Kinesin

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.

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).

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

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.

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

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

MPI-0479605 is an ATP competitive and selective inhibitor.

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

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

Mps1-IN-2 is a potent, selective, and ATP-competitive inhibitor of both Mps1 and Plk1.

Kif15-IN-1 is a kinesin family 15 (Kif15) inhibitor with antiproliferative activity and potential anticancer activity, which can be used to study gastric cancer.

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

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.

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

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

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

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.

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

Eg5 Inhibitor V, trans-24, is a specific and potent Eg5 inhibitor with an IC50 value of 0.65 μM, suitable for use in cancer research.

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

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

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

Kinesore is a cell-permeable small molecule modulator that binds primarily to the microtubule motor protein kinesin-1, thereby inhibiting the interaction between KLC2 (kinesin light chain 2) and SKIP (SKIP protein), and thus regulating the structure of the microtubule network to influence cytoskeletal organization and dynamics.

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

BRD9876 is a selective inhibitor of MM1S growth.

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

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.

KIF18A-IN-3 is an efficient KIF18A inhibitor (IC50 = 61nM) that induces mitotic arrest and increases the number of mitotic cells in tumor tissues. It can be used in tumor research.

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.

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

CCT251455, the mitotic kinase monopolar spindle 1 (MPS1 TTK) inhibitor, is a potent (IC50=3 nM) and specific chemical tool.

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

Betamethasone 17-benzoate, a representative steroid, is used in the treatment of recurrent aphthous ulcers (RAU).

KIF18A-IN-16 (Compound 15) is a polycyclic KIF18A inhibitor. It is applicable in research related to tumors, including colon cancer, breast cancer, and lung cancer.

PF-2771 is a potent and selective centromere protein E (CENP-E) inhibitor with an IC50 of 16.1 nM, used as an anticancer agent.

KIF18A-IN-14 (Compound Example 81) is an inhibitor of KIF18A that exists in two forms, EX81-A and its enantiomer EX81-B. EX81-A and EX81-B inhibit the viability of OVCAR-3 cells with IC50 values of 0-0.01 μM and 0.01-0.1 μM, respectively. KIF18A-IN-14 can be utilized in tumor research, including studies on colon cancer, breast cancer, and lung cancer.

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

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

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].

KIF18A-IN-15 (Compound Example 36) is a KIF18A inhibitor, available in two forms, EX36-A and its enantiomer EX36-B, both with an IC50 range of 0.01-0.1 μM. These compounds inhibit the viability of OVCAR-3 cells, with IC50 values of 0.01-0.1 μM for EX36-A and 0-0.01 μM for EX36-B. KIF18A-IN-15 is applicable in research on tumors, including colon, breast, and lung cancers.

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.

KSP ligand 1 is a protein ligand that targets KSP (Kinesin) and can be used in the synthesis of PROTAC KSP-IN-1 for cancer research.

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