KIF18A-IN-4

Names

[ CAS No. ]:
1197522-21-6

[ Name ]:
KIF18A-IN-4

Biological Activity

[Description]:

KIF18A-IN-4 is a moderately potent ATP and microtubule (MT) noncompetitive KIF18A inhibitor (IC50=6.16 μM). KIF18A-IN-4 has selectivity against a large panel of mitotic kinesins and kinases, and does not show any direct effects on tubulin assembly. KIF18A-IN-4 exhibits anti-tumor activity[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Cell Cycle/DNA Damage >> Microtubule/Tubulin
Signaling Pathways >> Cytoskeleton >> Microtubule/Tubulin

[Target]

IC50: 6.16 μM (KIF18A)[1]


[In Vitro]

KIF18A-IN-4 (15 μM; 24 hours) induces a phenotype characterized by multipolar spindle arrays emanating from multiple pericentriolar material (PCM) centers in mitotic MDA-MB-157 cells (pH3+)[1]. KIF18A-IN-4 (0-10 μM; overnight) has an EC50 of 6.35 μM in OVCAR-3 cells by the mitotic index assay[1].

[References]

[1]. Tamayo NA, et al. Targeting the Mitotic Kinesin KIF18A in Chromosomally Unstable Cancers: Hit Optimization Toward an In Vivo Chemical Probe. J Med Chem. 2022;65(6):4972-4990.

Chemical & Physical Properties

[ Molecular Formula ]:
C22H27N3O3S

[ Molecular Weight ]:
413.53

Related Compounds