For research use only. Not for therapeutic Use.
PD184352 (Cat No.: I002637) is a potent ATP non-competitive inhibitor of MEK1/2 (Mitogen-Activated Protein Kinase Kinase 1 and 2) with an IC50 of 17 nM in cell assays. Notably, its selectivity for MEK1/2 is approximately 100 times higher than that for MEK5. PD184352’s unique mechanism of action makes it an important tool for researchers studying intracellular signaling pathways. Additionally, it has shown the ability to selectively induce apoptosis in certain contexts. For further information or specific inquiries about PD184352, please don’t hesitate to contact us.
| Catalog Number | I002637 |
| CAS Number | 212631-79-3 |
| Synonyms | 2-(2-chloro-4-iodoanilino)-N-(cyclopropylmethoxy)-3,4-difluorobenzamide |
| Molecular Formula | C₁₇H₁₄ClF₂IN₂O₂ |
| Purity | ≥95% |
| Target | MEK1/2 |
| Solubility | 10 mM in DMSO |
| Storage | room temp |
| IUPAC Name | 2-(2-chloro-4-iodoanilino)-N-(cyclopropylmethoxy)-3,4-difluorobenzamide |
| InChI | InChI=1S/C17H14ClF2IN2O2/c18-12-7-10(21)3-6-14(12)22-16-11(4-5-13(19)15(16)20)17(24)23-25-8-9-1-2-9/h3-7,9,22H,1-2,8H2,(H,23,24) |
| InChIKey | GFMMXOIFOQCCGU-UHFFFAOYSA-N |
| SMILES | C1CC1CONC(=O)C2=C(C(=C(C=C2)F)F)NC3=C(C=C(C=C3)I)Cl |
| Reference | </br>1:The MEK-inhibitor CI-1040 displays a broad anti-influenza virus activity in vitro and provides a prolonged treatment window compared to standard of care in vivo. Haasbach E, Müller C, Ehrhardt C, Schreiber A, Pleschka S, Ludwig S, Planz O.Antiviral Res. 2017 Jun;142:178-184. doi: 10.1016/j.antiviral.2017.03.024. Epub 2017 Apr 2. PMID: 28377100 Free Article</br>2:MEK inhibitor CI-1040 induces apoptosis in acute myeloid leukemia cells in vitro. Wei CR, Ge XF, Wang Y, Li XR.Eur Rev Med Pharmacol Sci. 2016 May;20(10):1961-8. PMID: 27249593 Free Article</br>3:Inhibiting ERK Activation with CI-1040 Leads to Compensatory Upregulation of Alternate MAPKs and Plasminogen Activator Inhibitor-1 following Subtotal Nephrectomy with No Impact on Kidney Fibrosis. Nutter FH, Haylor JL, Khwaja A.PLoS One. 2015 Sep 28;10(9):e0137321. doi: 10.1371/journal.pone.0137321. eCollection 2015. PMID: 26415098 Free PMC Article</br>4:Combination of rapamycin, CI-1040, and 17-AAG inhibits metastatic capacity of prostate cancer via Slug inhibition. Ding G, Feng C, Jiang H, Ding Q, Zhang L, Na R, Xu H, Liu J.PLoS One. 2013 Oct 10;8(10):e77400. doi: 10.1371/journal.pone.0077400. eCollection 2013. PMID: 24130883 Free PMC Article</br>5:Induction of Bim expression contributes to the antitumor synergy between sorafenib and mitogen-activated protein kinase/extracellular signal-regulated kinase kinase inhibitor CI-1040 in hepatocellular carcinoma. Ou DL, Shen YC, Liang JD, Liou JY, Yu SL, Fan HH, Wang DS, Lu YS, Hsu C, Cheng AL.Clin Cancer Res. 2009 Sep 15;15(18):5820-8. doi: 10.1158/1078-0432.CCR-08-3294. Epub 2009 Sep 8. PMID: 19737956 Free Article</br>6:Inhibition of the growth of papillary thyroid carcinoma cells by CI-1040. Henderson YC, Ahn SH, Clayman GL.Arch Otolaryngol Head Neck Surg. 2009 Apr;135(4):347-54. doi: 10.1001/archoto.2009.17. PMID: 19380355 Free PMC Article</br>7:The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901. Barrett SD, Bridges AJ, Dudley DT, Saltiel AR, Fergus JH, Flamme CM, Delaney AM, Kaufman M, LePage S, Leopold WR, Przybranowski SA, Sebolt-Leopold J, Van Becelaere K, Doherty AM, Kennedy RM, Marston D, Howard WA Jr, Smith Y, Warmus JS, Tecle H.Bioorg Med Chem Lett. 2008 Dec 15;18(24):6501-4. doi: 10.1016/j.bmcl.2008.10.054. Epub 2008 Oct 15. PMID: 18952427 </br>8:Inhibitory effects of the mitogen-activated protein kinase kinase inhibitor CI-1040 on the proliferation and tumor growth of thyroid cancer cells with BRAF or RAS mutations. Liu D, Liu Z, Jiang D, Dackiw AP, Xing M.J Clin Endocrinol Metab. 2007 Dec;92(12):4686-95. Epub 2007 Oct 2. PMID: 17911174 </br>9:Assessment of gefitinib- and CI-1040-mediated changes in epidermal growth factor receptor signaling in HuCCT-1 human cholangiocarcinoma by serial fine needle aspiration. Hidalgo M, Amador ML, Jimeno A, Mezzadra H, Patel P, Chan A, Nielsen ME, Maitra A, Altiok S.Mol Cancer Ther. 2006 Jul;5(7):1895-903. PMID: 16891476 Free Article</br>10:The mitogen-activated protein kinase/extracellular signal-regulated kinase kinase inhibitor PD184352 (CI-1040) selectively induces apoptosis in malignant schwannoma cell lines. Mattingly RR, Kraniak JM, Dilworth JT, Mathieu P, Bealmear B, Nowak JE, Benjamins JA, Tainsky MA, Reiners JJ Jr.J Pharmacol Exp Ther. 2006 Jan;316(1):456-65. Epub 2005 Oct 20. PMID: 16239399 Free Article |
