PROTAC METTL3-14 degrader 1

PROTAC METTL3-14 degrader 1 (Compound 30) forms a stable ternary complex with recombinant METTL3-MTD/METTL14-MTD and CRBN-TBD, with an EC_max of 70 nM^[1].
PROTAC METTL3-14 degrader 1 potently inhibits the catalytic activity of the full-length recombinant METTL3-METTL14 complex, with an IC₅₀ of 27 nM^[1].
PROTAC METTL3-14 degrader 1 (2-10 μM; 24 h) reduces the m⁶A/A ratio in polyadenylated RNA of MOLM-13 acute myeloid leukemia (AML) cells to approximately 60% of that in the control group upon treatment with 10 μM for 24 h, while treatment with 2 μM causes no significant effect^[1].
PROTAC METTL3-14 degrader 1 (2 μM; 24 h) induces significant METTL3 degradation in THP-1, NOMO-1 and Kasumi-1 acute myeloid leukemia (AML) cells, as well as in PC3 prostate cancer cells at 2 μM for 24 h, but exhibits extremely low activity in DU145 prostate cancer cells^[1].
PROTAC METTL3-14 degrader 1 (0.01-10 μM; 72 h) reduces cell viability of MOLM-13, THP-1, Kasumi-1 AML cells and PC3 prostate cancer cells under the condition of 10 μM treatment for 72 h, while exhibits extremely low activity in DU145 prostate cancer cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.