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CENP-E inhibitor
GSK-923295, is a small-molecule inhibitor of the mitotic kinesin centromere-associated protein E, (CENP-E).- Amber S Zhou, .et al. , PLoS Biol, 2023, Oct 26;21(10):e3002339 PMID: 37883329
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TTK inhibitor
CFI-402257, a pyrazolopyridin derivative, has been found to be a TTK inhibitor that could influence chromosome segregation and induce cell death so that is significant in anticancer studies.- Jian Yu, .et al. , BMC Cancer, 2022, Jul 18;22(1):786 PMID: 35850753
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Mps1 inhibitor
AZ 3146 is a potent and selective monopolar spindle 1 (Mps1) kinase inhibitor (IC50 = 35 nM). It interferes with chromosome alignment and overrides spindle assembly checkpoint and also Inhibits the recruitment of Mad1, Mad2 and centromere protein E (CENP-E) to kinetochores.
- Junna Tanaka, .et al. , Cell Signal, 2024, Jul:119:111172 PMID: 38604342
- Ryuzaburo Yuki, .et al. , Eur J Pharmacol, 2024, Jan 15:963:176229 PMID: 38072041
- Ryoko Ota, .et al. , Cell Signal, 2023, Sep;109:110764 PMID: 37315749
- Ryuzaburo Yuki, .et al. , J Cell Mol Med, 2021, Feb;25(3):1677-1687 PMID: 33465289
- Yamagishi A, .et al. , Int J Mol Sci, 2020, Feb 5;21(3) PMID: 32033461
- Kakihana A, .et al. , FASEB J, 2018, Nov 29:fj201801369R PMID: 30496702
- Suzuki M, .et al. , Anticancer Res, 2016, Jun;36(6):2783-92 PMID: 27272789
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KSP Inhibitor
Ispinesib (SB-715992) is a potent inhibitor of kinesin spindle protein, a kinesin motor protein essential for the formation of a bipolar mitotic spindle and cell cycle progression through mitosis. -
KSP inhibitor
KSP inhibitor ARRY-520 specifically inhibits KSP (kinesin-5 or Eg5) with potential antineoplastic activity. -
KIF18A Inhibitor
Sovilnesib is a selective inhibitor of the kinesin-like protein KIF18A, exhibiting an IC50 value of 0.071 μM. This potent, orally active compound is utilized in cancer research, where it aids in the investigation of microtubule dynamics and the mechanisms of tumor cell proliferation. Sovilnesib facilitates the study of KIF18A's role in cancer progression and provides insights into potential therapeutic strategies targeting this protein. -
HSET Inhibitor
CCT368772 is a selective kinesin HSET inhibitor, demonstrating an IC50 value of 0.019 μM in the HSET ADP-Glo assay. This compound shows high selectivity for HSET, with minimal activity against Eg5 (IC50 >200 μM). CCT368772 is suitable for research into hyperproliferative diseases, including various cancer types, providing a valuable tool for understanding and potentially targeting these pathologies. -
KIF18A Inhibitor
KIF18A-IN-6 is a potent inhibitor of KIF18A, exhibiting an IC50 of 0.016 μM against KIF18A's microtubule-dependent ATPase activity. This compound is valuable for investigating the role of KIF18A in cellular processes, including mitotic spindle assembly and chromosome alignment. Researchers can utilize KIF18A-IN-6 to explore therapeutic strategies targeting cancer cell division by modulating KIF18A activity. -
KIF18A Inhibitor
KIF18A-IN-1 is a potent inhibitor of the mitotic kinesin KIF18A, demonstrating significant anti-tumor activity. By targeting KIF18A, this compound has the potential to activate mitotic checkpoints, selectively inducing apoptosis in chromosomally unstable cancer cells. It is a valuable tool for research focused on cancer biology and the development of targeted cancer therapeutics. -
KIF18A Inhibitor
AM-5308 is a potent inhibitor of KIF18A, showcasing an IC50 value of 47 nM. By inhibiting KIF18A-mediated microtubule ATPase activity, AM-5308 effectively activates mitotic checkpoints and regulates critical cell division processes, including chromosome segregation and spindle assembly. This compound demonstrates notable antitumor activity, making it a valuable tool for cancer research and studies focused on mitotic regulation. -
KIF18A Inhibitor
