YL-5092 is a YTHDC1 inhibitor (IC50=7.4 nM, KD=29.6 nM) that suppresses cancer cell proliferation, induces G0/G1 phase arrest and apoptosis, and can be used in studies of acute myeloid leukemia (AML).

YTHDC1:7.4 nM, YTHDC1:29.6 nM (Kd)

YL-5092 inhibits acute myeloid leukemia cells with an IC50 of 0.28–2.87 μM [1].
YL-5092 (1 μM) blocks YTHDC1 binding to its substrates (m6A-mRNAs) in HEK293T cells and reduces MYC mRNA levels in MOLM-13 cells [1].
YL-5092 (0.25–2 μM, 48–120 h) induces G0/G1 phase arrest and increases apoptotic cell numbers in MOLM-13 cells[1].
YL-5092 (1–3 μM, 14–16 days) inhibits colony-forming capacity of CD34+ cells[1].
GW2974 (0.5–50 μM, 3 h) exhibits significant cytotoxicity at ≥10 μM. At 0.5–5 μM, it inhibits proliferation of U87MG and U251MG cells after 24 h and impairs GBM cell invasion and migration [1].

Methods: YL-5092 was administered at 70 mg/kg via intraperitoneal injection twice daily for 18 days in a mouse MOLM-13/U937 tumor xenograft model.
Results: YL-5092 inhibited leukemia development and improved survival in the MOLM-13/U937 tumor xenograft model in mice [1].