kinesin

BRD9876 is a selective inhibitor of MM1S growth.

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).

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

Monastrol ((±)-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.

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

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

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.

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.

KIF2C-IN-1 (Compound 7S9) is a selective and potent small molecule inhibitor of KIF2C. It stabilizes the interaction between KIF2C and microtubule proteins, preventing the depolymerization of polyglutamylated microtubules. KIF2C-IN-1 enhances the cytotoxicity of Paclitaxel in Paclitaxel-resistant triple-negative breast cancer (TNBC) cells and, when combined with Paclitaxel, significantly reduces tumor growth in mouse models.

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.

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

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.

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.