AM-9022 is a potent and selective inhibitor of KIF18A, primarily targeting the kinesin family of motor proteins involved in cellular transport and mitosis. This compound demonstrates significant inhibitory activity, making it a valuable tool for research into cancer mechanisms and potential therapeutic strategies. Its efficacy in modulating KIF18A function provides insights into the role of mitotic regulation in tumorigenesis. -
Kinesin-5 Inhibitor
PVZB1194 is a selective inhibitor of Kinesin-5 ATPase, targeting the α4/α6 site within the motor domain in a nucleotide-competitive manner. With an IC50 of 0.12 μM for KSP ATPase, PVZB1194 effectively induces mitotic arrest characterized by the formation of monopolar spindles, leading to inhibition of HeLa cell proliferation (IC50: 5.5 μM). This compound is valuable for research applications focusing on tumor biology and cell division regulation. -
CENP-E Inhibitor
PF-2771 is a selective inhibitor of centromere protein E (CENP-E) that inhibits its motor activity with an IC50 of 16.1 nM. This compound exhibits significant potential as an anticancer agent by disrupting mitotic processes and leading to cell cycle arrest. PF-2771 is utilized in research investigating the mechanisms of cancer cell division and has applications in the development of novel cancer therapeutics. -
KIF18A Inhibitor
KIF18A-IN-13 is a potent inhibitor of KIF18A, demonstrating significant anticancer activity in vivo. This compound is particularly applicable in research focusing on ovarian cancer, providing a valuable tool for studying the mechanisms of tumor growth and potential therapeutic interventions. -
Kinesin
BRD9876 is a kinesin-5 (Eg5) inhibitor that functions by locking the protein in a conformation with enhanced microtubule binding, promoting microtubule bundling and stabilization. It specifically interacts with the tyrosine 104 residue within the α4-α6 allosteric binding pocket of Eg5, selectively inhibiting myeloma cells while sparing CD34+ hematopoietic stem cells. This compound is a valuable tool for studying the mechanisms of multiple myeloma and developing potential therapeutic strategies. -
CENP-E Inhibitor
Syntelin is a selective inhibitor of centromere protein E (CENP-E) with an IC50 of 160 nM. This compound exhibits significant antitumor activity, making it a valuable tool for cancer research. Its ability to modulate CENP-E function underscores its potential applications in studying mitotic processes and exploring therapeutic strategies for cancer treatment. -
KIFC1 Inhibitor
SR31527 chloride is a potent inhibitor of KIFC1, exhibiting an IC50 value of 6.6 µM. This compound effectively reduces cell viability and impairs colony formation in cellular assays. Its biological activity makes it a valuable tool for investigating the roles of KIFC1 in cell proliferation and cancer research. -
KIF18A Inhibitor
KIF18A-IN-2 is a selective inhibitor of KIF18A with an IC50 of 28 nM. This compound effectively induces mitotic arrest, leading to an increased population of mitotic cells in tumor tissues. KIF18A-IN-2 is suitable for use in cancer research, providing valuable insights into the mechanisms of cell division and the potential for therapeutic interventions. -
KIF18A Inhibitor
KIF18A-IN-3 is a selective inhibitor of kinesin motor protein KIF18A, with an IC50 of 61 nM. This compound induces significant mitotic arrest and enhances the population of mitotic cells within tumor tissues. KIF18A-IN-3 is suited for cancer research applications, providing insights into the roles of mitotic regulation and potential therapeutic strategies targeting KIF18A. -
KIF18A Inhibitor
KIF18A-IN-9 is a potent inhibitor of kinesin family member 18A (KIF18A), exhibiting an IC50 value of 3.8 nM. This compound demonstrates significant anticancer activity, showing IC50 values below 100 nM in ovarian cancer OVCAR3 and breast cancer MDA-MB-157 cell lines. KIF18A-IN-9 serves as a valuable tool for investigating the role of KIF18A in mitotic processes and its potential therapeutic implications in cancer research. -
KSP Inhibitor
Filanesib TFA is a selective kinesin spindle protein (KSP) inhibitor, demonstrating an IC50 of 6 nM against human KSP. This compound effectively induces apoptosis in vitro, providing potent anti-proliferative activity. Filanesib TFA is utilized in research applications focused on cancer biology and exploring novel therapeutic strategies targeting mitotic processes. -
