MI-1148 is a highly potent peptidomimetic inhibitor targeting furin, a proprotein convertase involved in the activation of various precursor proteins, including some implicated in cancer and viral pathogenesis. MI-1148 is a decanoylated peptide derivative (sequence: decanoyl-RVRR-CMK) that exhibits irreversible inhibition of furin by covalent modification of the active site. It shows an apparent Ki of 5.5 pM for furin and displays high selectivity over other proprotein convertases like PC5/6, PACE4, and PC7. In cell-based assays, MI-1148 has demonstrated potent inhibition of furin-dependent cleavage of substrates, effectively blocking activation of pro-VEGF-C and pro-MT1-MMP, both of which are critical for tumor progression. Its optimized structure offers increased metabolic stability compared to earlier furin inhibitors such as dec-RVKR-CMK, making MI-1148 a valuable tool compound for studying furin biology and a potential lead for anti-cancer or antiviral therapeutic development. (Ref: Hardes et al., Bioorg Med Chem Lett. 2015;25(2): 388–392)
MedKoo Cat#: 532182
Name: MI-1148
CAS#: NA
Chemical Formula: C36H57N15O4
Exact Mass: 763.4718
Molecular Weight: 763.95
Elemental Analysis: C, 56.60; H, 7.52; N, 27.50; O, 8.38
The following data is based on the product molecular weight 763.95 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Lam van TV, Ivanova T, Lindberg I, Böttcher-Friebertshäuser E, Steinmetzer T, Hardes K. Design, synthesis, and characterization of novel fluorogenic substrates of the proprotein convertases furin, PC1/3, PC2, PC5/6, and PC7. Anal Biochem. 2022 Oct 15;655:114836. doi: 10.1016/j.ab.2022.114836. Epub 2022 Aug 11. PMID: 35964735.
2: Ivanova T, Hardes K, Kallis S, Dahms SO, Than ME, Künzel S, Böttcher- Friebertshäuser E, Lindberg I, Jiao GS, Bartenschlager R, Steinmetzer T. Optimization of Substrate-Analogue Furin Inhibitors. ChemMedChem. 2017 Dec 7;12(23):1953-1968. doi: 10.1002/cmdc.201700596. Epub 2017 Nov 16. PMID: 29059503.
3: Hardes K, Becker GL, Lu Y, Dahms SO, Köhler S, Beyer W, Sandvig K, Yamamoto H, Lindberg I, Walz L, von Messling V, Than ME, Garten W, Steinmetzer T. Novel Furin Inhibitors with Potent Anti-infectious Activity. ChemMedChem. 2015 Jul;10(7):1218-31. doi: 10.1002/cmdc.201500103. Epub 2015 May 14. PMID: 25974265.
