYOgTIJTNWmwZIXj[YQhSVSILUKgdIhwe3Cqb4L5cIF1cW:w NF3wcG0zPDF{NkWzNi=>
AGS NW\XUXRFTnWwY4Tpc44hSXO|YYm= MWGxNEDPxE4EoB?= MW[wMlUhcA>? NILWRnRqdmirYnn0d{B1cGVidYDy[Yd2dGG2aX;uJI9nKHSqZTDJUE05KGenbnW= M4DiWlI1OTB4MU[2
Caco-2  NEHUeYdCeG:ydH;zbZMhSXO|YYm= Mkj2NVDDqM7:TR?= MoSzNlTDqGh? MknP[IVkemWjc3XzJINmdGxiYYDvdJRwe2m|IHnu[JVk\WRiYomgOU1HXQ>? MlKyNlQxQTV6NkO=
HCT-8 NIDCUGRCeG:ydH;zbZMhSXO|YYm= MmnENVDDqM7:TR?= MVmyOOKhcA>? MoHt[IVkemWjc3XzJINmdGxiYYDvdJRwe2m|IHnu[JVk\WRiYomgOU1HXQ>? NX\2enhHOjRyOUW4OlM>
A549 M2fHe2Z2dmO2aX;uJGF{e2G7 M3P1cVUxyqEQvF2= NHHsTVAzKGh? Mm\xZoxw[2u|IFXST{BxcG:|cHjvdplt[XSrb36gcYVlcWG2ZXSgZpkhOSx{LV7R M1G0dFI1ODZ5N{K3
HPMC M3;EfGZ2dmO2aX;uJGF{e2G7 M2PmT|ExyqEQvF2= NF;5b3Y1QCCq MWny[ZZmenOnczD0bIUh[2ijbnfld{BqdiClZXzsJI1wenCqb3zv[5khcW6mdXPl[EBjgSCKR2DEVy=> NEHPNHMzPDB2MkizPC=>
HPMC NFvPO3JCeG:ydH;zbZMhSXO|YYm= M37tZVExyqEQvF2= M{\2UFI1yqCq NHz0cFJz\X[ncoPld{Bl\WO{ZXHz[UBqdiClZXzsJJZq[WKrbHn0fUBqdmS3Y3XkJIJ6KEiJUFTT NVXPRppXOjRyNEK4N|g>
MGC803  MorWRZBweHSxc3nzJGF{e2G7 MojZNlDDqM7:TR?= NWrwZ2NuOSCq NV;G[Gp1cW6qaXLpeJMh[XCxcITvd4l{KGmwZIXj[YQh[nliSV\OMe6yyqCjbnSgOgKBui2GRmXS NEXxTXkzPDB{N{e1NC=>
SGC7901 NFfwNGJCeG:ydH;zbZMhSXO|YYm= MoX4NlDDqM7:TR?= NHm2TosyKGh? NXHNPIxUcW6qaXLpeJMh[XCxcITvd4l{KGmwZIXj[YQh[nliSV\OMe6yyqCjbnSgOgKBui2GRmXS MXGyOFAzPzd3MB?=
COLO205 NGX6OGNCeG:ydH;zbZMhSXO|YYm= NYjW[XRbOTBxMkCvOFAh|ryP M3OyfVI1KGh? NVv4UnBUcW6mdXPld{BFVkFibHHk[IVzKG[xcn3heIlwdg>? MUGyOFAyQTFyOB?=
G292  MnrtRZBweHSxc3nzJGF{e2G7 NUPJV|VDOzEEoN88US=> MWGyJIg> MoTMdoV{fG:{ZYOgZ4Fxe2GrY3nuMYlv\HWlZXSgZ4VtdCCmZXH0bC=> NVT3WoN6OjRyMUK5N|A>
BxPC-3 M3zTXGZ2dmO2aX;uJGF{e2G7 Mn24NVAh|ryPwrC= NHTQZpU3KGh? MWfpcoNz\WG|ZTDtbXIuOTR|IHX4dJJme3Orb36= NFXaVnIzOzl5M{exNC=>
HPAF-II NVqxeYM2TnWwY4Tpc44hSXO|YYm= MX6xNEDPxE4EoB?= NYPTfmtDPiCq NIrhe4xqdmO{ZXHz[UBucVJvMUSzJIV5eHKnc4Ppc44> MWmyN|k4OzdzMB?=
HL-60 MYrBdI9xfG:|aYOgRZN{[Xl? NEjhSm42OMLizszN MlnYNUBp MVHy[ZNkfWW|IFLBNVQ2KG2nZHnheIVlKGGyb4D0c5Nqew>? MXSyN|k1QDd3MR?=
