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.. 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 NXOxcXpbTnWwY4Tpc44hSXO|YYm= MVuyOUDPxE1? NFewfmMyKGh? MVvicJVvfHNidHjlJGJc[V2SLXnu[JVk\WRiaX7jdoVie2ViaX6gdIhwe3Cqbz3DbIsyKGGwZDDwbI9{eGixLVXST{BmgHC{ZYPzbY9v MYmyOVc3QTF6MR?=
MCF-7  M3W5[2Z2dmO2aX;uJGF{e2G7 NFr4U2IyOCEQvF2= NGrOdGsyKGh? MWDpcohq[mm2czDJUE0yQC2nbnjhcoNm\CClZXzsJI1q\3KjdHnvci=> NU[4PYhYOjV5MkewNVE>
HepG2  MXPGeY5kfGmxbjDBd5NigQ>? M4K5T|ExKM7:TR?= M2H6e|UhcA>? MXXicI9kc3NicHjvd5Bpd3K7bHH0[YQhVUGSS4OgbY5lfWOnZDDifUBmgG:pZX7veZMhXEeILd8yNS=> M4\6dVI2PTZyNEi4
HepG2  M2flcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVeyNEDPxE1? MlvENlQhcA>? MkDld5VxeHKnc4Pld{BVT0ZvzsKxMYlv\HWlZXSgZ4VtdCCycn;sbYZmemG2aX;uJIFv\CCrbo\hd4lwdg>? MW[yOVU3ODR6OB?=
MDA-MB-231 M2i5T2Z2dmO2aX;uJGF{e2G7 M4\ZXVI2KM7:TR?= NHjwR|MzNTNiaB?= Mm[w[IVkemWjc3XzJJAuTVKNMT:yJIFv\CCVMUCwRVQh\XiycnXzd4lwdg>? NIjhO3EzPTV3NUi3OS=>
SW480 M1jIbWZ2dmO2aX;uJGF{e2G7 NE[zPZYzOMLizszN NILSdIoyyqCq M{X3RpJm\HWlZYOgeIhmKGW6cILld5Nqd25ib3[gRXRHOyCycn;0[Ylv MUGyOVQ1PzhzNh?=
HCT-15 NYPwZnRPTnWwY4Tpc44hSXO|YYm= NFLmcFgyKGh? NGGye|BifHSnboXheIV{KFCJRUKtbY5lfWOnZDDwbI9{eGixconsZZRqd25ib3[gSZJsyqB? NE\tblAzPTR|MUSyOS=>
HCT-15 M4\VS2Fxd3C2b4Ppd{BCe3OjeR?= MUGxJIg> MkLMZYJwdGm|aHXzJJRp\SCycn;0[YN1cX[nIHXm[oVkfHNib3[gVGdGOsLiYXfhbY5{fCCldYLjeY1qdi2rbnT1Z4VlKGGyb4D0c5Nqew>? NIPOeVIzPTR|MUSyOS=>
786-O NHTNT4NCeG:ydH;zbZMhSXO|YYm= MVm1NOKh|ryP M33x[lI1KGh? MoLIdI91\W62aXH0[ZPDqHSqZTDwdo8u[XCxcITveIlkKGWoZnXjeJMhd2ZiTlO= M{W2blI1PTB6NEe2
A498 NFHQdVNCeG:ydH;zbZMhSXO|YYm= NXG5OldMPTEEoN88US=> Mki2NlQhcA>? NILqOJlxd3SnboTpZZRme8LidHjlJJBzdy2jcH;weI91cWNiZX\m[YN1eyCxZjDORy=> NInaOmszPDVyOES3Oi=>
NHBE NHnkVGlHfW6ldHnvckBCe3OjeR?= M33t[|IwOjBizszN NXq1boZpOiCq NXrwXokx[XS2ZX71ZZRmeyCLTD2zN{B{fGmvdXzheIVlKEO[Q1y4M2lNNThic3XjdoV1cW:w MmfpNlQ1Pzl3Mk[=
A375 NVLZSXZiS2WubDDJcpZie2mxbjDBd5NigQ>? NYHycY1MOTEkgKOyNEDDvU1? NHW0XokzPCCq MojUdoVlfWOnczDt[Yxidm:vYTDj[YxtKGmwdnHzbY9v M1K2WFI1PDZ4MEO2
HBMEC NFTMbI5HfW6ldHnvckBCe3OjeR?= MojRNVAh|ryP M1jTSVEhcA>? MmD2Zoxw[2u|IG\FS2YucW6mdXPl[EBGeGiDMjDlfJBz\XO|aX;u NUHtR2Y1OjR2NUi5PFI>
