AZ82 is a selective HSET/KIFC1 inhibitor, with a Ki of 43 nM and an IC50 of 300 nM for KIFC1.

Eg5 Inhibitor III, Dimethylenastron is a cell-permeable quinazoline-thione compound that acts as a strong, specific, and reversible inhibitor of the microtubule-stimulated ATPase activity of the mitotic motor, Eg5.

GSK923295 is a first-in-class, specific allosteric inhibitor of CENP-E kinesin motor ATPase with Ki of 3.2 nM, and less potent to mutant I182 and T183.

Ispinesib (SB 715992) is a potent mitotic kinesin KSP (Eg5) inhibitor with a Ki and an IC50 of 0.6 and 4.1 nM, respectively.

K 858 is an ATP-uncompetitive mitotic kinesin Eg5 inhibitor, which does not effect microtubule dynamics.

Kinesore is an inhibitor of the KLC2-SKIP Interaction.

Monastrol is a reversible, cell-permeable inhibitor of the motor protein Eg5 (kinesin family protein 11, Kif11), blocking basal ATPase activity in vitro (IC50 = 6.1 µM) and inducing the formation of monoastral spindles in cell-based assays (IC50 = 51.3 μM

SB743921 is a kinesin spindle protein (KSP) inhibitor with Ki of 0.1 nM, almost no affinity to MKLP1, Kin2, Kif1A, Kif15, KHC, Kif4 and CENP-E.

Azo-EMD is a cell permeable, photoswitchable compound that inhibits mitotic kinesin Eg5 more potently in its light-induced cis form, used for optical control mitosis.Under UV light conditions, HeLa cells undergo mitotic arrest, as evidenced by the formation of a monopolar spindle.

GSK-1 is an ATP-competitive inhibitor of the mitotic kinesin KSP with HCT116 cell IC50 of 36 nM; induces monopolar spindle formation in SKOV3 cells, and shows markedly greater potency (IC50 of 0.5 nM) in the ispinesib-resistant HCT116-D130V cell line.

KIF18A inhibitor 24 is a highly potent, in vivo active inhibitor of mitotic kinesin KIF18A with IC50 of 61 nM.KIF18A inhibitor 24 binds at the interface of KIF18A and tubulin.KIF18A inhibitor 24 exhibits significant mitotic arrest in MDA-MB-157 mitotic cells with EC50 of 11 nM, followed by cell death either in mitosis or in the subsequent interphase, which is sustained for 24 h.

PF-2771 is a potent, selective CENP-E inhibitor with IC50 of 16.1 nM; does not inhibit the ATPase activities of highly related kinesins (Eg5/KSP, chromokinesin and MCAK, IC50> 1 uM); selectively inhibits proliferation of basal breast cancer cell lines; regresses tumor growth correlated with increased phospho-HH3-Ser10 levels in a breast cancer xenograft tumor model.

Kolavenic acid analog (KAA) is an anticancer agent. Kolavenic acid analog shows strong activity against HSET-overproducing yeast cells. Kolavenic acid analog inhibits centrosome clustering in human cancer cells containing high HSET levels and supernumerary centrosomes.

AZD4877 is another isostere to Ispinesib and also a kinesin spindle protein (Eg5) inhibitor with IC50 of 2 nM.AZD4877 arrests cell mitosis, leads to the formation of the monopolar spindle phenotype and induces apoptosis. AZD4877 inhibits circulating peripheral blood mononuclear cells (PBMCs) and has anti-cancer activity.

AM-1882 (AM1882) is a potent, selective mitotic kinesin KIF18A inhibitor with IC50 of 230 nM in kinesin-8 microtubule (MT)-ATPase motor assays.

AM-9022 (AM9022) is a potent, selective and orally active mitotic kinesin KIF18A inhibitor with IC50 of 47 nM in kinesin-8 microtubule (MT)-ATPase motor assays.