<p>
IMD-0354 is a synthetic selective NF-kB inhibitor.
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<p>
in vitro: IMD-0354 inhibits p65 translocation to the nucleus promoted by FGF2 in PASMCs. Furthermore, the time courses of Erk1/2, MCP-1, and PAI-1 stimulated with FGF2 are each markedly shortened by IMD-0354. IMD-0354 suppresses proliferation and induced apoptosis of PASMCs. IMD-0354 decreases FGF2, PAI-1, t-PA mRNA expressions. IMD-0354 also inhibits the translocation of NF-kB subunit p65 into the nucleus.
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<p>
in vivo: IMD-0354 has potential as a new therapeutic tool for PAH. IMD-0354 improves survival in the PAH rats. IMD-0354 improves physical signs of RVH in the PAH rats. IMD-0354 also decreases medial hypertrophy in the pulmonary arterioles.
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| Catalog Number | I005720 |
| CAS Number | 978-62-1 |
| Synonyms | IMD0354;IMD 0354; |
| Molecular Formula | C15H8ClF6NO2 |
| Purity | 95% |
| Target | IκB/IKK |
| Solubility | 10 mM in DMSO |
| Storage | 3 years -20C powder |
| InChI | InChI=1S/C15H8ClF6NO2/c16-9-1-2-12(24)11(6-9)13(25)23-10-4-7(14(17,18)19)3-8(5-10)15(20,21)22/h1-6,24H,(H,23,25) |
| InChIKey | CHILCFMQWMQVAL-UHFFFAOYSA-N |
| SMILES | O=C(C1=C(O)C=CC(Cl)=C1)NC2=CC(C(F)(F)F)=CC(C(F)(F)F)=C2 |
| Reference | </br>1:IκB kinase β inhibitor, IMD-0354, prevents allergic asthma in a mouse model through inhibition of CD4(+) effector T cell responses in the lung-draining mediastinal lymph nodes. Maślanka T, Otrocka-Domagała I, Zuśka-Prot M, Mikiewicz M, Przybysz J, Jasiecka A, Jaroszewski JJ.Eur J Pharmacol. 2016 Mar 15;775:78-85. doi: 10.1016/j.ejphar.2016.02.023. Epub 2016 Feb 9. PMID: 26868187 </br>2:Activation of histamine H4 receptor inhibits TNFα/IMD-0354-induced apoptosis in human salivary NS-SV-AC cells. Stegajev V, Kouri VP, Salem A, Rozov S, Stark H, Nordström DC, Konttinen YT.Apoptosis. 2014 Dec;19(12):1702-11. doi: 10.1007/s10495-014-1036-6. PMID: 25239604 </br>3:IκB kinase-β inhibitor IMD-0354 beneficially suppresses retinal vascular permeability in streptozotocin-induced diabetic mice. Lennikov A, Hiraoka M, Abe A, Ohno S, Fujikawa T, Itai A, Ohguro H.Invest Ophthalmol Vis Sci. 2014 Sep 9;55(10):6365-73. doi: 10.1167/iovs.14-14671. PMID: 25205865 </br>4:IMD-0354 targets breast cancer stem cells: a novel approach for an adjuvant to chemotherapy to prevent multidrug resistance in a murine model. Gomez-Cabrero A, Wrasidlo W, Reisfeld RA.PLoS One. 2013 Aug 27;8(8):e73607. doi: 10.1371/journal.pone.0073607. eCollection 2013. PMID: 24014113 Free PMC Article</br>5:Pathophysiological roles of nuclear factor kappaB (NF-kB) in pulmonary arterial hypertension: effects of synthetic selective NF-kB inhibitor IMD-0354. Hosokawa S, Haraguchi G, Sasaki A, Arai H, Muto S, Itai A, Doi S, Mizutani S, Isobe M.Cardiovasc Res. 2013 Jul 1;99(1):35-43. doi: 10.1093/cvr/cvt105. Epub 2013 Apr 30. PMID: 23631839 </br>6:An IκB kinase 2 inhibitor IMD-0354 suppresses the survival of adult T-cell leukemia cells. Uota S, Zahidunnabi Dewan M, Saitoh Y, Muto S, Itai A, Utsunomiya A, Watanabe T, Yamamoto N, Yamaoka S.Cancer Sci. 2012 Jan;103(1):100-6. doi: 10.1111/j.1349-7006.2011.02110.x. Epub 2011 Nov 27. PMID: 21951590 Free Article</br>7:The novel NF-κB inhibitor IMD-0354 induces apoptosis in chronic lymphocytic leukemia. Kanduri M, Tobin G, Aleskog A, Nilsson K, Rosenquist R.Blood Cancer J. 2011 Mar;1(3):e12. doi: 10.1038/bcj.2011.9. Epub 2011 Mar 25. PMID: 22829125 Free PMC Article</br>8:IκB kinase β inhibitor IMD-0354 suppresses airway remodelling in a Dermatophagoides pteronyssinus-sensitized mouse model of chronic asthma. Ogawa H, Azuma M, Muto S, Nishioka Y, Honjo A, Tezuka T, Uehara H, Izumi K, Itai A, Sone S.Clin Exp Allergy. 2011 Jan;41(1):104-15. doi: 10.1111/j.1365-2222.2010.03564.x. PMID: 20573155 </br>9:Antiallergic and anti-inflammatory effects of a novel I kappaB kinase beta inhibitor, IMD-0354, in a mouse model of allergic inflammation. Sugita A, Ogawa H, Azuma M, Muto S, Honjo A, Yanagawa H, Nishioka Y, Tani K, Itai A, Sone S.Int Arch Allergy Immunol. 2009;148(3):186-98. doi: 10.1159/000161579. Epub 2008 Oct 10. PMID: 18849610 </br>10:A novel NF-kappaB inhibitor, IMD-0354, suppresses neoplastic proliferation of human mast cells with constitutively activated c-kit receptors. Tanaka A, Konno M, Muto S, Kambe N, Morii E, Nakahata T, Itai A, Matsuda H.Blood. 2005 Mar 15;105(6):2324-31. Epub 2004 Nov 23. PMID: 15561889 Free Article |