Eg5 Inhibitor
(S)-Monastrol is an allosteric inhibitor of the mitotic kinesin Eg5, known for its ability to disrupt mitotic spindle formation. This compound exhibits significant antiproliferative activity against various cancer cell lines by inducing a monopolar spindle formation, effectively arresting mammalian cells in mitosis. (S)-Monastrol serves as a valuable tool for research into cancer biology and the mechanisms of cell division. -
Eg5 Inhibitor
SB-743921 free base is a highly selective inhibitor of the mitotic kinesin Eg5, exhibiting a Ki of 0.1 nM. This compound effectively induces mitotic arrest, inhibits cell cycle progression, and promotes apoptosis. It serves as a valuable tool in cancer research, particularly in the study of myeloma, leukemia, and other malignancies. -
Anticancer Agent
Kolavenic acid analog (KAA) is an anticancer agent that inhibits centrosome clustering in human cancer cells characterized by elevated levels of HSET and supernumerary centrosomes. KAA demonstrates significant activity against HSET-overproducing yeast cells, making it a valuable tool for understanding the role of HSET in cancer biology. This compound is suitable for research applications targeting centrosome dynamics and their implications in tumorigenesis. -
HSET Motor Inhibitor
Solidagonic acid is an HSET motor inhibitor that facilitates the conversion of abnormal monopolar spindles to bipolar spindles, thus promoting proper mitotic progression. This compound has been shown to suppress cell death in fission yeast and can revert monopolar to bipolar spindle morphology. Additionally, Solidagonic acid demonstrates growth inhibitory effects on the seedlings of Lactuca sativa L. and Lolium multiflorum Lam, making it a valuable tool for studying spindle dynamics and plant development. -
KIF18A Inhibitor
KIF18A-IN-4 is a noncompetitive inhibitor of KIF18A, targeting ATP and microtubule interactions with an IC50 of 6.16 μM. This compound demonstrates selectivity against a wide range of mitotic kinesins and kinases, while not interfering with tubulin assembly. KIF18A-IN-4 is valuable for research applications focused on tumor biology, particularly in studies investigating its anti-tumor properties. -
MKLP2 Inhibitoe
LG157 is a potent inhibitor of mitotic kinesin-like protein 2 (MKLP2), a critical motor protein involved in maintaining mitotic spindle dynamics and cytokinesis. By selectively targeting MKLP2, LG157 effectively disrupts cell division, making it a valuable reagent for research into cancer cell proliferation and related therapeutic strategies. Its application in cell biology provides insight into the mechanisms of mitotic regulation and potential treatment approaches for tumors exhibiting aberrant cell division. -
KIF18A Inhibitor
EX05 is a potent KIF18A inhibitor, exhibiting an IC50 of 8.2 nM. This compound selectively disrupts the function of KIF18A, a motor protein involved in mitotic spindle positioning, making it a valuable tool for cancer research. Its ability to interfere with cell division processes makes EX05 suitable for studying mechanisms of tumorigenesis and potential therapeutic strategies in oncology. -
KIF18A Inhibitor
KIF18A-IN-19 is a potent inhibitor of KIF18A, demonstrating an IC50 of less than 0.1 μM. This compound exhibits significant anti-cancer activity, particularly against ovarian cancer, making it a valuable tool in cancer research. Its mechanism of action and high efficacy establish KIF18A-IN-19 as a promising candidate for investigating the role of KIF18A in tumor biology. -
KIF18A Inhibitor
KIF18A-IN-12 is a potent inhibitor of KIF18A, exhibiting an IC50 value of 45.54 nM. This compound is valuable for investigating the role of KIF18A in cell division and its implications in cancer research. Researchers can utilize KIF18A-IN-12 to study the mechanistic pathways involved in tumorigenesis and explore potential therapeutic strategies targeting this kinesin. -
KIF18A Inhibitor