HPAEpiCs  NFy0V4FHfW6ldHnvckBCe3OjeR?= MYmzNEDPxE1? MoPNNUBp Mny1bY5pcWKrdIOgWG5HNc7zIIP0bY12dGG2ZXSgdFQzN3B2NDDNRXBMKHCqb4PwbI9zgWyjdHnvci=> NIeyfm0zPDR2MUi3NC=>
BeWo M3\ROGZ2dmO2aX;uJGF{e2G7 NHvRemMyOMLizszN M3ey[FIhcA>? MkS1bY5pcWKrdIOgSXJMOS9{ MY[yOFQ{Ozh2Nh?=
PC3  Ml;5RZBweHSxc3nzJGF{e2G7 NVflWlJvPTBizszN M3;BTFAvPSCq NXLOZZlpcW6qaXLpeJMhVUi\LUS0PU1qdmS3Y3XkJIFxd3C2b4Ppd:Kh M4H4O|I1PDJ2OEi5
HGC-27 MWfBdI9xfG:|aYOgRZN{[Xl? NYi1fJlSOSEEtV2= MVyxJIg> M2n5OpN2eHC{ZYPz[ZMhWkGGMECxJJBtfXNiTVutNlIxPi2rbnT1Z4VlKGOnbHygeoli[mmuaYT5JIxwe3N? Mo\LNlQ1OTZ|NEm=
MCF-7 MXvGeY5kfGmxbjDBd5NigQ>? MXOxNOKh|ryP M4jLS|ExNzNyIH3pci=> Mn\TdoVlfWOnczD0bIUhXVSSLXTldIVv\GWwdDDFVmsheGixc4Doc5J6dGG2aX;u MWWyOFM6ODhzOR?=
HUVECs Mn7kSpVv[3Srb36gRZN{[Xl? MnLqNVDDqM7:TR?= NVLJXXhuOSCq M1LsSYlvcGmkaYTzJJRp\SCKRFygdoVlfWOnZDDDU3guOiCneIDy[ZN{cW:wIHHu[EBRT0lvMjDy[Yxm[XOn NIezfWczPDN6NUGwPS=>
HeLa NUL1SoU1TnWwY4Tpc44hSXO|YYm= Mkm2OVAh|ryP NV\hVWd{OC53IHi= M2nNVIJtd2OtczDUVnguOSCwdXPs[YFzKG2rZ4LheIlwdiCjbnSgWHhPUVBiZH;3ck1z\We3bHH0bY9v Mnv1NlQ{PzZ6Mke=
HL-60  MlfmSpVv[3Srb36gRZN{[Xl? MXyxNE8zOCEQvF2= NYn6SnlqOSCq M3m2fYlvcGmkaYTzJJRp\cLiTj6gZ4hqdmWwc3nz[Zh1emGldNMgbY5lfWOnZDDkbYZn\XKnboTpZZRqd25iaX70c{BoemGwdXzvZ5l1\XN? NV7hfmY4OjR|NUewNlA>
HL-60 MkTaSpVv[3Srb36gRZN{[Xl? M{nJSlIhyrWP MXmxOkBp MoPHSG1UVw>? NHHxUIdqdmirYnn0d{B1cGViYYPzc4Nq[XSrb36gc4YheFN4MkGgVoFnNTFiYX7kJG5HSVSlMzygZY5lKHSqZTDSRU1qdmS3Y3XkJJBpd3OyaH;yfYxifGmxbjDv[kBvfWOuZXHyJG5HSVSlMx?= NH3hSVEzPDN|MEC2PC=>
HEK 293 NX3UTWxFTnWwY4Tpc44hSXO|YYm= MXixNEDPxE1? MWi1JIg> NXjrZ3lCTE2VTx?= MYjpcohq[mm2czDXcpQucW6mdXPl[EDPui2lYYTlcolvN1SFRkSgZYN1cX[rdImgZY5lKG63Y3zlZZIh|rJvY3H0[Y5qdiCjY3P1cZVt[XSrb36= MUCyOFMzPDN4Nh?=
HEK 293 NGSxWphHfW6ldHnvckBCe3OjeR?= NXTkboxUOTBizszN M3rybVUhcA>? M36zZ2ROW09? M13tdZN2eHC{ZYPz[ZMhfGinIFPSWEBi[3Srdnn0fS=> MVyyOFMzPDN4Nh?=
SW480 MYPGeY5kfGmxbjDBd5NigQ>? NIDONmEyOCEQvF2= MXSyNEBp NHrxPItFVVOR MmX2d5VxeHKnc4Pld{B1cGViQ2LUJIFkfGm4aYT5 NWjS[XZYOjR|MkSzOlY>
HCSMCs M3n2ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrpNVAh|ryP NEPSUFUzPCCq NHnncpRjdG:la4OgSmFDWDRvaX7keYNm\CCKQ1HTUWMheHKxbHnm[ZJifGmxbh?= Mk\SNlQ{OTJ|OEG=
