Kinesin

BAY 1217389 is an effective and selective inhibitor of the monopolar spindle 1 (MPS1) kinase (IC50<10 nM).

GW406108X(Z/E) is a mixture of different configurations of GW406108X, which is an inhibitor of Kinesin-12 and ULK1 .

CFI-402257 is a selective inhibitor of Mps1/TTK kinase (Mps1 Ki = 0.09 nM; EC50 = 6.5 nM)and can be used in studies about hepatocellular carcinoma diseases.

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.

Eg5 Inhibitor V, trans-24 is a specific and potent Eg5 inhibitor that can be used in cancer research with an IC50 value of 0.65 uM.

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

Betamethasone 17-benzoate is a representative steroid. It also can be used in the treatment of recurrent aphothous ulcers (RAU).

BRD9876 is a selective inhibitor of MM1S growth.

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

Paprotrain ((alphaZ)-alpha-(3-Pyridinylmethylene)-1H-indole-3-acetonitrile) inhibits the ATPase activity of MKLP-2 with an IC50 of 1.35 μM and a Ki of 3.36 μM.

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

GSK923295 is a selective allosteric inhibitor of CENP-E kinesin motor ATPase(Ki=3.2 nM).

GW406108X (GW108X) is a Kif15 inhibitor with an IC50 of 0.82 uM in ATPase assays. GW406108X is also an ULK1 kinase inhibitor with pIC50 values of 6.37 (427 nM) and block autophagic flux.

NMS-P715 is a selective and ATP-competitive MPS1 inhibitor(IC50 of 182 nM).

Mps1-IN-2 is a potent, selective and ATP-competitive dual Mps1/Plk1 inhibitor.

CW-069 (IC50=75 μM）, an allosteric selective inhibitor of microtubule motor protein HSET, exhibits remarkable specificity over KSP.

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

Kif15-IN-2 is a kinesin Kif15 inhibitor with potential anticancer activity and can be used in prostate cancer research.

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].

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

UMK57 is a CENP-Ei and MCAK enhancer, selectively promoting k-MT attachment error correction to inhibit chromosome missegregation of small molecule compounds, and can improve chromosome separation conservation by disrupting the stability of kinetosomal microtubule (k-MT) attachment during mitosis.

EMD534085 is an effective and selective mitotic kinesin-5 inhibitor (IC50: 8 nM).

CCT251455 is an inhibitor of mitotic kinase monopolar spindle 1 (MPS1; IC50: 3 nM).

PF-2771 is a potent and selective centromere protein E (CENP-E) inhibitor. PF-2771 inhibits CENP-E motor activity with an IC 50 of 16.1 nM. PF-2771 is used as an anticancer agent.

TC-Mps1-12 is an effective and selective inhibitor of monopolar spindle 1 (IC50: 6.4 nM) .

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

MPI-0479605 is an ATP competitive and selective inhibitor.

Ispinesib (SB-715992), a selective, effectvie and reversible inhibitor of kinesin spindle protein (KSP), is derived from quinazolinone, with antineoplastic properties.

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.

BOS-172722 is an inhibitor of monopolar spindle 1 (MPS1) checkpoint(IC50 of 2 nM).

SR31527 (SR31527 chloride) is a potent KIFC1 inhibitor with an IC50 of 6.6 µM against KIFC1. SR31527 chloride has a moderate inhibitory effect on cell viability and colony formation.

Empesertib (BAY 1161909) is an orally bioavailable and selective inhibitor Mps1(IC50 < 1 nM), with potential antineoplastic activity.

SB-743921 hydrochloride (SB743921 HCl) is an effective inhibitor of kinesin spindle protein, KSP, (Ki =0.1 nM).

AZ3146 is a selective Mps1 inhibitor with IC50 of ~35 nM.

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).

Mps1-IN-3 is an effective and selective inhibitor of MPS1 kinase (IC50: 50 nM).