ALKBH5-IN-5 is a selective inhibitor of ALKBH5 with an IC50 of 0.62 μM and a Kd of 804 nM. This compound disrupts the interaction between ALKBH5 and its substrates, m6A-RNA and 6mA-DNA, leading to enhanced differentiation and apoptosis in cancer cells, as well as G2-M phase arrest. Notably, ALKBH5-IN-5 reduces the protein levels of TACC3 and MYC while increasing cleaved caspase-3 levels, demonstrating significant antiproliferative effects. Furthermore, it exhibits antitumor activity in xenograft mouse models and is relevant for research into acute myeloid leukemia.
ALKBH5-IN-5 is a selective inhibitor of ALKBH5 with an IC50 of 0.62 μM and a Kd of 804 nM. This compound disrupts the interaction between ALKBH5 and its substrates, m6A-RNA and 6mA-DNA, leading to enhanced differentiation and apoptosis in cancer cells, as well as G2-M phase arrest. Notably, ALKBH5-IN-5 reduces the protein levels of TACC3 and MYC while increasing cleaved caspase-3 levels, demonstrating significant antiproliferative effects. Furthermore, it exhibits antitumor activity in xenograft mouse models and is relevant for research into acute myeloid leukemia.
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