KIF18A-IN-14 is a selective inhibitor targeting KIF18A, a motor protein involved in spindle dynamics during cell division. This compound exhibits potent anti-proliferative effects, demonstrating IC50 values between 0-0.01 μM for the EX81-A form and 0.01-0.1 μM for its enantiomer, EX81-B, in OVCAR-3 cell lines. KIF18A-IN-14 is valuable for research applications in tumor biology, particularly in studies related to colon, breast, and lung cancers. -
S-enantiomer of AM-9022
(S)-AM-9022 is the S-enantiomer of AM-9022, functioning as a selective inhibitor of KIF18A. This compound exhibits significant potency and is utilized in cancer research, providing insights into the mechanisms of tumor progression and potential therapeutic strategies targeting kinesin motor proteins. Its application aids in understanding cell division and mitotic regulation in cancer biology. -
KIF18A Inhibitor
KIF18A-IN-10 is a potent inhibitor of KIF18A, exhibiting an IC50 value of 23.8 nM. This compound demonstrates significant anticancer activity, with IC50 values under 100 nM in ovarian cancer OVCAR3 and breast cancer MDA-MB-157 cell lines. KIF18A-IN-10 is a valuable tool for research investigating the role of KIF18A in cancer biology and potential therapeutic strategies. -
KSP Inhibitor
KSP-IA is a potent inhibitor of kinesin spindle protein (KSP), exhibiting an IC50 value of 3.6 nM. This compound effectively disrupts cell mitosis, making it a valuable tool for research in cancer biology and cellular division mechanisms. Its specificity for KSP underscores its potential in exploring therapeutic strategies that target mitotic processes. -
Kinesin Activator
TNH (TMP-NVOC linker-Halo) is a dimeric protein chemical inducer that activates kinesins, facilitating the targeted recruitment of proteins to cellular structures. This compound responds to light signals, enabling the dynamic interaction with kinetochores by either recruiting or releasing proteins, particularly CENP-E (kinesin-7). TNH is a valuable tool for studying protein dynamics in mitosis and investigating the mechanisms of cellular transport and division. -
Eg5 Inhibitor
Terpendole E is a specific inhibitor of the mitotic kinesin Eg5, targeting its motor and microtubule-stimulated ATPase activities in human cells. This compound effectively induces the formation of a monoastral spindle during the M phase of the cell cycle, making it a valuable tool for investigating mitotic processes. Terpendole E is suitable for research applications focused on cancer biology and drug discovery targeting cell division. -
CENP-M Inhibitor
Cenpemlin is a selective inhibitor of CENP-M, specifically disrupting the CENP-M/CENP-L interaction. This compound is valuable for studying centromere-kinetochore dynamics and assembly during cell division, providing insights into the mechanisms underlying chromosomal segregation. Research involving Cenpemlin can enhance the understanding of mitotic processes and potential therapeutic targets in cancer. -
Kinesin spindle protein
ALN-12115 is a small interfering RNA (siRNA) designed to specifically target kinesin spindle protein (KSP). It plays a key role in inhibiting mitotic spindle function, leading to cell cycle arrest and potential antitumor activity. ALN-12115 is part of the ALN-VSP lipid nanoparticle formulation, which also includes a siRNA targeting VEGF, making it suitable for research applications in cancer therapy and the study of tumor biology. -
Kinesin Inhibitor
MKLP2-IN-1 is a selective inhibitor of the kinesin MKLP2, demonstrating significant oral bioavailability. This compound effectively inhibits the microtubule-stimulated ATPase activity of recombinant MKLP2 in vitro, contributing to its potential as a therapeutic agent. In vivo studies reveal that MKLP2-IN-1 suppresses tumor growth in a mouse model of Calu-6 lung cancer, showcasing its relevance in cancer research and treatment strategies targeting kinesin-driven processes. -
KIF18A Inhibitor
KIF18A-IN-15 is a selective KIF18A inhibitor that demonstrates potent activity with IC50 values ranging from 0.01 to 0.1 μM. This compound effectively reduces the viability of OVCAR-3 cells, making it a valuable tool in cancer research. KIF18A-IN-15 can be utilized in studies related to various tumor models, including colon, breast, and lung cancers, facilitating the exploration of KIF18A's role in tumor growth and progression. -
