kinesin

S-trityl-L-Cysteine is a non-natural amino acid and an inhibitor of Eg5, also known as KSP and Kif11, a mitotic kinesin necessary for mitotic spindle formation. S-trityl-L-Cysteine inhibits the ATPase activity of Eg5 in basal and microtubule-stimulated states (IC50s = 1,000 and 140 nM, respectively). It is selective for Eg5 over nine other human kinesins in an enzyme-coupled assay. It reversibly inhibits Eg5-driven microtubule sliding velocity with an IC50 value of 500 nM using X. laevis recombinant Eg5. It induces cell cycle arrest in HeLa cells (IC50 = 700 nM), reversibly halting the cell cycle in the mitotic phase by inhibiting the separation of duplicated chromosomes and preventing bipolar spindle formation. S-trityl-L-Cysteine inhibits the growth of cancer cells in vitro when tested against the National Cancer Institute (NCI) 60 human cancer cell line panel (average GI50 = 1.3 μM) and in mouse xenograft models.

BRD9876 is a selective inhibitor of MM1S growth.

Paprotrain ((alphaZ)-alpha-(3-Pyridinylmethylene)-1H-indole-3-acetonitrile) inhibits the ATPase activity of MKLP-2 with an IC50 of 1.35 μM and a Ki of 3.36 μM.

GSK923295 is a selective allosteric inhibitor of CENP-E kinesin motor ATPase(Ki=3.2 nM).

Ispinesib (SB-715992), a selective, effectvie and reversible inhibitor of kinesin spindle protein (KSP), is derived from quinazolinone, with antineoplastic properties.

Mitotic kinesin-IN-3 (Page 135, fourteenth) hydrochloride is an inhibitor of the mitotic motor protein (Mitotickinesin). It interferes with cell proliferation by inhibiting mitosis. This compound can be utilized in research relating to cancer, cardiac hypertrophy, immune and inflammatory diseases, as well as fungal infections.

Mitotic kinesin-IN-2 (Page 135, fifteenth) hydrochloride is an inhibitor of mitotic motor proteins (Mitotickinesin). This compound suppresses cell proliferation by inhibiting mitosis. Mitotic kinesin-IN-2 hydrochloride is used in research related to cancer, cardiac hypertrophy, immune and inflammatory diseases, as well as fungal infections.

Mitotic kinesin-IN-1 hydrochloride (Example 80) is an inhibitor of mitotic kinesin, which suppresses cell proliferation by hindering mitosis. This compound is applicable in research related to cancer, cardiac hypertrophy, immune and inflammatory diseases, and fungal infections.

SB-743921 hydrochloride (SB743921 HCl) is an effective inhibitor of kinesin spindle protein, KSP, (Ki =0.1 nM).

SR31527 (SR31527 chloride) is a potent KIFC1 inhibitor with an IC50 of 6.6 µM against KIFC1. SR31527 chloride has a moderate inhibitory effect on cell viability and colony formation.

Dimethylenastron, an Eg5 inhibitor, arrests cells with monopolar spindles to which all chromosomes attach in a syntelic manner.

K858 Racemic (K858) is a selective mitotic kinesin Eg5 inhibitor which acts in an ATP-noncompetitive manner.

Monastrol ((±)-Monastrol) is a potent and cell-permeable inhibitor of the mitotic kinesin Eg5.

CW-069 (IC50=75 μM), an allosteric selective inhibitor of microtubule motor protein HSET, exhibits remarkable specificity over KSP.

ARQ 621 is an allosteric, and selective Eg5 mitotic motor protein inhibitor. Phase 1.

GW406108X (GW108X) is a Kif15 inhibitor with an IC50 of 0.82 uM in ATPase assays. GW406108X is also an ULK1 kinase inhibitor with pIC50 values of 6.37 (427 nM) and block autophagic flux.

Litronesib is a selective inhibitor of mitosis-specific kinesin Eg5. It also has antitumor activity.

AZD-4877 is a potent spindle kinesin (Eg5) inhibitor with an IC50 value of 2 nM. AZD-4877 is an alternative configuration of Ispinesib that inhibits mitosis, induces the formation of a unipolar spindle phenotype, and mediates apoptosis. AZD-4877 has antitumor activity and inhibits circulating peripheral blood mononuclear cells (PBMC).

Eg5 Inhibitor V, trans-24, is a specific and potent Eg5 inhibitor with an IC50 value of 0.65 μM, suitable for use in cancer research.

Mps1-IN-1 is a potent, selective, and ATP-competitive inhibitor of Mps1 kinase (IC50: 367 nM).

BAY 1217389 is an effective and selective inhibitor of the monopolar spindle 1 (MPS1) kinase (IC50<10 nM).

TTK/PLK1-IN-1 (Formula I) is an inhibitor of threonine tyrosine kinase (TTK) and polo-like kinase 1 (PLK1), with IC50 values of 7 nM and 72 nM, respectively. It regulates the spindle assembly checkpoint (SAC) and exhibits antitumor activity against triple-negative breast cancer (TNBC).

(R)-Filanesib is the R-enantiomer of ARRY-520. (R)-Filanesib is a synthetic kinesin spindle protein (KSP) inhibitor (IC50: 6 nM).

AZ82 is a selective inhibitor of kinesin-like protein KIFC1 (HSET/KIFC1), with a Ki of 43 nM and an IC50 of 300 nM for KIFC1.