HUHS015

HUHS015 is a novel and potent small molecule inhibitor of prostate cancer antigen-1 (PCA-1), also known as α-ketoglutarate-dependent dioxygenase alkB homolog 3 (ALKBH3), which is a DNA/RNA demethylase. ALKBH3 repairs alkylated DNA and RNA by mediating demethylation of 1-methyladenosine (1-meA) and 3-methylcytosine (3-meC). By inhibiting ALKBH3 activity, HUHS015 disrupts DNA and RNA alkylation repair processes that may play key roles in tumorigenesis and cancer progression. HUHS015 has demonstrated potent anti-proliferative effects against prostate cancer both in vitro (DU145 prostate cancer cell lines) and in vivo (mouse xenograft models) without overt toxicity. It exhibits a synergistic effect in combination with DNA-acting chemotherapeutics such as docetaxel, and its oral bioavailability in rats is approximately 7.2%. HUHS015 emerged from the optimization of a hit compound identified by random screening with recombinant ALKBH3 protein[1][3][5][7][9].

Other names

HUHS-015HUHS015HUHS 015