HMN-214 (IVX-214) is a potent inhibitor of Polo-like kinase (Plk) with IC50 of 118 nM. HMN-214 shows potent and broad-spectrum anti-tumor activity against various cancer cells, including HeLa, PC-3, DU-145, MIAPaCa-2, U937, MCF-7, A549, and WiDr, with a mean IC50 value of 118 nM. HMN-176 is also cytotoxic to drug-resistant human and murine cell lines, including P388/CDDP, P388/VCR, K2/CDDP, and K2/VP-16, with IC50 values ranging from 143 nM–265 nM. In HeLa cells, HMN-176 (3 μM) blocks cell cycle at G2/M phase. HMN-176 (3 μM) down-regulates the expression of the multi-drug resistance gene (MDR1), due to the disturbance of NF-Y transcription factor binding to the MDR1 promoter. HMN-176 (250 nM–2.5 μM) inhibits meiotic spindle assembly and aster formation of Spisula oocytes. HMN-176 (2.5 μM) also inhibits aster microtubule formation from human centrosomes.
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