A PCA-1 inhibitor
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HUHS015 is an inhibitor of prostate cancer antigen-1 (PCA-1; IC50 = 0.67 ?M), also known as α-ketoglutarate-dependent dioxygenase alkB homolog 3 (ALKBH3).1 It inhibits proliferation of DU145 human prostate cancer cells by 54 and 81% in 2D dish and 3D agar assays, respectively when used at a concentration of 10 ?M. HUHS015 (32 mg/kg) reduces tumor growth in a DU145 mouse xenograft model.
1.Nakao, S., Mabuchi, M., Shimizu, T., et al.Design and synthesis of prostate cancer antigen-1 (PCA-1/ALKBH3) inhibitors as anti-prostate cancer drugsBioorg. Med. Chem. Lett.24(4)1071-1074(2014)
LX1606 Hippurate (Telotristat etiprate)
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