PANC-1 M3vsdGZ2dmO2aX;uJGF{e2G7 M3HDNFIxKM7:TR?= NXPJRotZPDhiaB?= NHXKc4FqdmirYnn0d{B1cGViZYjwdoV{e2mxbjDv[kDPnD[GIHnuJJJme3CxboPlJJRwKHSqZTDQVGFT|rUEoHHnc45qe3UEoB?= NVXDO4JVOjR{OUSxN|M>
A549 NXKyWI1sTnWwY4Tpc44hSXO|YYm= MYKzNEDPxE1? NVnCWItROC53IHi= NVryZpBSTE2VTx?= MVjpcohq[mm2czD0bIUhfGi{b33ibY4ucW6mdXPl[EBKVC16L1PYR2w5NUy3YzDhZ5Rqfmm2eR?= NUTRdplwOjR{N{e2PVY>
A549 MnXhSpVv[3Srb36gRZN{[Xl? MYCzNEDPxE1? MmD5NE42KGh? Mn7CSG1UVw>? NUj1cFV[cW6qaXLpeJMhfGi{b33ibY4ucW6mdXPl[EBEN0WEUN8yJHRpejJ|NdMgdIhwe3Cqb4L5cIF1cW:w NYXPOZJqOjR{N{e2PVY>
MC-3 MUjBdI9xfG:|aYOgRZN{[Xl? MXWxNEDPxE1? NUfP[Wx5OjRiaB?= Mmn0dI91\W62aXH0[YQhVUWVQz3pcoR2[2WmIHHwc5B1d3OrczDpckAh[2WubIO= MoK2NlQzPzB3MkO=
Raji  NYTFXIUxTnWwY4Tpc44hSXO|YYm= NE\WTlgyOCEQvF2= NEjafo4yKGh? NF;LXG5jdG:la4OgbJNDSU[IIHnu[JVk\WRiRYLrNU8zKHCqb4PwbI9zgWyjdHnvci=> MYSyOFI3QTZ|MB?=
Raji  MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEK4ZVEyOCEQvF2= NITmOJAyKGh? MUfpcohq[mm2czD0bIUh[mG|YXygc5IhcHOEQV\GMZN1cW23bHH0[YQh[2WubDDwdo9tcW[ncnH0bY9vKGGwZDD2bYFjcWyrdIm= NYDENXU2OjR{Nkm2N|A>
HT29 NX;SSll[TnWwY4Tpc44hSXO|YYm= M33PflExKM7:TR?= M3TQflIhcA>? Ml\SbY5pcWKrdIOgc4YhUkGNMjygSXJMOS9{IHHu[EBUXEGWMzDwbI9{eGixconsZZRqd25? NFrHc4EzPDJ4NUK5Ny=>
HepG2 Mk\uRZBweHSxc3nzJGF{e2G7 NHWyOWkzOCEQvF2= MWKyOEBp M3\lbolvcGmkaYTzJGVTUzFxMjDwbI9{eGixconsZZRqd25iYX7kJIVvcGGwY3XzJHZDOS2rbnT1Z4VlKGGyb4D0c5Nqew>? NI\GVIYzPDJ2N{mwPS=>
HepG2 MWDGeY5kfGmxbjDBd5NigQ>? MXeyNEDPxE1? NGTaVlUzKGh? NGjyNZJmdmijbnPld{BXSjFvaX7keYNm\CCIT2jPN4EhfHKjboPjdolxfGmxbnHsJIFkfGm4aYT5 M3T4TlI1OjR5OUC5
TE4 MmPGSpVv[3Srb36gRZN{[Xl? NYixU2xVOjBxNUCvNVAxKM7:TR?= NHPyOZM1QCCq MkjHSG1UVw>? NXvRZYFLcW6qaXLpeJMheC2HcnugZY5lKHexcoTtZY5vcW5iZH;3cpJm\3WuYYTl[EBxNUGtdDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NF76S3UzPDJ2NECyNy=>
TE1 NIDXcYhHfW6ldHnvckBCe3OjeR?= NEXnS4YzOC93MD:xNFAh|ryP M{fyfFQ5KGh? MUHEUXNQ M2LjbolvcGmkaYTzJJAuTXKtIHHu[EB4d3K2bXHucolvKGSxd37y[Yd2dGG2ZXSgdE1Cc3RiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? Mke1NlQzPDRyMkO=
