Kif18A is a mitotic motor protein essential for the correct alignment of chromosomes at the spindle equator. BTB1 potently inhibits the ATPase activity of Kif18A with an IC50 value of 1.69μM. The re-synthesized BTB1 inhibited His-Kif18Amotor with equal potency (IC50=1.86μM). The flushing in of 100μM BTB1 almost completely inhibited His-Kif18AFL-dependent microtubule motility. After the wash-out of BTB1, His-Kif18AFL regained most of its activity. The ATPase activity of His-Kif18Amotor was not affected by BTB1(100μM) in the absence of microtubules. BTB1 significantly inhibited microtubule-stimulated ATPase activity of His-Kif18Amotor as compared to the DMSO-treated group. Incubation of HeLa cells with BTB1 (30 and 40μM) for 18h induced the accumulation of cells in mitosis[3].
作用机制
BTB1 is a potent and selective Kif18A inhibitor that reversibly inhibits the motility of Kif18A in an ATP-competitive manner[3].
BTB-1 细胞实验
Cell Line
Concentration
Treated Time
Description
References
A549 cells
A549 cells
To evaluate the effect of BTB-1 on IAV-induced cytopathic effect. BTB-1 treatment significantly reduced the IAV-induced cytopathic effect.
J Cell Mol Med. 2020 May;24(10):5463-5475.
HEK293 cells
HEK293 cells
To evaluate the effect of BTB-1 on IAV-induced cytopathic effect. BTB-1 treatment significantly reduced the IAV-induced cytopathic effect.
J Cell Mol Med. 2020 May;24(10):5463-5475.
MDCK cells
MDCK cells
To evaluate the effect of BTB-1 on IAV-induced cytopathic effect. BTB-1 treatment significantly reduced the IAV-induced cytopathic effect.
J Cell Mol Med. 2020 May;24(10):5463-5475.
BTB-1 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6 mice
IAV infection model
Intranasal administration
3 mg/kg
Administered at 10 minutes, 3 hours, and 6 hours post-infection
To evaluate the protective effect of BTB-1 on IAV-infected mice. BTB-1 treatment significantly improved the survival rate and reduced weight loss in infected mice.
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