Name: PD98059
Price: 188.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    PD98059 is a selective and reversible inhibitor of MAPK-activating enzyme, MAPK/ERK kinase (MEK) that inhibits either basal MEK (GST-MEK1) or a partially activated MEK produced by mutation of serine to glutamate at 218 and 222 residues (GST-MEK-2E) with IC50 values of 10uM [1].PD98059 treatment resulted in distinct changes in cell morphology and density compared to control cells treated with DMSO. PD98059 inhibited proliferation or induced cell death in human leukemic U937 cells. Additionally, PD98059 dose-dependently inhibited the ERK1/2 phosphorylation as well as down-regulated cyclin E/Cdk2 and cyclin D1/Cdk4 levels, resulting in G1 phase arrest and apoptosis induction in U937 cells [2].
    
    [1] Dudley DT1, Pang L, Decker SJ, Bridges AJ, Saltiel AR. A synthetic inhibitor of the mitogen-activated protein kinase cascade. Proc Natl Acad Sci U S A. 1995 Aug 15;92(17):7686-9.
    [2] Moon DO1, Park C, Heo MS, Park YM, Choi YH, Kim GY. PD98059 triggers G1 arrest and apoptosis in human leukemic U937 cells through downregulation of Akt signal pathway. Int Immunopharmacol. 2007 Jan;7(1):36-45. Epub 2006 Sep 8.
- Properties
  - Alternative Name
    
    2-(2-amino-3-methoxyphenyl)chromen-4-one
    
    CAS Number
    
    167869-21-8
    
    Molecular Formula
    
    C16H13NO3
    
    Molecular Weight
    
    267.28
    
    Appearance
    
    A solid
    
    Purity
    
    99.22%
    
    Solubility
    
    insoluble in EtOH; insoluble in H2O; ≥40.23 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Lijuan Zhu, Chenxi Luo, et al. "Inhibition of the NF-κB pathway and ERK-mediated mitochondrial apoptotic pathway takes part in the mitigative effect of betulinic acid on inflammation and oxidative stress in cyclophosphamide-triggered renal damage of mice." Ecotoxicol Environ Saf. 2022 Oct 7;246:114150. PMID: 36215883
    2. Lina Shan, Wenqian Zheng, et al. "BMAL1 promotes colorectal cancer cell migration and invasion through ERK‐and JNK‐dependent c‐Myc expression." Cancer Medicine. 2022 August.
    3. Danhui Liu, Yuzhen Liu, et al. "Trichostatin A promotes esophageal squamous cell carcinoma cell migration and EMT through BRD4/ERK1/2-dependent pathway." Cancer Med. 2021 Aug;10(15):5235-5245. PMID: 34160902
    4. Wenli Yuan, Deyao Deng, et al. "IFNγ/PD-L1 Signaling Improves the Responsiveness of Anti-PD-1 Therapy in Colorectal Cancer: An in vitro Study." Onco Targets Ther. 2021 May 7;14:3051-3062. PMID: 33994797
    5. Qiang Li, Dongmei Yu, et al. "TIPE3 promotes non-small cell lung cancer progression via the protein kinase B/extracellular signal-regulated kinase 1/2-glycogen synthase kinase 3β-β-catenin/Snail axis." Transl Lung Cancer Res. 2021 Feb;10(2):936-954. PMID: 33718034
    6. Qin Yu, Jianzhang Wang, et al. "Recepteur d'origine nantais contributes to the development of endometriosis via promoting epithelial-mesenchymal transition of a endometrial epithelial cells."
    J Cell Mol Med. 2021 Feb;25(3):1601-1612. PMID: 33410267
    7. Lee L, Ramos-Alvarez I, et al. "Neuropeptide bombesin receptor activation stimulates growth of lung cancer cells through HER3 with a MAPK-dependent mechanism." Biochim Biophys Acta Mol Cell Res. 2019 Dec 17;1867(4):118625. PMID: 31862538
    8. Chen P, Zhang H, et al. "Basic Fibroblast Growth Factor Reduces Permeability and Apoptosis of Human Brain Microvascular Endothelial Cells in Response to Oxygen and Glucose Deprivation Followed by Reoxygenation via the Fibroblast Growth Factor Receptor 1 (FGFR1)/ERK Pathway." Med Sci Monit. 2019 Sep 25;25:7191-7201. PMID: 31551405
    9. Lan YY, Wang YQ, et al. "CCR5 silencing reduces inflammatory response, inhibits viability, and promotes apoptosis of synovial cells in rat models of rheumatoid arthritis through the MAPK signaling pathway." J Cell Physiol. 2019 Aug;234(10):18748-18762. PMID: 31066041
    10. Ramos-Alvarez I, Lee L, et al. "Cyclic AMP-dependent protein kinase A and EPAC mediate VIP and secretin stimulation of PAK4 and activation of Na(+),K(+)-ATPase in pancreatic acinar cells." Am J Physiol Gastrointest Liver Physiol. 2019 Feb 1;316(2):G263-G277. PMID: 30520694
    11. Yuan W, Deng D,et al."Hyperresponsiveness to interferon gamma exposure as a response mechanism to anti-PD-1 therapy in microsatellite instability colorectal cancer." Cancer Immunol Immunother. 2018 Nov 7. PMID: 30406373
    12. Wu Y, Liu L, et al. "MicroRNA let-7b inhibits keratinocyte differentiation by targeting IL-6 mediated ERK signaling in psoriasis." Cell Commun Signal. 2018 Sep 15;16(1):58. PMID: 30219085
    13. Ramos-Alvarez I, Jensen RT. "P21-activated kinase 4 in pancreatic acinar cells is activated by numerous gastrointestinal hormones/neurotransmitters and growth factors by novel signaling, and its activation stimulates secretory/growth cascades." Am J Physiol Gastrointest Liver Physiol. 2018 Aug 1;315(2):G302-G317. PMID: 29672153
    14. MXinwei Feng1, Junfeng Lu2, et al. "Mycobacterium smegmatis Induces Neurite Outgrowth and Differentiation in an Autophagy-Independent Manner in PC12 and C17.2 Cells." Front. Cell. Infect. Microbiol., 19 June 2018.
    15. He GR, Lin XK, et al. "Dexmedetomidine impairs Pglycoprotein mediated efflux function in L02 cells via the denosine 5' monophosphate activated protein kinase/nuclear factor κB pathway." Mol Med Rep.2018 Apr;17(4):5049-5056. PMID: 29393492
    16. Zuo Q, Liu J, et al. "AXL/AKT axis mediated-resistance to BRAF inhibitor depends on PTEN status in melanoma." Oncogene. 2018 Mar 19. PMID: 29551771
    17. Wang H, Tian L, et al. "Bone-in-culture array as a platform to model early-stage bone metastases and discover anti-metastasis therapies." Nat Commun. 2017 Apr 21;8:15045. PMID: 28429794
    18. Xia G, Wang X, et al. "Carnosic acid (CA) attenuates collagen-induced arthritis in db/db mice via inflammation suppression by regulating ROS-dependent p38 pathway." Free Radic Biol Med. 2017 Mar 23;108:418-432. PMID: 28343998

PD98059

PD98059

Background

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