MD13

MD13 is a macrophage migration inhibitory factor (MIF)-directed PROTAC with a Ki of 71 nM. MD13 can be used for cancer research[1].

Research Areas >> Cancer

Signaling Pathways >> PROTAC >> PROTAC

Ki: 71 nM (MIF)[1]

MD13 degrades 91±5% and 71±7% MIF at 2 μM and 0.2 μM, respectively. MD13 induces MIF degradation through binding to E3 ligase cereblon[1]. MD13 (0-20 μM; 72 h) inhibits cell proliferation of A549 cancer cells[1]. MD13 (1-5 μM; 48 h) arrests cell cycle at G2/M phase in A549 cells[1]. MD13 (2 μM; 6-48 h) inhibits ERK signaling[1]. Western Blot Analysis[1] Cell Line: A549 cells Concentration: 0-20 μM Incubation Time: 12 h Result: Caused depletion of MIF protein. Western Blot Analysis[1] Cell Line: A549 cells Concentration: 2 μM Incubation Time: 6, 24 or 48 h Result: Inhibited ERK phosphorylation. Cell Proliferation Assay[1] Cell Line: A549 cells Concentration: 0-20 μM Incubation Time: 72 h Result: Inhibited the growth of A549 cells in a dose-dependent manner. The inhibitory effect reached about 50% inhibition of cell proliferation at a concentration of 20 µM. Cell Cycle Analysis[1] Cell Line: A549 cells Concentration: 1, 2, or 5 μM Incubation Time: 48 h Result: Dose-dependently induced cell cycle arrest at the G2/M phase.

[1]. Xiao Z, et al. Proteolysis Targeting Chimera (PROTAC) for Macrophage Migration Inhibitory Factor (MIF) Has Anti-Proliferative Activity in Lung Cancer Cells. Angew Chem Int Ed Engl. 2021 Aug 2;60(32):17514-17521.