KIF18A Inhibitor
KIF18A-IN-18 is a selective inhibitor of KIF18A, a motor protein involved in chromosome segregation during cell division. This compound has demonstrated the ability to disrupt KIF18A’s function, making it a valuable tool for studying chromosomal instability in tumors. Its application extends to research focused on understanding the mechanisms of tumorigenesis and potential therapeutic strategies in the context of cancer. -
HSET Inhibitor
CCT369834 is an ATP-competitive inhibitor of HSET, exhibiting an IC50 of 39 nM. This compound is a trans-cyclooctene-tagged probe that demonstrates specific co-localization with HSET on mitotic spindles. CCT369834 serves as a valuable tool for studying the role of HSET in cancer research and may contribute to understanding its function in mitotic processes. -
Kinesin Protein Ligand
KSP Ligand 1 is a selective ligand for kinesin spindle protein (KSP), which plays a critical role in cell division. This compound serves as a valuable tool in the development of proteolysis-targeting chimeras (PROTACs), specifically KSP-IN-1, for cancer research applications. Its ability to modulate KSP activity offers potential insights into therapeutic strategies for various malignancies. -
KIF18A Inhibitor
KIF18A-IN-16 is a potent inhibitor of KIF18A, a kinesin motor protein involved in mitotic spindle assembly and chromosome segregation. This compound has demonstrated significant biological activity in preclinical models and is valuable for research applications in oncology, particularly in the study of various cancer types, including colon, breast, and lung cancer. Its ability to disrupt KIF18A function makes it a promising candidate for investigating novel therapeutic strategies in cancer treatment. -
KSP Inhibitor
CK0106023 is a selective allosteric inhibitor of kinesin spindle protein (KSP) with a Ki value of 12 nM. This compound induces mitotic arrest and growth inhibition across various tumor cell lines, demonstrating significant antitumor activity. Additionally, CK0106023 has shown efficacy in preclinical models, specifically in tumor-bearing mice, making it a valuable reagent for cancer research and therapeutic development. -
Kinesin Inhibitor
4'-Methoxy-S-trityl-L-cysteinol is an allosteric inhibitor targeting vertebrate Kinesin Spindle Protein (KSP). This compound demonstrates enhanced inhibitory activity against NCI60 tumor cell lines, attributed to modifications in its trityl and cysteine groups. It exhibits an EC50 of 28 μM for bipolar spindle formation, indicating superior potency compared to its parent compound and monastrol. This makes it a valuable tool for investigating KSP's role in mitosis and potential therapeutic strategies in cancer research. -
Kinesin Inhibitor
Monastroline (HR22C16) is a selective inhibitor of the mitotic kinesin Eg5, which plays a critical role in mitosis and cell division. This compound effectively disrupts mitotic processes, making it a valuable tool for studying cell cycle regulation and kinesin function in cancer research and related fields. Monastroline demonstrates strong cell permeability, facilitating its use in cellular assays to explore the therapeutic potential of kinesin inhibition. -
Kinesin-13 Inhibitor
DHTP is a selective allosteric inhibitor of the kinesin-13 family of microtubule depolymerases, targeting ATPase activity and microtubule depolymerization. It inhibits Kif2a and MCAK with IC50 values of 1.2 μM and 4.6 μM, respectively, without affecting other kinesin families. By modulating microtubule dynamics in cells, DHTP results in reduced microtubule activity, linking kinesin-13 overexpression to cancer progression and resistance to Paclitaxel. This compound is suitable for cancer research applications. -
SKP Inhibitor
KSP-IN-1 is a potent kinesin spindle protein (KSP) inhibitor, exhibiting an IC50 of 450 nM. This compound effectively disrupts mitotic spindle formation, thereby hindering cell division. KSP-IN-1 is valuable for researchers investigating cancer mechanisms and the role of mitotic regulation in oncology.

