Home Cytoskeletal Signaling -Cell Cycle Kinesin

Kinesin

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.

Cytoskeletal Signaling

Caspase Bcl-2 p53 Survivin TNF-alpha MDM2/MDMX Ras IAP PD-1/PD-L1 ASK Bax/Bak RIP kinase Cyt C Bcl-6 cytohesin Heme Oxygenase OXPHOS Apoptosis related FKBP PKD DAPK Pyroptosis Thymidylate Synthase TRADD TACE Cuproptosis ADAM10

Isoform-selective Products

  • All (18)
  • Kinesin Inhibitors (18)
  • New Kinesin Products
Cat.No. Product Name Information Product Use Citations Product Validations
S7090 GSK923295 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. This compound induces post-mitotic apoptosis. Phase 1.
Cancer Res, 2025, 10.1158/0008-5472.CAN-25-0999
Nat Cancer, 2024, 5(1):66-84
EMBO J, 2024, 43(19):4324-4355
Verified customer review of GSK923295
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.
Clin Transl Med, 2025, 15(1):e70164
Life Sci Alliance, 2025, 8(1)e202402927
bioRxiv, 2025, 2025.01.08.631954
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
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 Rep, 2023, e57234.
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 Discov, 2025, 11(1):130
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.
S6953 GW406108X GW406108X (GW108X) is an inhibitor of Kif15 (Kinesin-12) with an IC50 of 0.82 μM in the ATPase assay. This compound inhibits recombinant ULK1 kinase activity with a pIC50 of 6.37 and blocks autophagy in cells, without affecting the upstream signalling kinases mTORC1 and AMPK.
E5883New AM-9022 AM-9022 is an orally active, potent, and selective inhibitor of KIF18A, a mitotic kinesin motor protein critical for chromosome alignment and segregation. It exhibits significant anti-cancer effects in human breast and ovarian tumor models.
S7972 Litronesib Litronesib (LY2523355) is a selective allosteric inhibitor of the human mitosis-specific kinesin Eg5. LY2523355 also exhibits highly schedule-dependent, broad-spectrum anticancer activity against tumor models and causes mitotic arrest and apoptosis in cancer cells.
E0779 Paprotrain Paprotrain is a cell-permeable inhibitor of the kinesin MKLP-2, inhibits the ATPase activity of MKLP-2 with an IC50 of 1.35 μM and a Ki of 3.36 μM and shows a moderate inhibition activity on DYRK1A with an IC50 of 5.5 μM.
E5992New VLS-1272 VLS-1272 is an orally bioavailable, potent, ATP non-competitive, microtubule-dependent, and highly selective inhibitor of KIF18A with an IC50 of 41 nM. It induces mitotic defects with strong anti-mitotic, anti-cancer, and anti-proliferative effects, leading to dose-dependent tumor growth inhibition and can be used for the study of cancers with high chromosomal instability.
S7354 Filanesib hydrochloride Filanesib (ARRY-520) hydrochloride is a kinesin spindle protein (KSP) inhibitor that blocks the separation of centrosomes and assembly of spindles in the early stage of cell mitosis, and cell proliferation.
S5522 H-Cys(Trt)-OH H-Cys(Trt)-OH (L-Cys(Trt)-OH, H-L-Cys(Trt)-OH, S-Tritylcysteine,S-Trityl-L-cysteine) is a specific inhibitor of Eg5 that inhibits Eg5-driven microtubule sliding velocity in a reversible fashion with an IC50 of 500 nM.
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
E1180 Sovilnesib AMG 650 (Sovilnesib) is an oral, first in class, selective kinesin-like protein KIF18A inhibitor, can be used for the research of cancer.
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
S7090 GSK923295 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. This compound induces post-mitotic apoptosis. Phase 1.
Cancer Res, 2025, 10.1158/0008-5472.CAN-25-0999
Nat Cancer, 2024, 5(1):66-84
EMBO J, 2024, 43(19):4324-4355
 Verified customer review of GSK923295
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.
Clin Transl Med, 2025, 15(1):e70164
Life Sci Alliance, 2025, 8(1)e202402927
bioRxiv, 2025, 2025.01.08.631954
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
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 Rep, 2023, e57234.
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 Discov, 2025, 11(1):130
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.
S6953 GW406108X GW406108X (GW108X) is an inhibitor of Kif15 (Kinesin-12) with an IC50 of 0.82 μM in the ATPase assay. This compound inhibits recombinant ULK1 kinase activity with a pIC50 of 6.37 and blocks autophagy in cells, without affecting the upstream signalling kinases mTORC1 and AMPK.
E5883New AM-9022 AM-9022 is an orally active, potent, and selective inhibitor of KIF18A, a mitotic kinesin motor protein critical for chromosome alignment and segregation. It exhibits significant anti-cancer effects in human breast and ovarian tumor models.
S7972 Litronesib Litronesib (LY2523355) is a selective allosteric inhibitor of the human mitosis-specific kinesin Eg5. LY2523355 also exhibits highly schedule-dependent, broad-spectrum anticancer activity against tumor models and causes mitotic arrest and apoptosis in cancer cells.
E0779 Paprotrain Paprotrain is a cell-permeable inhibitor of the kinesin MKLP-2, inhibits the ATPase activity of MKLP-2 with an IC50 of 1.35 μM and a Ki of 3.36 μM and shows a moderate inhibition activity on DYRK1A with an IC50 of 5.5 μM.
E5992New VLS-1272 VLS-1272 is an orally bioavailable, potent, ATP non-competitive, microtubule-dependent, and highly selective inhibitor of KIF18A with an IC50 of 41 nM. It induces mitotic defects with strong anti-mitotic, anti-cancer, and anti-proliferative effects, leading to dose-dependent tumor growth inhibition and can be used for the study of cancers with high chromosomal instability.
S7354 Filanesib hydrochloride Filanesib (ARRY-520) hydrochloride is a kinesin spindle protein (KSP) inhibitor that blocks the separation of centrosomes and assembly of spindles in the early stage of cell mitosis, and cell proliferation.
S5522 H-Cys(Trt)-OH H-Cys(Trt)-OH (L-Cys(Trt)-OH, H-L-Cys(Trt)-OH, S-Tritylcysteine,S-Trityl-L-cysteine) is a specific inhibitor of Eg5 that inhibits Eg5-driven microtubule sliding velocity in a reversible fashion with an IC50 of 500 nM.
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
E1180 Sovilnesib AMG 650 (Sovilnesib) is an oral, first in class, selective kinesin-like protein KIF18A inhibitor, can be used for the research of cancer.
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
E5883New AM-9022 AM-9022 is an orally active, potent, and selective inhibitor of KIF18A, a mitotic kinesin motor protein critical for chromosome alignment and segregation. It exhibits significant anti-cancer effects in human breast and ovarian tumor models.
E5992New VLS-1272 VLS-1272 is an orally bioavailable, potent, ATP non-competitive, microtubule-dependent, and highly selective inhibitor of KIF18A with an IC50 of 41 nM. It induces mitotic defects with strong anti-mitotic, anti-cancer, and anti-proliferative effects, leading to dose-dependent tumor growth inhibition and can be used for the study of cancers with high chromosomal instability.

Signaling Pathway Map