kinesin eg5

AZD-4877 is a potent spindle kinesin (Eg5) inhibitor with an IC50 value of 2 nM. AZD-4877 is an alternative configuration of Ispinesib that inhibits mitosis, induces the formation of a unipolar spindle phenotype, and mediates apoptosis. AZD-4877 has antitumor activity and inhibits circulating peripheral blood mononuclear cells (PBMC).

S-trityl-L-Cysteine is a non-natural amino acid and an inhibitor of Eg5, also known as KSP and Kif11, a mitotic kinesin necessary for mitotic spindle formation. S-trityl-L-Cysteine inhibits the ATPase activity of Eg5 in basal and microtubule-stimulated states (IC50s = 1,000 and 140 nM, respectively). It is selective for Eg5 over nine other human kinesins in an enzyme-coupled assay. It reversibly inhibits Eg5-driven microtubule sliding velocity with an IC50 value of 500 nM using X. laevis recombinant Eg5. It induces cell cycle arrest in HeLa cells (IC50 = 700 nM), reversibly halting the cell cycle in the mitotic phase by inhibiting the separation of duplicated chromosomes and preventing bipolar spindle formation. S-trityl-L-Cysteine inhibits the growth of cancer cells in vitro when tested against the National Cancer Institute (NCI) 60 human cancer cell line panel (average GI50 = 1.3 μM) and in mouse xenograft models.

Litronesib is a selective inhibitor of mitosis-specific kinesin Eg5. It also has antitumor activity.

Monastrol ((±)-Monastrol) is a potent and cell-permeable inhibitor of the mitotic kinesin Eg5.

Eg5-IN-1 is a potent inhibitor of the kinesin family of motor proteins (Eg5) with an IC50 value of 1.97 µM for Eg5.Eg5-IN-1 can be used in cancer research.

Litronesib is a selective, allosteric inhibitor of kinesin Eg5.Litronesib (Racemate) is the racemate of litronesib.

HR22C16 is an effective, selective, and cell-permeable mitotic kinesin Eg5 inhibitor.

Filanesib (ARRY-520) targets the kinesin spindle protein (KSP) with potential antineoplastic activity. ARRY-520 specifically inhibits KSP (kinesin-5 or Eg5), resulting in activation of the spindle assembly checkpoint, induction of cell cycle arrest during

BDPSB is a highly efficient photocontroller of mitotic kinesin Eg5 ATPase activity.

Dimethylenastron, an Eg5 inhibitor, arrests cells with monopolar spindles to which all chromosomes attach in a syntelic manner.

K858 Racemic (K858) is a selective mitotic kinesin Eg5 inhibitor which acts in an ATP-noncompetitive manner.

Monastrol is a potent and cell-permeable inhibitor of the mitotic kinesin Eg5.

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

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.

PVZB1194, a biphenyl-type inhibitor of Kinesin spindle protein Eg5 (KIF11), exhibits anticancer potential by inducing cell cycle arrest and apoptosis through inhibiting Eg5 ATPase activity. It binds to the α4 α6 allosteric pocket and demonstrates ATP-competitive activity [1].