HepG2 MVzGeY5kfGmxbjDBd5NigQ>? M1\5b|QxKM7:TR?= MnzZOk8yOiCq NEXpcopqdmirYnn0d{B1cGViaX7jdoVie2Vib3[gdE1GWktzIHHu[EBxNWNvSoXuJJBzd3SnaX6g[ZhxemW|c3nvckBjgSCSTB?= M3jPb|I{QTR{OEWx
HUVECs MV\GeY5kfGmxbjDBd5NigQ>? NH;jTlIzPSEQvF2= M3HqclEhcA>? Mn\2bY5kemWjc3WgUmYu|rqEIIC2OUBvfWOuZXHyJJRz[W6|bH;jZZRqd25? MUGyN|kxOTByOB?=
LNCaP  MYPGeY5kfGmxbjDBd5NigQ>? NWfidWxlOTBizszNxsA> NY[yZpBTOSCq MkS2[IVkemWjc3XzJJRp\SCHR1[geZBz\We3bHH0[YQheC2\Qj2x NWj0Rmx3OjN6M{izNVg>
HL60  M{PzPWZ2dmO2aX;uJGF{e2G7 M17WOVIxyqEQvF2= NH[y[mg4OiCq MW\EUXNQ NF61fmRqdmirYnn0d{Bl[XOjdHnubYIucW6mdXPl[EBETDFzYjDlfJBz\XO|aX;u MU[yN|gzPTV6NR?=
NB4  Mn6ySpVv[3Srb36gRZN{[Xl? NIHZcGoyOCEQvF5CpC=> MUe3NkBp MXjEUXNQ NF\pN5hqdmirYnn0d{Bl[XOjdHnubYIucW6mdXPl[EBETDFzYjDlfJBz\XO|aX;u NX;WW25UOjN6MkW1PFU>
EPOR/CR3 NWi5TJptTnWwY4Tpc44hSXO|YYm= NWHlVY0{PTEEoN88US=> NG\wNpY{KGh? NU[3b2JwemWmdXPld{BGWE9iYX7kM49zKEmOLUOtbY5lfWOnZDD0bIUhfHm{b4PpcoUheGixc4Doc5J6dGG2aX;uxsA> NVGwWIV3OjN6MkC3N|E>
HUASMCs MmTISpVv[3Srb36gRZN{[Xl? MV:xNEDPxE4EoB?= M2\2WFI1KGh? NVTjPWlH\GmvaX7pd4hmeyCDbnegTWku[2G3c3XkJHNQS1N|IH3SUmEh[W6mIIDyc5RmcW5iZYjwdoV{e2mxbtMg MWSyN|gyPjR4OB?=
HUASMCs MXrGeY5kfGmxbjDBd5NigQ>? MlX3NVAh|ryPwrC= M3\lcVI1KGh? NV35b3htcW6qaXLpeJMhSW6pIFnJMYlv\HWlZXSgSXJMOS9{IIDoc5NxcG:{eXzheIlwdiCuZY\lcC=> NGnWdngzOzhzNkS2PC=>
SGC7901 MVXGeY5kfGmxbjDBd5NigQ>? NIrlb|QyOCEQvF5CpC=> Ml7wNlQhcA>? NWi3NGJUcW6qaXLpeJMhfGinIHX4dJJme3Orb36gc4YheGixc4Doc5J6dGG2ZXSgSXJMOS9{ NFT5VZYzOzd7MkW4PC=>
MKN45 MoPWSpVv[3Srb36gRZN{[Xl? NGnMe28yOCEQvF5CpC=> NELheXkzPCCq M37hWolvcGmkaYTzJJRp\SCneIDy[ZN{cW:wIH;mJJBpd3OyaH;yfYxifGWmIFXST|EwOg>? MnjjNlM4QTJ3OEi=
SGC7901 MlezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU[xNEDPxE4EoB?= M1;HcFI1NzR6L{eyJIg> MULpcohq[mm2czDj[YxtKGe{b4f0bEBkdy22cnXheIVlKHerdHigSGFRXA>? MXGyN|c6OjV6OB?=
