TMX-4100

TMX-4100 is a selective phosphodiesterase 6D (PDE6D) degrader. TMX-4100 shows a high degradation preference for PDE6D with the DC50 values less than 200 nM in MOLT4, Jurkat, and MM.1S cells. TMX-4100 can be used for the research of multiple myeloma[1].

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE)

PDE6D

TMX-4100 (compound 3; 1 μM; 4 h) shows a high degradation preference for PDE6D in MOLT4 cells[1]. TMX-4100 has better proteome-wide degradation selectivity in MOLT4 cells, compare to PDE6D degrader FPFT-2216[1]. TMX-4100 does not impede the growth of KRAS-dependent cell lines (MIA PaCa-2, NCI-H358, AGS, PA-TU-8988T cells)[1]. Western Blot Analysis[1] Cell Line: MOLT4 cells Concentration: 1 μM Incubation Time: 4 hours Result: Showed a high degradation preference for PDE6D. Western Blot Analysis[1] Cell Line: MOLT4, Jurkat, and MM.1S cells Concentration: 0 nM, 40 nM, 200 nM, 1 μM; Incubation Time: 4 hours Result: Showed a high degradation preference for PDE6D with the DC50 value less than 200 nM.

[1]. Teng M, et al. Development of PDE6D and CK1α Degraders through Chemical Derivatization of FPFT-2216. J Med Chem. 2022 Jan 13;65(1):747-756.