KYSE30 NVrvN4llTnWwY4Tpc44hSXO|YYm= M3exWlIxNzVyL{GwNEDPxE1? MVG0PEBp Ml;MSG1UVw>? M4C5e4lvcGmkaYTzJJAuTXKtIHHu[EB4d3K2bXHucolvKGSxd37y[Yd2dGG2ZXSgdE1Cc3RiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NYXBRm5COjR{NESwNlM>
TE1 MWHGeY5kfGmxbjDBd5NigQ>? NXzuO2dRPTBizszN MmTSOFghcA>? M13kUmROW09? NIriVYJ2eHKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCKTFGgZ4xie3NiSR?= NYTFNZVoOjR{NESwNlM>
TE3 NILZcYRHfW6ldHnvckBCe3OjeR?= M2nkZlUxKM7:TR?= NUDrUlk1PDhiaB?= NULJVppLTE2VTx?= M17FTJVxemWpdXzheIV{KHSqZTDlfJBz\XO|aX;uJI9nKEiOQTDjcIF{eyCL M2HlXFI1OjR2MEKz
TE4 NGnXO2ZHfW6ldHnvckBCe3OjeR?= M1zTc|UxKM7:TR?= NI\ib2Y1QCCq Mlq0SG1UVw>? NWPFbIRJfXC{ZXf1cIF1\XNidHjlJIV5eHKnc4Ppc44hd2ZiSFzBJINt[XO|IFm= MVyyOFI1PDB{Mx?=
TE5 NFjl[GZHfW6ldHnvckBCe3OjeR?= MXy1NEDPxE1? MmDtOFghcA>? NYnieI8xTE2VTx?= Ml3seZBz\We3bHH0[ZMhfGinIHX4dJJme3Orb36gc4YhUEyDIHPsZZN{KEl? MUiyOFI1PDB{Mx?=
KYSE30 M3\iS2Z2dmO2aX;uJGF{e2G7 M3fubFUxKM7:TR?= NH3BWVU1QCCq MVXEUXNQ NUjKXoJNfXC{ZXf1cIF1\XNidHjlJIV5eHKnc4Ppc44hd2ZiSFzBJINt[XO|IFm= NVHwUZRxOjR{NESwNlM>
MKN7 NF34SFRHfW6ldHnvckBCe3OjeR?= MoLTOVAh|ryP NG\j[Xc1QCCq NG\PT5ZFVVOR MnLBbY5kemWjc3XzJIV5eHKnc4Ppc44hd2ZiSFzBMWExOiCxcjDIUGEuSTJ2IH3vcIVkfWyncx?= Mne1NlQzPDRyMkO=
OE19 M4q2XmZ2dmO2aX;uJGF{e2G7 MU[1NEDPxE1? M{nhRVQ5KGh? NGTCOJRFVVOR M2C0N4lv[3KnYYPld{BmgHC{ZYPzbY9vKG:oIFjMRU1CODJib4KgTGxCNUF{NDDtc4xm[3WuZYO= M2fMbVI1OjR2MEKz
KATOIII  MUfGeY5kfGmxbjDBd5NigQ>? NUjNXW9MPTBizszN M37tclQ5KGh? M3OwO2ROW09? MUHpcoNz\WG|ZYOg[ZhxemW|c3nvckBw\iCKTFGtRVAzKG:{IFjMRU1COjRibX;s[YN2dGW| NGr4WIkzPDJ2NECyNy=>
NCI-N87  NF\DXFFHfW6ldHnvckBCe3OjeR?= NHXQfVg2OCEQvF2= M3TCRVQ5KGh? MUXEUXNQ M4PoUolv[3KnYYPld{BmgHC{ZYPzbY9vKG:oIFjMRU1CODJib4KgTGxCNUF{NDDtc4xm[3WuZYO= NVzWRXNCOjR{NESwNlM>
NUGC3 MVjGeY5kfGmxbjDBd5NigQ>? NGe5Xmw2OCEQvF2= NV\zXXZsPDhiaB?= NHrGNXdFVVOR MU\pcoNz\WG|ZYOg[ZhxemW|c3nvckBw\iCKTFGtRVAzKG:{IFjMRU1COjRibX;s[YN2dGW| NGfvNoEzPDJ2NECyNy=>
NUGC2 Mkj3SpVv[3Srb36gRZN{[Xl? Mnv0OVAh|ryP Ml3OOFghcA>? NWj6cJVQTE2VTx?= MlnibY5kemWjc3XzJIV5eHKnc4Ppc44hd2ZiSFzBMWExOiCxcjDIUGEuSTJ2IH3vcIVkfWyncx?= M{HTVFI1OjR2MEKz
SGC-7901  NH60[mpCeG:ydH;zbZMhSXO|YYm= NWXT[IF{OjBizszN NEP3XmEzPCCq M3vONYlvcGmkaYTzJGNRNW2nZHnheIVlKGGyb4D0c5Nqew>? NIPrNHQzPDJ2MUO1NS=>
