Kinesin

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Kinesinシグナル伝達経路

Kinesin製品

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  • Kinesin阻害剤 (14)
  • 新製品
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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. GSK923295 induces post-mitotic apoptosis. Phase 1.
Nat Cancer, 2024, 5(1):66-84
Nature, 2023, 619(7968):176-183
Nature, 2023, 619(7968):176-183
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, no inhibition to CENP-E, RabK6, MCAK, MKLP1, KHC or Kif1A. Ispinesib induces mitotic arrest and apoptotic cell death.
Nat Cancer, 2024, 5(1):66-84
Biomed Pharmacother, 2023, 160:114305
Cancers (Basel), 2023, 15(12)3173
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.
Biochem Biophys Res Commun, 2023, 678:84-89
Cancer Cell, 2022, 40(7):754-767.e6
Cell Death Dis, 2022, 13-9:799
S8439 Monastrol Monastrol ((±)-Monastrol) is a cell-permeable small molecule inhibitor of kinesin-5(KIF11) which is essential for maintaining separation of the half-spindles.
Cell Rep Med, 2023, 4(2):100937
iScience, 2023, 26(6):106855
Nature, 2022, 604(7904):146-151
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. Dimethylenastron induces mitotic arrest and apoptosis and upregulate Hsp70 in human multiple myeloma cells.
EMBO Rep, 2023, e57234.
S6953 GW406108X GW406108X (GW108X) is an inhibitor of Kif15 (Kinesin-12) with an IC50 of 0.82 μM in the ATPase assay. GW406108X 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.
S7972New 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.
S7354New 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.
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.
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. GSK923295 induces post-mitotic apoptosis. Phase 1.
Nat Cancer, 2024, 5(1):66-84
Nature, 2023, 619(7968):176-183
Nature, 2023, 619(7968):176-183
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, no inhibition to CENP-E, RabK6, MCAK, MKLP1, KHC or Kif1A. Ispinesib induces mitotic arrest and apoptotic cell death.
Nat Cancer, 2024, 5(1):66-84
Biomed Pharmacother, 2023, 160:114305
Cancers (Basel), 2023, 15(12)3173
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.
Biochem Biophys Res Commun, 2023, 678:84-89
Cancer Cell, 2022, 40(7):754-767.e6
Cell Death Dis, 2022, 13-9:799
S8439 Monastrol Monastrol ((±)-Monastrol) is a cell-permeable small molecule inhibitor of kinesin-5(KIF11) which is essential for maintaining separation of the half-spindles.
Cell Rep Med, 2023, 4(2):100937
iScience, 2023, 26(6):106855
Nature, 2022, 604(7904):146-151
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. Dimethylenastron induces mitotic arrest and apoptosis and upregulate Hsp70 in human multiple myeloma cells.
EMBO Rep, 2023, e57234.
S6953 GW406108X GW406108X (GW108X) is an inhibitor of Kif15 (Kinesin-12) with an IC50 of 0.82 μM in the ATPase assay. GW406108X 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.
S7972New 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.
S7354New 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.
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.
S7972New 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.
S7354New 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.

Kinesin阻害剤の選択性比較

Tags: KSP inhibition | Kinesin inhibition | Kinesin assay | Kinesin phosphorylation | Kinesin cancer | KSP inhibitors cancer | KSP inhibitor clinical trial | Kinesin inhibitors list | Kinesin inhibitor review