W23-1006 is a selective covalent ALKBH5 inhibitor. It binds to the ALKBH5 C200 residue with an IC50 value of 3.848 μM. The inhibitory activity of W23-1006 is approximately 30 times stronger than that of FTO and 8 times greater than that of ALKBH3. W23-1006 is applicable for research in triple-negative breast cancer (TNBC).

W23-1006 (5 μM; 24 h) significantly increases m A abundance in MDA-MB-231 and BT549 cells [1]. At concentrations of 3.16-31.6 μM for 24 hours, W23-1006 inhibits the viability of these cells [1]. W23-1006 at 5 μM effectively reduces colony area and inhibits migration in TNBC cells [1]. Additionally, in the range of 5-10 μM, it induces apoptosis and reduces the G2/M phase in MDA-MB-231 cells [1].

W23-1006, administered at a dose of 25 mg/kg via intraperitoneal injection (i.p.) once daily for 14 consecutive days, exhibits antitumor effects against breast cancer in vivo [1]. Additionally, a similar regimen over 10 days significantly suppresses TNBC lung metastasis [1]. A single dose of 25 mg/kg (i.p.) reveals a half-life (t 1/2) ranging from 0.509 to 0.983 hours, with peak plasma concentration (C max) of 1715-2108 ng/mL reached within 15 minutes in mice [1]. No adverse events or mortalities were observed in Kunming mice (22-27g) administered W23-1006 at doses of 100 mg/kg and 250 mg/kg via intraperitoneal injection [1].