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ARPE-19 MXPGeY5kfGmxbjDBd5NigQ>? MWCyNEDPxE1? NHHGXnkxNjViaB?= NYjiToFrcW6qaXLpeJMhSXCnbHnuMYlv\HWlZXSgdIhwe3Cqb4L5cIF1cW:wIH;mJGVzcyCjbnSgRYt1 MV:yOFIzPzlzOB?=
CRL-2302 M4fnb2Z2dmO2aX;uJGF{e2G7 MkftNlAh|ryP NY\mc4FlOC53IHi= MnSwbY5pcWKrdIOgRZBmdGmwLXnu[JVk\WRicHjvd5Bpd3K7bHH0bY9vKG:oIFXyb{BidmRiQXv0 NI\heHczPDJ{N{mxPC=>
MCF-7 MWDGeY5kfGmxbjDBd5NigQ>? MXGyNEDPxE1? M{L3blEhcA>? MnTPZYJwdGm|aHXzJIV5eHKnc4Ppc44hd2ZicHjvd5Bpd3K7bHH0[YQhTVKNIHPvMZRz\WG2bXXueEB4cXSqIHPvcop2\2G2ZR?= NIHKR|IzPDJzNkK4PS=>
MCF-7 NWP6fGZuSXCxcITvd4l{KEG|c3H5 NGPjTnQzOCEQvF2= M2jqTFEhcA>? M3:2VYlv[3KnYYPld{Bk[XOyYYPlMVkh\W68eX3lJIFkfGm4aYT5 NITTdnQzPDJzNkK4PS=>
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HT-29 NXf5PJVqTnWwY4Tpc44hSXO|YYm= M{PzRlIxyqEQvF2= NHLLUoc1QCCq M1fGU5Jm\HWlZYOgeIhmKEKQSWCzJIV5eHKnc4Ppc44heHKnLYTy[YF1\WRid3n0bEA2NWG8YT3kRy=> M2W3VFI1OjFzNUix
7402 MWfBdI9xfG:|aYOgRZN{[Xl? MUmzNEDPxE1? NFfQUnE2KGR? NGnJO25l\WO{ZXHz[ZMh[2WubDDwdo9tcW[ncnH0bY9v M2H4TVI1OjFzMkWz
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SGC7901  MXvBdI9xfG:|aYOgRZN{[Xl? MonMOVDDqM7:TR?= MWGyOE81QC95MjDo MnfpSG1UVw>? M3qwPIlv\HWlZYOgZZBweHSxc3nzJINwdWKrbnXkJJdqfGhiSlHLNkB{cFKQQR?= NXL1OVFFOjRzN{iyOFA>
SMMC7721 NXXLfVRnTnWwY4Tpc44hSXO|YYm= MXKyOU82OCEQvF2= MUCyOEBp M3\IRZN2eHC{ZYPz[ZMhfGinIHX4dJJme3Orb36gc4YheC2Da4Sgc5IheC2HUluxM|LDqA>? MYeyOFE3QDB3Nh?=
MCF-7 Mm\hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLG[pNmOTBizszN MVy0PIg> NWXQeoZxTE2VTx?= MlTBdoV3\XK|ZYOgRm5HNWmwZIXj[YQh[2WubDDjfYNt\SCjcoLld5Q> MXmyOFE3OzRyNB?=
Caco-2 M1TzS2Z2dmO2aX;uJGF{e2G7 MnTiOVDDqM7:TR?= NGfkfZc1QGh? M3;KbGROW09? NInuNFNmdmijbnPld{B1cGVibWLORUBt\X[nbIOgc4bDqFOFTl6xRUxHYFmGMz|CpGxEXC{EoFzPXEzDqEiLRkPBMOKhYkdzNj|CpHBFTT[DwrDhcoTDqEyJQVzTNVbDqGenbnXzxsBkdy22cnXheIVlKHerdHigSIV5 NELoSIEzPDF4MU[5OS=>
HAECs M{XRXWZ2dmO2aX;uJGF{e2G7 NUPu[nBLOTBizszN NVK2c2RQOSCq NHrOd4vDqGG2dHXueYF1\XNiVF7GMe6yNXO2aX31cIF1\WRiSVPBUU0yKGGwZDDWR2FONTFiZYjwdoV{e2mxbh?= MlnSNlQyOzR4NUe=
