Kinesin

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-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-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-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)-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-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-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.

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.

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.

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.

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.

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-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-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.

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.

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-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.

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.

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.

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.

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.

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.

NSC-80141 is a selective inhibitor of kinesin-5, targeting the human kinesin-5 (HsEg5) with an IC50 of 9.4 μM, while exhibiting weaker inhibition against Plasmodium kinesin-5 (PvEg5) at an IC50 of 27.3 μM. This compound is valuable for research applications focused on differentiating human kinesin-5 from its Plasmodium counterpart, making it a useful tool for studying cellular transport mechanisms and potential therapeutic interventions in parasitic infections.