Kinesin Inhibitor

EMD534085 is a potent and selective inhibitor of the mitotic kinesin-5 with an IC₅₀ of 8 nM.

KIF2C-IN-1 is a cell-penetrating, selective KIF2C inhibitor with fluorescent properties (E_x/E_m = 410/510 nm). KIF2C-IN-1 exhibits notable cytotoxicity and weak inhibitory effects on KIF2A/B. KIF2C-IN-1 prohibits the dissociation of KIF2C from microtubules. KIF2C-IN-1 inhibiting KIF2C reverses cross-resistance to microtubule-targeting agents. KIF2C-IN-1 reduces tumorigenesis in chemoresistant triple-negative breast cancer (TNBC) model in mice with the combination of Paclitaxel (HY-B0015).

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.

AM-9022 is an orally active, potent, selective KIF18A inhibitor that can be used for research on cancer.

MC-Val-Cit-PAB-Ispinesib (Compound 509) is a drug-linker conjugate for ADC, consisting of a cleavable ADC linker and Eg5 inhibitor. MC-Val-Cit-PAB-Ispinesib can be used for the synthesis of antibody-drug conjugates (ADCs).

GW406108X is a specific Kif15 (Kinesin-12) inhibitor with an IC₅₀ of 0.82 uM in ATPase assays. GW406108X, a potent autophagy inhibitor, shows ATP competitive inhibition against ULK1 with a pIC₅₀ of 6.37 (427 nM). GW406108X inhibits ULK1 kinase activity and blocks autophagic flux, without affecting the upstream signaling kinases mTORC1 and AMPK.

AM-5308 is the inhibitor for KIF18A (IC₅₀=47 nM) that inhibits KIF18A-mediated microtubule ATPase activity. AM-5308 activates mitotic checkpoints, regulates cell division processes, including chromosome segregation and spindle assembly. AM-5308 exhibits antitumor activity.

PVZB1194 is a biphenyl-type inhibitor of Kinesin-5 ATPase activity that binds to the α4/α6 site of the motor domain in a nucleotide competitive manner. PVZB1194 has an IC₅₀ of 0.12 μM for KSP ATPase. PVZB1194 induces mitotic arrest with the formation of a monopolar spindle, and inhibits HeLa cells proliferatio (IC₅₀: 5.5 μM). PVZB1194 can be used in the study of tumors.

ARQ 621 is an allosteric, potent and selective inhibitor of Eg5, a microtubule-based ATPase motor protein involved in cell division. Anti-tumor activity. ARQ 621 is a kinesin inhibitor. ARQ 621 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

K858 Racemic is an ATP-uncompetitive inhibitor of kinesin Eg5 with an IC₅₀ of 1.3 μM.

SR31527 chloride is a potent KIFC1 inhibitor with an IC₅₀ value of 6.6 µM. SR31527 chloride decreases cell viability and colony formation.

PF-2771 is a potent and selective centromere protein E (CENP-E) inhibitor, inhibiting CENP-E motor activity with an IC₅₀ of 16.1 nM; PF-2771 is used as an anticancer agent.

KIF18A-IN-13 (Compound 16) is an effective and orally active inhibitor of KIF18A with anticancer activity in vivo. KIF18A-IN-13 can be utilized for research in ovarian cancer.

LP-6 TFA is a Drug-Linker Conjugate for ADC, and can be used for synthesis of ADCs. LP-6 TFA consists of an Eg5 inhibitor and a linker.

Syntelin is a selective centromere protein E (CENP-E) inhibitor with IC₅₀ at 160 nM. Syntelin has antitumor activity.

Mitotic kinesin-IN-1 (Example 80) hydrochloride is a Mitotic kinesin inhibitor. Mitotic kinesin-IN-1 hydrochloride inhibits cell proliferation by suppressing mitosis. Mitotic kinesin-IN-1 hydrochloride can be used for cancer, cardiac hypertrophy, immune and inflammatory disorders, fungal infections research.

KIF18A-IN-2 is a potent KIF18A inhibitor (IC₅₀=28 nM). KIF18A-IN-2 causes significant mitotic arrest and increases the number of mitotic cells in tumor tissues. KIF18A-IN-2 can be used for researching cancer.

KIF18A-IN-3 is a potent KIF18A inhibitor (IC₅₀=61 nM). KIF18A-IN-3 causes significant mitotic arrest and increases the number of mitotic cells in tumor tissues. KIF18A-IN-3 can be used for researching cancer.

Mitotic kinesin-IN-2 (Page 135, fifteenth) hydrochloride is a Mitotic kinesin inhibitor. Mitotic kinesin-IN-2 hydrochloride inhibits cell proliferation by suppressing mitosis. Mitotic kinesin-IN-2 hydrochloride can be used for cancer, cardiac hypertrophy, immune and inflammatory disorders, fungal infections research.

LP-6 is a Drug-Linker Conjugate for ADC, and can be used for synthesis of ADCs. LP-6 consists of an Eg5 inhibitor and a linker.