Home Cytoskeletal Signaling Kinesin

Kinesin inhibitors

As a member of the kinesin superfamily of microtubule-basedmotors, Kinesin spindle protein (KSP) not only plays an important role in centrosome separation, but mediates the assembly and maintenance of bipolar spindle. Kinesins are a large superfamily of motor proteins that participate in various biological phenomena including mitosis and intracellular transport of vesicles and organelles. As targeting KSP provides a novel route for the manipulation of the cell cycle, KSP inhibitors can be used for cancer treatment because cell will stay in mitosis without the function of KSP.

Other Cytoskeletal Signaling Related Inhibitors

HSP Microtubule Associated Integrin PAK Dynamin MLCK TACC3 Gap-Junction Actin Cardiac Myosin

Isoform-selective Products

Cat.No. Product Name Information Product Use Citations Product Validations
S7090 GSK-923295 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. GSK923295 induces post-mitotic apoptosis. Phase 1.
Cancer Res, 2025, 85(15):2921-2938
Cancer Res, 2025, 10.1158/0008-5472.CAN-25-0999
Nat Cancer, 2024, 5(1):66-84
Verified customer review of GSK-923295
S1452 Ispinesib (SB-715992) Ispinesib (SB-715992, CK0238273) is a potent, specific and reversible inhibitor of kinesin spindle protein (KSP) with Ki app of 1.7 nM in a cell-free assay, showing no inhibition to CENP-E, RabK6, MCAK, MKLP1, KHC or Kif1A. This compound induces mitotic arrest and apoptotic cell death.
Nat Cancer, 2024, 5(1):66-84
Cells, 2024, 13(7)607
Cancers (Basel), 2024, 16(23)4075
Verified customer review of Ispinesib (SB-715992)
S2182 SB743921 HCl 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. Phase 1/2.
Int J Mol Sci, 2024, 25(13)7230
Life Sci Alliance, 2024, 7(10)e202402670
Biochem Biophys Res Commun, 2023, 678:84-89
Verified customer review of SB743921 HCl
S8439 Monastrol Monastrol ((±)-Monastrol) is a cell-permeable small molecule inhibitor of kinesin-5(KIF11) with an IC50 of 14μM, which is essential for maintaining separation of the half-spindles.
Adv Sci (Weinh), 2025, 12(45):e07839
Clin Transl Med, 2025, 15(1):e70164
Life Sci Alliance, 2025, 8(1)e202402927
S7355 ARQ 621 ARQ 621 is an allosteric, and selective Eg5 mitotic motor protein inhibitor. Phase 1.
Nat Commun, 2024, 15(1):1041
Mol Cell Proteomics, 2017, 16(3):428-437
Assay Drug Dev Technol, 2016, 14(7):395-406
E4602 VLS-1488(KIF18A-IN-6 ) VLS-1488 (KIF18A-IN-6) is an oral inhibitor of KIF18A with an IC50 of 0.016 μM. KIF18A is a mitotic kinesin motor protein that localizes at the plus-end of kinetochore microtubule spindle fibers and is crucial for cell division in aneuploid cancer cells with high chromosomal instability (CIN).
Cell Death Discovery, 2025, 130
Cell Death Discov, 2025, 11(1):130
S0279 Dimethylenastron Dimethylenastron is a potent, specific and reversible inhibitor of kinesin Eg5 (kinesin-5/kinesin spindle protein, KSP) with IC50 of 200 nM. This compound induces mitotic arrest and apoptosis and upregulate Hsp70 in human multiple myeloma cells.
EMBO Reports, 2023, e57234
EMBO Rep, 2023, e57234.
S5933 K 858 K858 is a novel and potent inhibitor of Eg5 with an IC50 of 1.3 μM for inhibiting the ATPase activity of Eg5, showing at least 150-fold more selective for Eg5 than other members of the kinesin superfamily.
Front Pharmacol, 2024, 15:1392352
S6796 BTB-1 BTB-1 is a novel, selective and reversible inhibitor of the mitotic motor protein Kif18A with IC50 of 1.69 μM.
Nat Commun, 2024, 15(1):5448
E4595 SB-743921 SB-743921 (SB-921) is an inhibitor of Kinesin Spindle Protein (KSP), a mitotic protein essential for cell cycle control and motility. It functions by selectively targeting rapidly dividing cells and disrupting spindle formation during cell division, leading to G2/M phase arrest and ultimately causing cell death. It also inhibits proliferation and induces apoptosis in diffuse large B-cell lymphoma (DLBCL) cell lines.

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