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PD 0325901

Catalog #: 4192
46 Citations Datasheet
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4192/10
4192/50
PD 0325901 | CAS No. 391210-10-9 | MEK Inhibitors
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Description: Potent inhibitor of MEK1/2
Alternative Names: PD325901

Chemical Name: N-[(2R)-2,3-Dihydroxypropoxy]-3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-benzamide

Purity: ≥99%

Product Details
Citations (46)
Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

PD 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.

Technical Data

M.Wt:
482.19
Formula:
C16H14F3IN2O4
Solubility:
Soluble to 25 mM in DMSO
Purity:
≥99%
Storage:
Store at -20°C
CAS No:
391210-10-9

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.

Additional Information

Licensing Caveats:
Sold for research purposes under agreement from Pfizer Inc.

Background References

  1. 3D mouse embryonic stem cell culture for generating inner ear organoids.
    Koehler KR, Hashino E.
    Nat Protoc
  2. Inhibition of transforming growth factor beta (TGF-beta) signaling can substitute for Oct4 protein in reprogramming and maintain pluripotency.
    Tan F, Qian C, Tang K, Abd-Allah S, Jing N
    J Biol Chem, 2015;290(7):4500-11.
  3. EHT 1864, a small molecule inhibitor of Ras-related C3 botulinum toxin substrate 1 (Rac1), attenuates glucose-stimulated insulin secretion in pancreatic beta-cells.
    Sidarala V, Veluthakal R, Syeda K, Kowluru A
    Cell Signal, 2015;27(6):1159-67.
  4. Endophilin marks and controls a clathrin-independent endocytic pathway.
    Boucrot E, Ferreira A, Almeida-Souza L, Debard S, Vallis Y, Howard G, Bertot L, Sauvonnet N, McMahon H
    Nature, 2015;517(7535):460-5.
  5. Acetate supplementation induces growth arrest of NG2/PDGFRalpha-positive oligodendroglioma-derived tumor-initiating cells.
    Long P, Tighe S, Driscoll H, Moffett J, Namboodiri A, Viapiano M, Lawler S, Jaworski D
    PLoS ONE, 2013;8(11):e80714.
  6. Increased susceptibility to a? toxicity in neuronal cultures derived from familial Azheimer's disease (PSEN1-A246E) induced pluripotent stem cells
    Enrique Armijo
    Neurosci. Lett, 2016;0(0):.
  7. MTCH2-mediated mitochondrial fusion drives exit from na�ve pluripotency in embryonic stem cells
    A Bahat, A Goldman, Y Zaltsman, DH Khan, C Halperin, E Amzallag, V Krupalnik, M Mullokando, A Silberman, A Erez, AD Schimmer, JH Hanna, A Gross
    Nat Commun, 2018;9(1):5132.
  8. A chemical platform for improved induction of human iPSCs.
    Lin et al.
    Nat.Methods., 2009;6:805
  9. The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901.
    Barrett et al.
    Bioorg.Med.Chem.Lett., 2008;18:6501
  10. Growth-inhibitor and antiangiogenic activity of the MEK inhibitor PD0325901 in malignant melanoma with or without BRAF mutations.
    Ciuffreda et al.
    Neoplasia, 2009;11:720
  11. 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
  12. Hyperglycemia Altered DNA Methylation Status and Impaired Pancreatic Differentiation from Embryonic Stem Cells
    ACH Chen, W Huang, SW Fong, C Chan, KC Lee, WSB Yeung, YL Lee
    International Journal of Molecular Sciences, 2021;22(19):.

Product Datasheets

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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

