| 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
|
|
| 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.
|
|
|
| E1180 |
Sovilnesib (AMG 650)
|
AMG 650 (Sovilnesib) is an oral, first in class, selective kinesin-like protein KIF18A inhibitor, can be used for the research of cancer.
|
|
|