Chemical Name: N-[(2R)-2,3-Dihydroxypropoxy]-3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-benzamide
Biological ActivityPD 0325901 is a potent MEK1 and MEK2 inhibitor. PD 0325901 inhibits MEK activity in mouse colon 26 cells (IC50 = 0.33 nM). PD 0325901 inhibits the growth of melanoma cell lines in vitro and in vivo; induces G1-phase cell cycle arrest and apoptosis in a mouse xenograft model. PD 0325901 also inhibits production of proangiogenic cytokines such as VEGF. PD 0325901 enhances generation of induced pluripotent stem cells (iPSCs). PD 0325901 in combination with Vitamin C sustains mouse ES cells at an undifferentiated and hypomethylated state. PD 0325901 promotes myelin recovery in drug-induced demyelination in vivo in mice model. Orally active.
For more information about how PD 0325901 may be used, see our protocols: Culturing Transcriptomically Distinct Pluripotent mESCs, Highly Efficient Generation of CiPSCs from MEFs, Accelerated Induction of Cortical Neurons from hiPSCs.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
3D mouse embryonic stem cell culture for generating inner ear organoids.
Koehler KR, Hashino E.
A chemical platform for improved induction of human iPSCs.
Lin et al.
The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901.
Barrett et al.
Growth-inhibitor and antiangiogenic activity of the MEK inhibitor PD0325901 in malignant melanoma with or without BRAF mutations.
Ciuffreda et al.
The biological profile of PD 0325901: a second generation analog of CI-1040 with improved pharmaceutical potential.
Sebolt-Leopold et al.
Proc.Amer.Assoc.Cancer Res., 2004;45:925
Citations for PD 0325901
The citations listed below are publications that use Tocris products. Selected citations for PD 0325901 include:
46 Citations: Showing 1 - 10
Stimulation of GHRH Neuron Axon Growth by Leptin and Impact of Nutrition during Suckling in Mice.
Authors: Yves Et al.
Retrotransposon instability dominates the acquired mutation landscape of mouse induced pluripotent stem cells.
Authors: Francisco J Et al.
Nat Commun 2022;13:7470
Dynamic enlargement and mobilization of lipid droplets in pluripotent cells coordinate morphogenesis during mouse peri-implantation development.
Authors: Vincent Et al.
Nat Commun 2022;13:3861
Naïve-like pluripotency to pave the way for saving the northern white rhinoceros from extinction.
Authors: Dmitry Et al.
Sci Rep 2022;12:3100
The human amniotic epithelium confers a bias to differentiate toward the neuroectoderm lineage in human embryonic stem cells.
Authors: Wendy Et al.
TENET: gene network reconstruction using transfer entropy reveals key regulatory factors from single cell transcriptomic data.
Authors: Kyoung-Jae Et al.
Nucleic Acids Res 2021;49:e1
Optimized protocol for naive human pluripotent stem cell-derived trophoblast induction.
Authors: Yasuhiro Et al.
STAR Protoc 2021;2:100921
Cell Surface Mechanics Gate Embryonic Stem Cell Differentiation.
Authors: Jamie A Et al.
Cell Stem Cell 2021;28:209-216.e4
Capturing human trophoblast development with naive pluripotent stem cells in vitro.
Authors: Masaki Et al.
Cell Stem Cell 2021;28:1023-1039.e13
Evaluating totipotency using criteria of increasing stringency.
Authors: Andrea Et al.
Nat Cell Biol 2021;23:49-60
The histone demethylase KDM2B regulates human primordial germ cell-like cells specification.
Authors: Yi Et al.
Int J Biol Sci 2021;17:527-538
Generation of mouse-human chimeric embryos.
Authors: Boyang Et al.
Nat Protoc 2021;16:3954-3980
Human ribonuclease 1 serves as a secretory ligand of ephrin A4 receptor and induces breast tumor initiation.
Authors: Jun Et al.
Nat Commun 2021;12:2788
Cdk5 and GSK3β inhibit fast endophilin-mediated endocytosis.
Authors: Konstantinos Et al.
Nat Commun 2021;12:2424
ERK1/2 Signaling Induces Upregulation of ANGPT2 and CXCR4 to Mediate Liver Metastasis in Colon Cancer.
Authors: Eduard Et al.
Cancer Res 2020;80:4668-4680
A novel cardiomyogenic role for Isl1+ neural crest cells in the inflow tract.
Authors: Joshua M Et al.
Sci Adv 2020;6
Naive Pluripotent Stem Cells Exhibit Phenotypic Variability that Is Driven by Genetic Variation.
Authors: Ludovic Et al.
Cell Stem Cell 2020;27:470-481.e6
Gastruloids: Embryonic Organoids from Mouse Embryonic Stem Cells to Study Patterning and Development in Early Mammalian Embryos.
Authors: Krisztina Et al.
