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
-
EMBO J, 2024, 43(19):4324-4355
-
Curr Biol, 2024, 34(5):1133-1141.e4
|
|
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
-
Cells, 2024, 13(7)607
-
Biomed Pharmacother, 2023, 160:114305
|
|
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
|
|
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. |
-
Mol Biol Cell, 2024, 35(8):br15
-
Cell Rep Med, 2023, 4(2):100937
-
iScience, 2023, 26(6):106855
|
|
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.
|
|
E4602New |
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). |
|
|
E4595New |
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. 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. |
|
|
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. |
|
|
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
- EMBO J, 2024, 43(19):4324-4355
- Curr Biol, 2024, 34(5):1133-1141.e4
|
|
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
- Cells, 2024, 13(7)607
- Biomed Pharmacother, 2023, 160:114305
|
|
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
|
|
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. |
- Mol Biol Cell, 2024, 35(8):br15
- Cell Rep Med, 2023, 4(2):100937
- iScience, 2023, 26(6):106855
|
|
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.
|
|
E4602New |
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). |
|
|
E4595New |
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. 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. |
|
|
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. |
|
|