eg5 mitotic motor protein

ARQ 621 is an allosteric, and selective Eg5 mitotic motor protein inhibitor. Phase 1.

NVP-BQS481 (Compound 1) is a selective inhibitor of spindle motor protein 5 (Eg5), with an IC50 of less than 0.5 nM. It demonstrates significant anti-mitotic and anti-tumor activities, exhibiting an IC50 of 0.09 nM against SK-OV-3ip cells. NVP-BQS481 is suitable for use as a cytotoxic payload in the synthesis of antibody-drug conjugates (ADCs).

AZD4877 is a synthetic kinesin spindle protein (KSP) inhibitor with potential antineoplastic activity. KSP inhibitor AZD4877 selectively inhibits microtubule motor protein KSP (also called kinesin-5 or Eg5), which may result in the inhibition of mitotic spindle assembly; activation of the spindle assembly checkpoint; induction of cell cycle arrest during the mitotic phase; and cell death in tumor cells that are actively dividing. Because KSP is not involved in postmitotic processes, such as neuronal transport, this agent may be less likely to cause the peripheral neuropathy often associated with the tubulin-targeting agents. Eg5 is essential for the formation of bipolar spindles and the proper segregation of sister chromatids during mitosis.