Structure of CK-666
CAS No.: 442633-00-3
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
CK 666 is an inhibitor of Arp2/3 complex. It can inhibit actin polymerization (IC50 = 4 μM).
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CAS No. : | 442633-00-3 |
Formula : | C18H17FN2O |
M.W : | 296.34 |
SMILES Code : | CC(NC1=CC=CC=C21)=C2CCNC(C3=C(F)C=CC=C3)=O |
MDL No. : | MFCD03036271 |
InChI Key : | UXRKUKRXVWJFER-UHFFFAOYSA-N |
Pubchem ID : | 589075 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302 |
Precautionary Statements: | P264-P270-P301+P312-P330-P501 |
Description |
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].
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In Vitro:
Cell Line
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Concentration | Treated Time | Description | References |
Pfa1 cells | 100 μM | 72 h | CK-666 significantly mitigated tamoxifen-induced ferroptosis | J Biol Chem. 2024 Dec;300(12):107942. |
293T cells | 100 μM | 24 h | CK-666 significantly mitigated RSL3-induced ferroptosis | J Biol Chem. 2024 Dec;300(12):107942. |
BJ fibroblasts | 100 μM | 24 h | CK-666 significantly mitigated RSL3-induced ferroptosis | J Biol Chem. 2024 Dec;300(12):107942. |
bone marrow-derived macrophages | 100 µM | 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 |
In Vivo:
Species
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Animal Model
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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 | Plant Cell. 2024 Feb 26;36(3):764-789 |
Bio Calculators | ||||
Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
3.37mL 0.67mL 0.34mL |
16.87mL 3.37mL 1.69mL |
33.75mL 6.75mL 3.37mL |
Tags: CK-666 | CK666 | CK 666 | Arp2/3 Complex | HIV | Actin-related protein 2/3 complex | Human immunodeficiency virus | trabecular | meshwork | allosteric | effector | state | inhibitor | 442633-00-3 |
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