CK-666 is a potent inhibitor of the Arp2/3 complex, an actin-related protein, displaying an IC50 value of 12 μM. By binding to the Arp2/3 complex, CK-666 stabilizes its inactive form and prevents the movement of Arp2 and Arp3 subunits into an activated, filament-like conformation[1].[2].
Study the effects of CK-666 and CK-869 on macrophage phagocytosis and motility. CK-869 significantly impacted phagocytosis and cell migration, while CK-666 had no discernible effect.
EMBO Rep. 2024 Aug;25(8):3221-3239
HeLa cells
50, 100, 200, 300 µM
60 min
Investigate the effects of CK-666 and CK-869 on vaccinia virus-induced actin polymerization. CK-869 nearly completely inhibited virus-induced actin assembly, while CK-666 reduced actin polymerization by ~30% even at 300 µM.
EMBO Rep. 2024 Aug;25(8):3221-3239
Ptk2 cells
100 μM
To study the effect of CK-666 on L. monocytogenes motility in Ptk2 cells, results showed immediate cessation of bacterial movement and disintegration of comet tails upon CK-666 treatment
mBio. 2018 Apr 10;9(2):e02259-17
HeLa cells
100 μM
To study the effect of CK-666 on L. monocytogenes motility in HeLa cells, results showed immediate cessation of bacterial movement and disintegration of comet tails upon CK-666 treatment
mBio. 2018 Apr 10;9(2):e02259-17
Human trabecular meshwork cells
100 μM
24 h
CK-666 significantly reduced the number and length of filopodia on the surface of TM cells and decreased the transfer of fluorescently labeled vesicles.
Invest Ophthalmol Vis Sci. 2017 Oct 1;58(12):5298-5307
HT1080 cells
100 μM
24 h
CK-666 significantly mitigated ferroptosis induced by both RSL3 and erastin
J Biol Chem. 2024 Dec;300(12):107942.
human brain microvascular endothelial cells (hCMEC/D3 cells)
80 μM
1 hour
Inhibition of Arp2/3 complex activity protected against METH-induced enhanced F-actin formation and occludin internalization
J Biol Chem. 2013 Nov 15;288(46):33324-34
Mouse embryonic fibroblasts (IA32)
150 µM
2 h
Used to synchronize lamellipodia in cells, CK-666 treatment caused complete loss of lamellipodia, which regrew upon drug washout
J Cell Biol. 2015 Jun 22;209(6):803-12
Arabidopsis epidermal cells
10 µM
5 min
Inhibits Arp2/3 complex activity, significantly reducing the frequency of side-branched nucleation events and overall actin filament abundance
Plant Cell. 2024 Feb 26;36(3):764-789
CK-666 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6 mice
Renal ischemia-reperfusion injury model
Intraperitoneal injection
30 mg/kg
24 hours and 2 hours before surgery
CK-666 significantly ameliorated renal ischemia-reperfusion injury and ferroptosis
J Biol Chem. 2024 Dec;300(12):107942.
C57BL/6 mice
METH-induced blood-brain barrier disruption model
Intraperitoneal injection
5 mg/kg
Single dose, lasting 1 hour
Pretreatment with CK-666 attenuated METH-induced decrease in occludin levels in brain microvessels and increased BBB permeability
J Biol Chem. 2013 Nov 15;288(46):33324-34
Arabidopsis
Arabidopsis epidermal cells
Solution treatment
10 µM
Single treatment, lasting 5 minutes
Acutely inhibits Arp2/3 complex activity, mimicking the phenotypes of arp2/3 mutants, reducing actin filament abundance and side-branched nucleation events
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