kinesin

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.

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

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

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.

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].

11H-Benzo[a]carbazole is a kinesin-like protein KIF11 inhibitor that can inhibit the viability of HeLa cells.

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

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

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.

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.

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.

MKLP2-IN-1 (compound 12a) is an inhibitor of MKLP2 that demonstrates excellent oral bioactivity. In vitro, MKLP2-IN-1 inhibits the ATPase activity stimulated by recombinant MKLP2 microtubules and, in a mouse Calu-6 lung cancer model, it effectively suppresses tumor growth.

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.

MPI-0479605 is an ATP competitive and selective inhibitor.

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).

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.

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

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.

BRD9876 is a selective inhibitor of MM1S growth.

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

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

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.

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.

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