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Chemical Structure| 167869-21-8 Chemical Structure| 167869-21-8

Structure of PD98059
CAS No.: 167869-21-8

Chemical Structure| 167869-21-8

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PD98059 is a non-ATP competitive MEK inhibitor with IC50 of 2 μM, specifically inhibits MEK-1-mediated activation of MAPK and does not directly inhibit ERK1 or ERK2.

Synonyms: NSC 679828

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Product Details of PD98059

CAS No. :167869-21-8
Formula : C16H13NO3
M.W : 267.28
SMILES Code : O=C1C=C(C2=CC=CC(OC)=C2N)OC3=C1C=CC=C3
Synonyms :
NSC 679828
MDL No. :MFCD00671789
InChI Key :QFWCYNPOPKQOKV-UHFFFAOYSA-N
Pubchem ID :4713

Safety of PD98059

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P264-P270-P301+P312-P330-P501

Related Pathways of PD98059

MAPK

Isoform Comparison

Biological Activity

Target
  • MEK1

    MEK1, IC50:2 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
MIA-PaCa-2 cells 25 µM PD98059 completely blocked KIF15-mediated pancreatic cancer cell proliferation PMC5520515
PANC-1 cells 25 µM PD98059 completely blocked KIF15-mediated pancreatic cancer cell proliferation PMC5520515
Human intrahepatic biliary epithelial cells (HIBEpiCs) 10 μM 24 h Pretreatment with PD98059 reduced apelin-induced ERK phosphorylation and cholangiocyte proliferation PMC9288669
Y79 cells 0.1 µM, 0.2 µM, 0.39 µM, 0.78 µM, 1.56 µM, 3.12 µM, 6.25 µM, 12.5 µM 22 h To evaluate the effects of PD98059 on the metabolic activity and cytotoxicity of Y79 cells. PD98059 significantly inhibited cellular metabolic activity at a concentration of 3.12 µM or higher, but did not significantly increase cytotoxicity. PMC9516241
HuPMCs cells 0.1 µM, 0.2 µM, 0.39 µM, 0.78 µM, 1.56 µM, 3.12 µM, 6.25 µM, 12.5 µM 22 h To evaluate the effects of PD98059 on the metabolic activity and cytotoxicity of huPMCs cells. PD98059 did not significantly inhibit cellular metabolic activity at concentrations up to 12.5 µM, nor did it significantly increase cytotoxicity. PMC9516241
MIO-M1 cells 0.1 µM, 0.2 µM, 0.39 µM, 0.78 µM, 1.56 µM, 3.12 µM, 6.25 µM, 12.5 µM 22 h To evaluate the effects of PD98059 on the metabolic activity and cytotoxicity of MIO-M1 cells. PD98059 significantly inhibited cellular metabolic activity at a concentration of 1.56 µM or higher, but did not significantly increase cytotoxicity. PMC9516241
U87 cells 5 μM 12 h To investigate the effect of PD98059 on RRM2 overexpression in U87 cells, the results showed that PD98059 inhibited the phosphorylation of ERK1/2 and blocked the upregulation of cyclin B1, cyclin D1, and N-cadherin expression induced by RRM2 overexpression. PMC6367584
Human adipose-derived stem cells (hASCs) 5 μM 48 h To investigate the effect of PD98059 on FGF-2-mediated proliferation of hASCs, results showed that PD98059 significantly inhibited FGF-2-mediated cell proliferation. PMC6882332
Human adipose tissue-derived stem cells (hADSCs) 40 μM 30 min PD98059 abolished the ERK1/2 phosphorylation and proliferation induced by silica NPs PMC4378289

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Photo-oxidative damage model Intravitreal injection 100 µM Single injection, lasting 4 days To evaluate the protective effects of PD98059 on the retina of photo-oxidative damage mice. PD98059 significantly inhibited the phosphorylation of pERK1/2, reduced the expression of the gliotic marker GFAP in Müller cells, and increased the levels of the neuroprotective factor IRBP in photoreceptors. PD98059 also reduced photoreceptor apoptosis in photo-oxidative damage mice and assessed its protective effects on retinal function through OCT and ERG. PMC9516241
Balb/c nude mice Orthotopic pancreatic cancer transplantation model Subcutaneous injection 10 mg/kg Once daily for 9 weeks PD98059 blocked KIF15-mediated pancreatic cancer proliferation and prolonged the survival time of mice PMC5520515

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

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10 mM

3.74mL

0.75mL

0.37mL

18.71mL

3.74mL

1.87mL

37.41mL

7.48mL

3.74mL

 

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