AZ82 is a selective HSET/KIFC1 inhibitor, with a Ki of 43 nM and an IC50 of 300 nM for KIFC1.
SB-743921 is a potent inhibitor of the mitotic kinesin KSP (Eg5), with a Ki of 0.1 nM.
BRD9876 is the “rigor” inhibitor that locks kinesin-5 (Eg5) in a state with enhanced microtubules (MTs) binding, leading to bundling and stabilization of MTs. BRD9876 interacts with the tyrosine 104 residue that is part of the α4-α6 allosteric binding pocket. BRD9876 specifically targets microtubule-bound Eg5 and selectively inhibits myeloma over CD34 cells. BRD9876 has the potential for multiple myeloma (MM) research[1][2][3][4].
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.
Solidagonic acid inhibits HSET motor activity by promoting the conversion from abnormal monopolar to bipolar spindles. Solidagonic acid suppresses fission yeast cell death and enables reversion of the mitotic spindles from a monopolar to bipolar morphology. Solidagonic acid showed the growth inhibitory activity on the seedlings of Lactuca sativa L. and Lolium multiflorum Lam[1][2].
PVZB-1194 is a bis(hetero)aryl derivative that inhibits kinesin spindle protein (KSP) ATPase witn IC50 of 0.12 uM; inhibits HeLa cell proliferation with IC50 of 5.5 uM; potently inhibits KSP in a microruble dependent manner and induces a monoastral phenotype to arrest mitotic progression, abnormal KSP localization.
(S)-Monastrol ((+)-Monastrol) is an allosteric inhibitor of the mitotic kinesin Eg5 that exhibits an antiproliferative effect against several cancer cell lines. (S)-Monastrol arrests mammalian cells in mitosis with monopolar spindles[1][2].
SR31527 is a novel allosteric Kinesin-like protein KIFC1 inhibitor that inhibits microtubule-stimulated KIFC1 ATPase activity with IC50 of 6.6 uM, binds directly to KIFC1 with Kd of 25.4 nM; prevents bipolar clustering of extra centrosomes in TNBC cells and significantly reducesTNBC cell colony formation and viability (MDA-MB-231, BT549 and MDA-MB-435s cells IC50=20-30 uM), with less toxicity to normal fibroblasts.
K858 Racemic is an ATP-uncompetitive inhibitor of Eg5 with an IC50 of 1.3 μM.
Litronesib (Racemate) is the racemate of litronesib. Litronesib is a selective, allosteric inhibitor of Eg5.
AZD4877 is another isostere to Ispinesib (HY-50759)and also a kinesin spindle protein (Eg5) inhibitor with IC50 of 2 nM.AZD4877 arrests cell mitosis, leads to the formation of the monopolar spindle phenotype and induces apoptosis. AZD4877 inhibits circulating peripheral blood mononuclear cells (PBMCs) and has anti-cancer activity[1][2][3][4][5].
SB-743921 free base is a potent selective inhibitor of the mitotic kinesin KSP (Eg5), with a Ki of 0.1 nM. SB-743921 free base can induce mitotic arrest, block cell cycle progression, induce apoptosis, and can be used in the research of myeloma, leukemia and other diseases[1][2].
S-Trityl-L-cysteine (NSC 83265) is a selective and allosteric kinesin Eg5 inhibitor with an IC50 of 1 μM for the inhibition of basal ATPase activity and 140 nM for the microtubule-activated ATPase activity. S-Trityl-L-cysteine has antitumor activities[1][2].
Monastrol is a potent and cell-permeable inhibitor of the mitotic kinesin Eg5 with an IC50 value of 14 μM.
CW-069 is an allosteric inhibitor of HSET with an IC50 of 75 μM.
Dimethylenastron is a potent Eg5 inhibitor, with an IC50 of 200 nM.
MK-0731 is a selective, non-competitive and allosteric kinesin spindle protein (KSP) inhibitor with an IC50 of 2.2 nM and a pKa of 7.6. MK-0731 is >20,000 fold selectivity against other kinesins. MK-0731 induces mitotic arrest and induces apoptosis in tumors. MK-0731 provides significant antitumor efficacy[1][2].
Kolavenic acid analog (KAA) is an anticancer agent. Kolavenic acid analog shows strong activity against HSET-overproducing yeast cells. Kolavenic acid analog inhibits centrosome clustering in human cancer cells containing high HSET levels and supernumerary centrosomes[1].
GSK-923295 is a special, allosteric inhibitor of CENP-E kinesin motor ATPase activity, with Ki of 3.2±0.2 nM and 1.6± 0.1 nM for human and canine, respectively.
Ispinesib is a specific inhibitor of KSP, with a Ki app of 1.7 nM.
Filanesib (ARRY-520) is a synthetic kinesin spindle protein (KSP) inhibitor with IC50 of 6 nM.
ARRY-520 R enantiomer is the R-enantiomer of ARRY-520. ARRY-520 is a synthetic kinesin spindle protein (KSP) inhibitor with IC50 of 6 nM.
Litronesib is a selective Eg5 inhibitor, with antitumor activity.
ARQ 621 is an allosteric, potent and selective inhibitor of Eg5, a microtubule-based ATPase motor protein involved in cell division. Anti-tumor activity[1]. ARQ 621 is a kinesin inhibitor[2].
Kif15-IN-2 is an inhibitor of the mitotic kinesin Kif15, and is used for the research of cellular proliferative diseases.
Kif15-IN-1 is an inhibitor of the mitotic kinesin Kif15, and is used for the research of cellular proliferative diseases.
Eg5 Inhibitor V, trans-24 is a potent and specific Eg5 inhibitor with an IC50 of 0.65 μM, and can be used in the research of cancer.
EMD534085 is a potent and selective inhibitor of the mitotic kinesin-5 with an IC50 of 8 nM.
A potent, specific, allosteric and cell-active inhibitor of KSP with IC50 of 11 nM; has no ihibitory activity toward other kinesins, includin CENP-E, MKLP-1, KIF-3A, and uKHC (IC50>50 uM); induces the formation of monoastral spindles, causes mitotic arrest in a dose-dependent manner (EC50=30 nM) in A2780 ovarian carcinoma cells; sustained KSP inhibition activates the proapoptotic protein, Bax, and both activation of the spindle checkpoint and subsequent mitotic slippage are required for Bax activation.