For research use only. Not for therapeutic Use.
PD-184161(Cat No.:R051791)is a potent and selective inhibitor of MEK1 and MEK2, which are critical components of the MAPK/ERK signaling pathway. By inhibiting MEK, PD-184161 effectively blocks downstream ERK phosphorylation, leading to reduced cell proliferation and increased apoptosis, particularly in tumors dependent on MAPK signaling. It has demonstrated antitumor activity in various cancer models, including hepatocellular carcinoma and other solid tumors. PD-184161 is a valuable research tool for studying the role of MEK/ERK signaling in cancer biology and evaluating the therapeutic potential of MEK inhibition in targeted cancer therapies.
Catalog Number | R051791 |
CAS Number | 212631-67-9 |
Synonyms | 5-Bromo-2-[(2-chloro-4-iodophenyl)amino]-N-(cyclopropylmethoxy)-3,4-difluorobenzamide; |
Molecular Formula | C17H13BrClF2IN2O2 |
Purity | ≥95% |
Target | MEK1/2 |
Solubility | Soluble in DMSO |
Storage | Store at -20°C |
IUPAC Name | 5-bromo-2-(2-chloro-4-iodoanilino)-N-(cyclopropylmethoxy)-3,4-difluorobenzamide |
InChI | InChI=1S/C17H13BrClF2IN2O2/c18-11-6-10(17(25)24-26-7-8-1-2-8)16(15(21)14(11)20)23-13-4-3-9(22)5-12(13)19/h3-6,8,23H,1-2,7H2,(H,24,25) |
InChIKey | VJNZMSLGVUSPCF-UHFFFAOYSA-N |
SMILES | C1CC1CONC(=O)C2=CC(=C(C(=C2NC3=C(C=C(C=C3)I)Cl)F)F)Br |
Reference | </br>1: Matsushita H, Matsuzaki M, Han XJ, Nishiki TI, Ohmori I, Michiue H, Matsui H, Tomizawa K. Antidepressant-like effect of sildenafil through oxytocin-dependent cyclic AMP response element-binding protein phosphorylation. Neuroscience. 2012 Jan 3;200:13-8. doi: 10.1016/j.neuroscience.2011.11.001. Epub 2011 Nov 9. PubMed PMID: 22088430.</br>2: Mazharian A, Watson SP, Séverin S. Critical role for ERK1/2 in bone marrow and fetal liver-derived primary megakaryocyte differentiation, motility, and proplatelet formation. Exp Hematol. 2009 Oct;37(10):1238-1249.e5. doi: 10.1016/j.exphem.2009.07.006. Epub 2009 Jul 18. PubMed PMID: 19619605; PubMed Central PMCID: PMC2755112.</br>3: Yip-Schneider MT, Klein PJ, Wentz SC, Zeni A, Menze A, Schmidt CM. Resistance to mitogen-activated protein kinase kinase (MEK) inhibitors correlates with up-regulation of the MEK/extracellular signal-regulated kinase pathway in hepatocellular carcinoma cells. J Pharmacol Exp Ther. 2009 Jun;329(3):1063-70. doi: 10.1124/jpet.108.147306. Epub 2009 Mar 3. PubMed PMID: 19258520.</br>4: Choi J, Yip-Schneider M, Albertin F, Wiesenauer C, Wang Y, Schmidt CM. The effect of doxorubicin on MEK-ERK signaling predicts its efficacy in HCC. J Surg Res. 2008 Dec;150(2):219-26. doi: 10.1016/j.jss.2008.01.029. Epub 2008 Mar 3. PubMed PMID: 18468633.</br>5: Duman CH, Schlesinger L, Russell DS, Duman RS. Voluntary exercise produces antidepressant and anxiolytic behavioral effects in mice. Brain Res. 2008 Mar 14;1199:148-58. doi: 10.1016/j.brainres.2007.12.047. Epub 2008 Jan 3. Erratum in: Brain Res. 2008 Jul 7;1218:313. PubMed PMID: 18267317; PubMed Central PMCID: PMC2330082.</br>6: Duman CH, Schlesinger L, Kodama M, Russell DS, Duman RS. A role for MAP kinase signaling in behavioral models of depression and antidepressant treatment. Biol Psychiatry. 2007 Mar 1;61(5):661-70. Epub 2006 Aug 30. PubMed PMID: 16945347.</br>7: Klein PJ, Schmidt CM, Wiesenauer CA, Choi JN, Gage EA, Yip-Schneider MT, Wiebke EA, Wang Y, Omer C, Sebolt-Leopold JS. The effects of a novel MEK inhibitor PD184161 on MEK-ERK signaling and growth in human liver cancer. Neoplasia. 2006 Jan;8(1):1-8. PubMed PMID: 16533420; PubMed Central PMCID: PMC1601146.</br>8: Thottassery JV, Sun Y, Westbrook L, Rentz SS, Manuvakhova M, Qu Z, Samuel S, Upshaw R, Cunningham A, Kern FG. Prolonged extracellular signal-regulated kinase 1/2 activation during fibroblast growth factor 1- or heregulin beta1-induced antiestrogen-resistant growth of breast cancer cells is resistant to mitogen-activated protein/extracellular regulated kinase kinase inhibitors. Cancer Res. 2004 Jul 1;64(13):4637-47. PubMed PMID: 15231676.</br>9: Yung HW, Wyttenbach A, Tolkovsky AM. Aggravation of necrotic death of glucose-deprived cells by the MEK1 inhibitors U0126 and PD184161 through depletion of ATP. Biochem Pharmacol. 2004 Jul 15;68(2):351-60. PubMed PMID: 15194007.</br>10: Marshall SJ, Senis YA, Auger JM, Feil R, Hofmann F, Salmon G, Peterson JT, Burslem F, Watson SP. GPIb-dependent platelet activation is dependent on Src kinases but not MAP kinase or cGMP-dependent kinase. Blood. 2004 Apr 1;103(7):2601-9. Epub 2003 Dec 18. PubMed PMID: 14684423.</br> |