Ca9-22 NX3BPJVQTnWwY4Tpc44hSXO|YYm= NYDEVIZNOyEQvF2= NGHR[ngyKGh? NUDDcpFS[WKxbHnzbIV{KHSqZTDhZoltcXS7IH;mJGhjWiC2bzDpcoR2[2ViSVytPEBxem:mdXP0bY9v M1XkcVI1OTJ4NUOy
Ca9-22 MVfGeY5kfGmxbjDBd5NigQ>? MmnGN{DPxE1? NVfVZZBmOS9{IHi= MV3y[YR2[2W|IFjiVk1qdmS3Y3XkJGFVTi1{IIDoc5NxcG:{eXzheIlwdg>? MlOwNlQyOjZ3M{K=
AGS Mof2SpVv[3Srb36gRZN{[Xl? NYq3VI9jOTBizszNxsA> NUXNPWVsOC53IHi= M1GyOolvcGmkaYTzJJRp\SC3cILl[5Vt[XSrb36gc4YhfGinIFnMMVgh\2WwZR?= MUmyOFExPjF4Nh?=
Caco-2  MYLBdI9xfG:|aYOgRZN{[Xl? NV[5RXFCOTEEoN88US=> NEiyVIYzPMLiaB?= MVjk[YNz\WG|ZYOgZ4VtdCCjcH;weI9{cXNiaX7keYNm\CCkeTC1MWZW M3rESFI1ODl3OE[z
HCT-8 MmXDRZBweHSxc3nzJGF{e2G7 M1rCdlExyqEQvF2= MX:yOOKhcA>? NW\EXHBL\GWlcnXhd4V{KGOnbHygZZBweHSxc3nzJIlv\HWlZXSgZpkhPS2IVR?= M4\BclI1ODl3OE[z
A549 NX;iPVRwTnWwY4Tpc44hSXO|YYm= NGXTS2E2OMLizszN MX6yJIg> MYHicI9kc3NiRWLLJJBpd3OyaH;yfYxifGmxbjDt[YRq[XSnZDDifUAyNDJvTmG= NIf2VIIzPDB4N{eyOy=>
HPMC M{fCbmZ2dmO2aX;uJGF{e2G7 NYT2N4Z4OTEEoN88US=> NVi2VVZ6PDhiaB?= NVTDT|RzemW4ZYLz[ZMhfGinIHPoZY5o\XNiaX6gZ4VtdCCvb4LwbI9td2e7IHnu[JVk\WRiYomgTGdRTFN? NUK4VIwyOjRyNEK4N|g>
HPMC NGPk[WhCeG:ydH;zbZMhSXO|YYm= MnTuNVDDqM7:TR?= NInvTYYzPMLiaB?= NIm1SlVz\X[ncoPld{Bl\WO{ZXHz[UBqdiClZXzsJJZq[WKrbHn0fUBqdmS3Y3XkJIJ6KEiJUFTT NGjqbZgzPDB2MkizPC=>
MGC803  NF75dG1CeG:ydH;zbZMhSXO|YYm= Ml;ZNlDDqM7:TR?= M4n4cFEhcA>? M2LmbIlvcGmkaYTzJIFxd3C2b4Ppd{BqdmS3Y3XkJIJ6KEmITj5OteKh[W6mIEZihNIuTE[XUh?= MVKyOFAzPzd3MB?=
SGC7901 M{jV[mFxd3C2b4Ppd{BCe3OjeR?= MXiyNOKh|ryP NWP2ZW1jOSCq NYrOPYYzcW6qaXLpeJMh[XCxcITvd4l{KGmwZIXj[YQh[nliSV\OMe6yyqCjbnSgOgKBui2GRmXS MUSyOFAzPzd3MB?=
COLO205 MXjBdI9xfG:|aYOgRZN{[Xl? MmS5NVAwOjBxNECg{txO MnKxNlQhcA>? MnzUbY5lfWOnczDEUmEhdGGmZHXyJIZwem2jdHnvci=> MYGyOFAyQTFyOB?=
G292  NI\kbVhCeG:ydH;zbZMhSXO|YYm= NWfXbpNsOzEEoN88US=> MXOyJIg> M2rvUZJme3SxcnXzJINieHOjaXPpck1qdmS3Y3XkJINmdGxiZHXheIg> NGC0fYUzPDBzMkmzNC=>
BxPC-3 NYjt[oplTnWwY4Tpc44hSXO|YYm= Mn7PNVAh|ryPwrC= MV62JIg> MWDpcoNz\WG|ZTDtbXIuOTR|IHX4dJJme3Orb36= NYDoRY1DOjN7N{O3NVA>
HPAF-II NHX0XJhHfW6ldHnvckBCe3OjeR?= NWXxTJB[OTBizszNxsA> MmT4OkBp Mm\KbY5kemWjc3WgcYlTNTF2MzDlfJBz\XO|aX;u MlXENlM6PzN5MUC=
HL-60 M4e1SWFxd3C2b4Ppd{BCe3OjeR?= NGTGcZE2OMLizszN Ml3NNUBp NYrjV4hxemW|Y4Xld{BDSTF2NTDt[YRq[XSnZDDhdI9xfG:|aYO= M2TVO|I{QTR6N{Wx