  1. Stimulation of GHRH Neuron Axon Growth by Leptin and Impact of Nutrition during Suckling in Mice.
    Authors: Yves Et al.
    Nutrients  2023;15
  2. Retrotransposon instability dominates the acquired mutation landscape of mouse induced pluripotent stem cells.
    Authors: Francisco J Et al.
    Nat Commun  2022;13:7470
  3. 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
  4. Naïve-like pluripotency to pave the way for saving the northern white rhinoceros from extinction.
    Authors: Dmitry Et al.
    Sci Rep  2022;12:3100
  5. The human amniotic epithelium confers a bias to differentiate toward the neuroectoderm lineage in human embryonic stem cells.
    Authors: Wendy Et al.
    Elife  2022;11
  6. 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
  7. Optimized protocol for naive human pluripotent stem cell-derived trophoblast induction.
    Authors: Yasuhiro Et al.
    STAR Protoc  2021;2:100921
  8. Cell Surface Mechanics Gate Embryonic Stem Cell Differentiation.
    Authors: Jamie A Et al.
    Cell Stem Cell  2021;28:209-216.e4
  9. Capturing human trophoblast development with naive pluripotent stem cells in vitro.
    Authors: Masaki Et al.
    Cell Stem Cell  2021;28:1023-1039.e13
  10. Evaluating totipotency using criteria of increasing stringency.
    Authors: Andrea Et al.
    Nat Cell Biol  2021;23:49-60
  11. The histone demethylase KDM2B regulates human primordial germ cell-like cells specification.
    Authors: Yi Et al.
    Int J Biol Sci  2021;17:527-538
  12. Generation of mouse-human chimeric embryos.
    Authors: Boyang Et al.
    Nat Protoc  2021;16:3954-3980
  13. 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
  14. Cdk5 and GSK3β inhibit fast endophilin-mediated endocytosis.
    Authors: Konstantinos Et al.
    Nat Commun  2021;12:2424
  15. 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
  16. A novel cardiomyogenic role for Isl1+ neural crest cells in the inflow tract.
    Authors: Joshua M Et al.
    Sci Adv  2020;6
  17. 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
  18. 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
  19. 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
  20. CHIP mutations affect the heat shock response differently in human fibroblasts and iPSC-derived neurons.
    Authors: S Et al.
    Dis Model Mech  2020;13
  21. Bisphenol A Induces Agrp Gene Expression in Hypothalamic Neurons through a Mechanism Involving ATF3.
    Authors: Denise D Et al.
    Neuroendocrinology  2020;111:678-695
  22. Efficient generation of thymic epithelium from induced pluripotent stem cells that prolongs allograft survival.
    Authors: Haruka Et al.
    Sci Rep  2020;10:224
  23. A dose-dependent response to MEK inhibition determines hypoblast fate in bovine embryos.
    Authors: Canizo Et al.
    BMC Dev Biol  2019;19:13
  24. 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
  25. Basal-type lumenogenesis in extraembryonic endoderm stem cells models the early visceral endoderm.
    Authors: Kyoung Hwa Et al.
    J Cell Sci  2019;132
  26. 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
  27. Discordant congenital Zika syndrome twins show differential in vitro viral susceptibility of neural progenitor cells.
    Authors: Caires-J?nior
    Nat Commun  2018;9(1):475
  28. Gain of toxic apolipoprotein E4 effects in human iPSC-derived neurons is ameliorated by a small-molecule structure corrector.
    Authors: Wang
    Nat Med  2018;24(5):647
  29. 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
  30. Distinctive features of lincRNA gene expression suggest widespread RNA-independent functions.
    Authors: Tuck Et al.
    Life Sci Alliance  2018;1:e201800124
  31. PARK2 Depletion Connects Energy and Oxidative Stress to PI3K/Akt Activation via PTEN S-Nitrosylation.
    Authors: Gupta Et al.
    Mol Cell  2017;65:999
  32. 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
  33. Stem Cell Differentiation as a Non-Markov Stochastic Process.
    Authors: Stumpf Et al.
    Cell Syst  2017;5:268
  34. Establishment of mouse expanded potential stem cells.
    Authors: Yang Et al.
    Nature  2017;550:393
  35. Derivation of Pluripotent Stem Cells with In Vivo Embryonic and Extraembryonic Potency.
    Authors: Jun Et al.
    Cell  2017;169:243-257.e25
  36. The intrinsically kinase-inactive EPHB6 receptor predisposes cancer cells to DR5-induced apoptosis by promoting mitochondrial fragmentation.
    Authors: Zawily Et al.
    Oncotarget  2016;7:77865
  37. 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
  38. Transient acquisition of pluripotency during somatic cell transdifferentiation with iPSC reprogramming factors.
    Authors: Maza Et al.
    Nat Biotechnol  2015;33:769
  39. 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
  40. 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
  41. Functional annotation of native enhancers with a Cas9-histone demethylase fusion.
    Authors: Kearns Et al.
    Nat Methods  2015;12:401
  42. The bimodally expressed microRNA miR-142 gates exit from pluripotency.
    Authors: Sladitschek and Neveu
    J Neuroinflammation  2015;11:850
  43. 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
  44. 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
  45. 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.
    Development  2012;30:2400
  46. 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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