TM-5441

• CAT Number: I012016
• CAS Number: 1190221-43-2
• Molecular Formula: C21H17ClN2O6
• Molecular Weight: 428.825
• Purity: ≥95%
• Synonyms: TM-5441; TM 5441; TM5441; BMS-790052; BMS-790052; BMS790052; EBP 883; EBP-883; EBP883.;5-chloro-2-(2-(2-((3-(furan-3-yl)phenyl)amino)-2-oxoethoxy)acetamido)benzoic acid
• Solubility: Soluble in DMSO
• Storage: Store at 0-8 °C
• IUPAC Name: 5-chloro-2-[[2-[2-[3-(furan-3-yl)anilino]-2-oxoethoxy]acetyl]amino]benzoic acid
• InChI: InChI=1S/C21H17ClN2O6/c22-15-4-5-18(17(9-15)21(27)28)24-20(26)12-30-11-19(25)23-16-3-1-2-13(8-16)14-6-7-29-10-14/h1-10H,11-12H2,(H,23,25)(H,24,26)(H,27,28)
• InChIKey: BGGMLMAPVODXAU-UHFFFAOYSA-N
• SMILES: C1=CC(=CC(=C1)NC(=O)COCC(=O)NC2=C(C=C(C=C2)Cl)C(=O)O)C3=COC=C3

TM-5441 (Cat.No:I012016), also known as EBP 883 and BMS-790052, is a potent plasminogen activator inhibitor-1 (PAI-1). TM-5441 inhibits several tumor cell lines with IC50 values between 9.7 and 60.3 μM. TM5441 protects against high-fat diet-induced obesity and adipocyte injury in mice.

Reference

1: Ghosh AK, Rai R, Park KE, Eren M, Miyata T, Wilsbacher LD, Vaughan DE. A small molecule inhibitor of PAI-1 protects against doxorubicin-induced cellular senescence. Oncotarget. 2016 Nov 8;7(45):72443-72457. doi: 10.18632/oncotarget.12494. PubMed PMID: 27736799; PubMed Central PMCID: PMC5341920.2: Piao L, Jung I, Huh JY, Miyata T, Ha H. A novel plasminogen activator inhibitor-1 inhibitor, TM5441, protects against high-fat diet-induced obesity and adipocyte injury in mice. Br J Pharmacol. 2016 Sep;173(17):2622-32. doi: 10.1111/bph.13541. Epub 2016 Jul 28. PubMed PMID: 27339909; PubMed Central PMCID: PMC4978161.3: Jeong BY, Uddin MJ, Park JH, Lee JH, Lee HB, Miyata T, Ha H. Novel Plasminogen Activator Inhibitor-1 Inhibitors Prevent Diabetic Kidney Injury in a Mouse Model. PLoS One. 2016 Jun 3;11(6):e0157012. doi: 10.1371/journal.pone.0157012. eCollection 2016. PubMed PMID: 27258009; PubMed Central PMCID: PMC4892642.4: Placencio VR, Ichimura A, Miyata T, DeClerck YA. Small Molecule Inhibitors of Plasminogen Activator Inhibitor-1 Elicit Anti-Tumorigenic and Anti-Angiogenic Activity. PLoS One. 2015 Jul 24;10(7):e0133786. doi: 10.1371/journal.pone.0133786. eCollection 2015. PubMed PMID: 26207899; PubMed Central PMCID: PMC4514594.5: Tsuda K. Letter by Tsuda regarding article, /Plasminogen activator inhibitor-1 antagonist TM5441 attenuates Nω-nitro-L-arginine methyl ester-induced hypertension and vascular senescence/. Circulation. 2014 Aug 26;130(9):e83. doi: 10.1161/CIRCULATIONAHA.113.007940. PubMed PMID: 25156921.6: Eren M, Boe AE, Murphy SB, Place AT, Nagpal V, Morales-Nebreda L, Urich D, Quaggin SE, Budinger GR, Mutlu GM, Miyata T, Vaughan DE. PAI-1-regulated extracellular proteolysis governs senescence and survival in Klotho mice. Proc Natl Acad Sci U S A. 2014 May 13;111(19):7090-5. doi: 10.1073/pnas.1321942111. Epub 2014 Apr 28. PubMed PMID: 24778222; PubMed Central PMCID: PMC4024885.7: Boe AE, Eren M, Murphy SB, Kamide CE, Ichimura A, Terry D, McAnally D, Smith LH, Miyata T, Vaughan DE. Plasminogen activator inhibitor-1 antagonist TM5441 attenuates Nω-nitro-L-arginine methyl ester-induced hypertension and vascular senescence. Circulation. 2013 Nov 19;128(21):2318-24. doi: 10.1161/CIRCULATIONAHA.113.003192. Epub 2013 Oct 3. PubMed PMID: 24092817; PubMed Central PMCID: PMC3933362.