HepG2 MmrSSpVv[3Srb36gRZN{[Xl? NFPUWXo1OCEQvF2= M{LVflYwOTJiaB?= NXzCXJJicW6qaXLpeJMhfGinIHnuZ5Jm[XOnIH;mJJAuTVKNMTDhcoQheC2lLVr1ckBxem:2ZXnuJIV5eHKnc4Ppc44h[nliUFy= MUCyN|k1Ojh3MR?=
HUVECs M2DuT2Z2dmO2aX;uJGF{e2G7 MVOyOUDPxE1? NVjIcIVKOSCq MmT3bY5kemWjc3WgUmYu|rqEIIC2OUBvfWOuZXHyJJRz[W6|bH;jZZRqd25? NHO5b|YzOzlyMUCwPC=>
LNCaP  NUfvZotWTnWwY4Tpc44hSXO|YYm= NVjI[|RROTBizszNxsA> MV:xJIg> MnS0[IVkemWjc3XzJJRp\SCHR1[geZBz\We3bHH0[YQheC2\Qj2x NUDIOXg2OjN6M{izNVg>
HL60  M4rWdmZ2dmO2aX;uJGF{e2G7 NGDmUmwzOMLizszN NYq5R3ZIPzJiaB?= NH7PWYNFVVOR MUfpcohq[mm2czDkZZNifGmwaXKtbY5lfWOnZDDDSFEy[iCneIDy[ZN{cW:w MnrBNlM5OjV3OEW=
NB4  NGjER3BHfW6ldHnvckBCe3OjeR?= MVSxNEDPxE4EoB?= NVHocVlzPzJiaB?= NXv6N4FOTE2VTx?= MUfpcohq[mm2czDkZZNifGmwaXKtbY5lfWOnZDDDSFEy[iCneIDy[ZN{cW:w MlXsNlM5OjV3OEW=
EPOR/CR3 M1j6cmZ2dmO2aX;uJGF{e2G7 NFL1Ook2OMLizszN NIjNTGw{KGh? MVjy[YR2[2W|IFXQU{BidmRxb4KgTWwuOy2rbnT1Z4VlKHSqZTD0fZJwe2mwZTDwbI9{eGixconsZZRqd28EoB?= Mn[zNlM5OjB5M{G=
HUASMCs NWKyNJZ{TnWwY4Tpc44hSXO|YYm= Mln2NVAh|ryPwrC= NXnJd25GOjRiaB?= NXHvO4hE\GmvaX7pd4hmeyCDbnegTWku[2G3c3XkJHNQS1N|IH3SUmEh[W6mIIDyc5RmcW5iZYjwdoV{e2mxbtMg NYfCXmh1OjN6MU[0Olg>
HUASMCs MkC5SpVv[3Srb36gRZN{[Xl? Ml34NVAh|ryPwrC= MmrMNlQhcA>? Mlu3bY5pcWKrdIOgRY5oKEmLLXnu[JVk\WRiRWLLNU8zKHCqb4PwbI9zgWyjdHnvckBt\X[nbB?= M3i0RVI{QDF4NE[4
SGC7901 NYT3cmd4TnWwY4Tpc44hSXO|YYm= NF3v[mwyOCEQvF5CpC=> Mn7yNlQhcA>? NH24W|NqdmirYnn0d{B1cGViZYjwdoV{e2mxbjDv[kBxcG:|cHjvdplt[XSnZDDFVmsyNzJ? NVnuToFPOjN5OUK1PFg>
MKN45 MUTGeY5kfGmxbjDBd5NigQ>? NXjCSoRuOTBizszNxsA> MnHZNlQhcA>? NEfaOo9qdmirYnn0d{B1cGViZYjwdoV{e2mxbjDv[kBxcG:|cHjvdplt[XSnZDDFVmsyNzJ? M3vSV|I{Pzl{NUi4
SGC7901 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXJblV7OTBizszNxsA> NH\MXnYzPC92OD:3NkBp M1K5WYlvcGmkaYTzJINmdGxiZ4Lve5RpKGOxLYTy[YF1\WRid3n0bEBFSVCW MkD6NlM4QTJ3OEi=
MKN45 M2rWS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWWxNEDPxE4EoB?= NVnTTod6OjRxNEivO|IhcA>? NVfVe5JwcW6qaXLpeJMh[2WubDDndo94fGhiY3:teJJm[XSnZDD3bZRpKESDUGS= MYCyN|c6OjV6OB?=