MKN45 NWnFdpdoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkHWNVAh|ryPwrC= NHLIV2ozPC92OD:3NkBp NYDQfJJDcW6qaXLpeJMh[2WubDDndo94fGhiY3:teJJm[XSnZDD3bZRpKESDUGS= M13uSlI{Pzl{NUi4
SGC7901 MUfBdI9xfG:|aYOgRZN{[Xl? NUTMN|V1OTBizszNxsA> Mmm3NlQhcA>? NV7KdXk1cW6lcnXhd4V{KHSqZTDERXBVNWmwZIXj[YQh[2WubDDhdI9xfG:|aYO= MnGxNlM4QTJ3OEi=
MKN45 NIi3dnNCeG:ydH;zbZMhSXO|YYm= MmT3NVAh|ryPwrC= NISyVmwzPCCq MUTpcoNz\WG|ZYOgeIhmKESDUGStbY5lfWOnZDDj[YxtKGGyb4D0c5Nqew>? NXzkN29nOjN5OUK1PFg>
BxPC-3 cells NGXBNJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPTU2RoOjEEoN88US=> MWKwMlUhcA>? Moe3bY5pcWKrdIOgWmVITi2DLYLl[5Vt[XSnZDDIWXZGSyCpcn;3eIgh[W6mIIT1ZoUh\m:{bXH0bY9vKGmwZIXj[YQh[nliUFHSMVIhSVB? M1\jPVI{PzZ2MES2
NB4  MlTVRZBweHSxc3nzJGF{e2G7 NWPad|YzOTBxMkCvOlAh|ryP Ml\ENU42KGh? M{HZPWROW09? Mofr[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHPvMZRz\WG2ZXSge4l1cCCSYXPsbZRigGWu NX\nTYx5OjN5M{W1OFE>
HepG2  NGHUVY9HfW6ldHnvckBCe3OjeR?= MUSyNOKh|ryP MVOyOEBp M{jlNIlvcGmkaYTzJJRp\SCKTz2xJJBzd3SnaX6g[ZhxemW|c3nvckBkdy22cnXheIVlKHerdHigcYV1\m:{bXnu MVuyN|cxPzZyOR?=
HUVECs MVTBdI9xfG:|aYOgRZN{[Xl? NYrQeZJNOi92IN88US=> MnviNlQwPDhiaB?= NH7o[opqdmS3Y3XzJINmdGxiZHXheIg> M1\3fFI{PzB5NUKw
KG-1  M1\3W2Fxd3C2b4Ppd{BCe3OjeR?= NH\jVWkzOMLizszN NUHpfHZYOTJiaB?= MU\lcohidmOnczDj[YxtKGGyb4D0c5NqeyCrbnT1Z4VlKGK7IGOx NXzuS|R6OjN5ME[2PVE>
AML 1# M3nKOGFxd3C2b4Ppd{BCe3OjeR?= MkTZNlDDqM7:TR?= NFn3fG4yOiCq M4rY[4VvcGGwY3XzJINmdGxiYYDvdJRwe2m|IHnu[JVk\WRiYomgV|E> M{LpSVI{PzB4Nkmx
A2780  Mn\SSpVv[3Srb36gRZN{[Xl? M1y3O|IxyqEQvF2= NWP3UYFKOSCq M37wc4Jtd2OtczDEWGNFNWmwZIXj[YQhTFJ3IHX4dJJme3Orb36= MVSyN|Y6Pjh4Mh?=

... 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

Molarity Calculator

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

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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:

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Molecular Weight Calculator

Molecular Weight 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