Kinesin-5/Eg5/KSP Inhibitor

Ispinesib is a specific inhibitor of kinesin spindle protein (KSP), with a K_{i app} of 1.7 nM.

Monastrol is a potent and cell-permeable inhibitor of the mitotic kinesin Eg5 with an IC₅₀ value of 14 μM.

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.

Filanesib (ARRY-520) is a selective and noncompetitive kinesin spindle protein (KSP) inhibitor, with an IC₅₀ of 6 nM for human KSP. Filanesib induces cell death by apoptosis in vitro. Filanesib has potent anti-proliferative activity.

SB-743921 hydrochloride is a potent inhibitor of the mitotic kinesin KSP (Eg5), with a K_i of 0.1 nM.

Kolaflavanone is an biflavonoid allosteric inhibitor of Eg5. Kolaflavanone inhibits the ATPase and tyrosinase activities of Eg5 under both basal and microtubule-activated conditions, suppresses microtubule sliding activity, binds to the L5/α2/α3 allosteric pocket of Eg5, induces conformational changes of Eg5 and microtubule dissociation, interacts with aldehyde dehydrogenase, inhibits the ATPase activity of kinesin-1, and binds to HSA via pH-dependent forces. Kolaflavanone exhibits antihepatotoxic activity and can be used in studies related to Phalloidin (HY-P0028)-induced liver injury.

O-Trityl-L-serine is an inhibitor of human mitotic kinesin Eg5, with a K_i^app of 750 nM. O-Trityl-L-serine does not induce monopolar spindle formation or mitotic arrest in cancer cells. O-Trityl-L-serine can be used in cancer-related research.

Dimethylenastron is a potent kinesin 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 pK_a 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.

Litronesib (LY2523355) is a selective mitosis-specific kinesin Eg5 inhibitor, with antitumor activity.

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

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.

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.

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.

Eg5 Inhibitor V, trans-24 is a potent and specific kinesin Eg5 inhibitor with an IC₅₀ of 0.65 μM, and can be used in the research of cancer.

CCT368772 (compound 35) is a selective kinesin HSET inhibitor (HSET ADP-Glo IC₅₀ = 0.019 μM). CCT368772 exhibits selectivity over Eg5 (Eg5 ADP-Glo IC₅₀ >200 μM). CCT368772 (compound 152) can be used for the study of hyperproliferative diseases and disorders such as cancer.

NVP-BQS481 (Compound 1) is a selective Kinesin spindle protein-5 (Eg5) inhibitor with an IC₅₀< 0.5 nM. NVP-BQS481 has significant antimitotic and antitumor activity (IC₅₀: 0.0.9 nM for SK-OV-3ip cells). NVP-BQS481 can be used as a cytotoxic payload for synthesis of antibody-drug conjugates (ADCs).

Terpendole E is a mitotic kinesin Eg5 inhibitor. Terpendole E inhibits both motor and microtubule-stimulated ATPase activities of human Eg5. Terpendole E induces formation of a monoastral spindle in M phase.