SGC7901 NWL2OGJsSXCxcITvd4l{KEG|c3H5 M2XUVVExKM7:TdMg Mn7jNlQhcA>? NH6wWYJqdmO{ZXHz[ZMhfGinIFTBVHQucW6mdXPl[EBk\WyuIHHwc5B1d3Orcx?= NXTrTYNTOjN5OUK1PFg>
MKN45 Mnv4RZBweHSxc3nzJGF{e2G7 MnfpNVAh|ryPwrC= NEL4UGUzPCCq MkHTbY5kemWjc3XzJJRp\SCGQWDUMYlv\HWlZXSgZ4VtdCCjcH;weI9{cXN? NGj0cmwzOzd7MkW4PC=>
BxPC-3 cells M4\DO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mkj5NlDDqM7:TR?= M1jtNlAvPSCq M{LPOolvcGmkaYTzJHZGT0ZvQT3y[Yd2dGG2ZXSgTHVXTUNiZ4Lve5RpKGGwZDD0eYJmKG[xcn3heIlwdiCrbnT1Z4VlKGK7IGDBVk0zKEGS M{T2V|I{PzZ2MES2
NB4  MWnBdI9xfG:|aYOgRZN{[Xl? NUe1RmMxOTBxMkCvOlAh|ryP NUTWd4FsOS53IHi= NFPnUoZFVVOR NEPHR4ll\WO{ZXHz[ZMh[2WubDD2bYFjcWyrdImgZ48ufHKnYYTl[EB4cXSqIGDhZ4xqfGG6ZXy= NXvaZ3BDOjN5M{W1OFE>
HepG2  MXrGeY5kfGmxbjDBd5NigQ>? NIDX[XczOMLizszN Mm[0NlQhcA>? MYjpcohq[mm2czD0bIUhUE9vMTDwdo91\WmwIHX4dJJme3Orb36gZ48ufHKnYYTl[EB4cXSqIH3leIZwem2rbh?= M2DURlI{PzB5NkC5
HUVECs M4W3eWFxd3C2b4Ppd{BCe3OjeR?= MWqyM|Qh|ryP NYLre2RYOjRxNEigbC=> Mlz6bY5lfWOnczDj[YxtKGSnYYTo MlLpNlM4ODd3MkC=
KG-1  M1fRXWFxd3C2b4Ppd{BCe3OjeR?= NFq0VnEzOMLizszN MXSxNkBp NYPVWFFM\W6qYX7j[ZMh[2WubDDhdI9xfG:|aYOgbY5lfWOnZDDifUBUOQ>? MmLxNlM4ODZ4OUG=
AML 1# MWfBdI9xfG:|aYOgRZN{[Xl? NFrUepIzOMLizszN MXqxNkBp MmDs[Y5p[W6lZYOgZ4VtdCCjcH;weI9{cXNiaX7keYNm\CCkeTDTNS=> NWL0e|F[OjN5ME[2PVE>
A2780  NU\TO3F1TnWwY4Tpc44hSXO|YYm= M1;ycFIxyqEQvF2= MnP4NUBp MUXicI9kc3NiRGTDSE1qdmS3Y3XkJGRTPSCneIDy[ZN{cW:w NIPx[ZAzOzZ7Nki2Ni=>

... 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 individually and in order:
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
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
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:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

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

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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  • Computed Result

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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:

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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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