Methods Mol Biol 2020;2258:131-147
Differential gene expression elicited by ZIKV infection in trophoblasts from congenital Zika syndrome discordant twins.
Authors: Mayana Et al.
PLoS Negl Trop Dis 2020;14:e0008424
CHIP mutations affect the heat shock response differently in human fibroblasts and iPSC-derived neurons.
Authors: S Et al.
Dis Model Mech 2020;13
Bisphenol A Induces Agrp Gene Expression in Hypothalamic Neurons through a Mechanism Involving ATF3.
Authors: Denise D Et al.
Efficient generation of thymic epithelium from induced pluripotent stem cells that prolongs allograft survival.
Authors: Haruka Et al.
Sci Rep 2020;10:224
A dose-dependent response to MEK inhibition determines hypoblast fate in bovine embryos.
Authors: Canizo Et al.
BMC Dev Biol 2019;19:13
In vitro establishment of expanded-potential stem cells from mouse pre-implantation embryos or embryonic stem cells.
Authors: Pentao Et al.
Nat Protoc 2019;14:350-378
Basal-type lumenogenesis in extraembryonic endoderm stem cells models the early visceral endoderm.
Authors: Kyoung Hwa Et al.
J Cell Sci 2019;132
Implantation initiation of self-assembled embryo-like structures generated using three types of mouse blastocyst-derived stem cells.
Authors: Zhang Et al.
Nat Commun 2019;10:496
Discordant congenital Zika syndrome twins show differential in vitro viral susceptibility of neural progenitor cells.
Nat Commun 2018;9(1):475
Gain of toxic apolipoprotein E4 effects in human iPSC-derived neurons is ameliorated by a small-molecule structure corrector.
Nat Med 2018;24(5):647
CRISPR-based chromatin remodeling of the endogenous Oct4 or Sox2 locus enables reprogramming to pluripotency.
Authors: Liu Et al.
Cell Stem Cell. 2018;22:252
Distinctive features of lincRNA gene expression suggest widespread RNA-independent functions.
Authors: Tuck Et al.
Life Sci Alliance 2018;1:e201800124
PARK2 Depletion Connects Energy and Oxidative Stress to PI3K/Akt Activation via PTEN S-Nitrosylation.
Authors: Gupta Et al.
Mol Cell 2017;65:999
Gene Resistance to Transcriptional Reprogramming following Nuclear Transfer Is Directly Mediated by Multiple Chromatin-Repressive Pathways.
Authors: Jullien Et al.
Mol Cell 2017;65:873
Stem Cell Differentiation as a Non-Markov Stochastic Process.
Authors: Stumpf Et al.
Cell Syst 2017;5:268
Establishment of mouse expanded potential stem cells.
Authors: Yang Et al.
Derivation of Pluripotent Stem Cells with In Vivo Embryonic and Extraembryonic Potency.
Authors: Jun Et al.
The intrinsically kinase-inactive EPHB6 receptor predisposes cancer cells to DR5-induced apoptosis by promoting mitochondrial fragmentation.
Authors: Zawily Et al.
Poly(I:C) increases the expression of mPGES-1 and COX-2 in rat primary microglia.
Authors: Oliveira Et al.
Stem Cells 2016;13:11
Transient acquisition of pluripotency during somatic cell transdifferentiation with iPSC reprogramming factors.
Authors: Maza Et al.
Nat Biotechnol 2015;33:769
HD iPSC-derived neural progenitors accumulate in culture and are susceptible to BDNF withdrawal due to glutamate toxicity.
Authors: Mattis Et al.
PLoS One 2015;24:3257
Effects of AKT inhibition on HGF-mediated erlo. resistance in non-small cell lung cancer cell lines.
Authors: Holland Et al.
J Cancer Res Clin Oncol 2015;141:615
Functional annotation of native enhancers with a Cas9-histone demethylase fusion.
Authors: Kearns Et al.
Nat Methods 2015;12:401
The bimodally expressed microRNA miR-142 gates exit from pluripotency.
Authors: Sladitschek and Neveu
J Neuroinflammation 2015;11:850
Manganese Superoxide Dismutase Gene Expression Is Induced by Nanog and Oct4, Essential Pluripotent Stem Cells' Transcription Factors.
Authors: Solari Et al.
Mol Syst Biol 2015;10:e0144336
A method to identify and isolate pluripotent human stem cells and mouse epiblast stem cells using lipid body-associated retinyl ester fluorescence.
Authors: Muthusamy Et al.
Stem Cell Reports 2014;3:169
Glycogen synthase kinase 3β and activin/nodal inhibition in human embryonic stem cells induces a pre-neuroepithelial state that is required for specification to a floor plate cell lineage.
Authors: Denham Et al.
Conversion from mouse embryonic to extra-embryonic endoderm stem cells reveals distinct differentiation capacities of pluripotent stem cell states.
Authors: Cho Et al.
Cancer Biol Ther 2012;139:2866
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