CK 666 |
| رقم الكتالوجGC14060 |
CK 666 هو مثبط مركب Arp2 / 3 البروتين المرتبط بالأكتين المنفذ للخلايا (IC50 \u003d 12 ميكرومتر).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 442633-00-3
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
CK 666 is a cell-permeable actin-related protein Arp2/3 complex inhibitor (IC50=12μM)[1]. CK 666 binds to Arp2/3 complex, stabilizes the inactive state of the complex, blocking movement of the Arp2 and Arp3 subunits into the activated filament-like (short pitch) conformation[2]. CK 666 is routinely used in studies of cytoskeletal dynamics such as cell migration, phagocytosis and cytokinesis[3][4].
In vitro, CK 666 (100μM; 24h) inhibited proliferation in KYSE-30 esophageal, T24 bladder, MDA-MB-231 breast, FaDu hypopharyngeal and SKOV3 ovarian cancer cells, elevated LC3-II, decreased p62 to promote autophagy, and increased release of CD63⁺exosome-like vesicles[5]. Pretreatment of human lung microvascular endothelial cells (HLMVEC) and pulmonary artery endothelial cells (HPAEC)with CK 666 (50μM) 1h before sphingosine-1-phosphate (S1P)-induction significantly reduced trans-endothelial electrical resistance (TER), attenuated S1P-induced barrier enhancement, and markedly decreased individual lamellipodium depth[6].
In vivo, CK 666 (30mg/kg; i.p.; once 24h and once 2h before ischemia) markedly decreased serum creatinine and blood urea nitrogen levels, reduced renal malondialdehyde (MDA) content, attenuated tubular necrosis, and significantly lowered TUNEL-positive apoptotic cells in a mouse renal ischemia–reperfusion injury model[7].
References:
[1] Hetrick B, Han MS, Helgeson LA, Nolen BJ. Small molecules CK-666 and CK-869 inhibit actin-related protein 2/3 complex by blocking an activating conformational change. Chem Biol. 2013;20(5):701-712.
[2] Nolen BJ, Tomasevic N, Russell A, et al. Characterization of two classes of small molecule inhibitors of Arp2/3 complex. Nature. 2009;460(7258):1031-1034.
[3] Liu CS, Cheung PW, Dinesh A, et al. Actin-related protein 2/3 complex plays a critical role in the aquaporin-2 exocytotic pathway. Am J Physiol Renal Physiol. 2021;321(2):F179-F194.
[4] Efremov YM, Dokrunova AA, Efremenko AV, Kirpichnikov MP, Shaitan KV, Sokolova OS. Distinct impact of targeted actin cytoskeleton reorganization on mechanical properties of normal and malignant cells. Biochim Biophys Acta. 2015;1853(11 Pt B):3117-3125.
[5] Li L, Cai S, Chen J, et al. CK-666 exerts anticancer effects by regulating autophagy, tunneling nanotubes and extracellular vesicles formation. Biomed Pharmacother. 2025;183:117825.
[6] Belvitch P, Brown ME, Brinley BN, et al. The ARP 2/3 complex mediates endothelial barrier function and recovery. Pulm Circ. 2017;7(1):200-210.
[7] Hu Q, Zhao Y, Sun WY, et al. CK-666 protects against ferroptosis and renal ischemia-reperfusion injury through a microfilament-independent mechanism. J Biol Chem. 2024;300(12):107942.
| Cell experiment [1]: | |
Cell lines | Human pulmonary artery EC (HPAECs) or human lung microvascular EC (HLMVECs) |
Preparation Method | Human pulmonary artery EC (HPAECs) or human lung microvascular EC (HLMVECs) were cultured in Endothelial Basal Medium (EBM)-2 complete medium supplemented with 10% (v/v) fetal bovine serum (FBS) in a humidified incubator with 5% CO2 at 37°C. EC monolayer barrier function was assessed by an electrical cell-substrate impedance sensing system. In this assay, ECs are grown in wells containing gold microelectrodes on the basal surface allowing the measurement of impedance to a small AC electrical current at a frequency of 4000Hz. Once a baseline resistance (TER) was established, the monolayer was treated with vehicle (0.3% DMSO) or CK 666 (50μM) for 1h followed by thrombin (1U/mL) or S1P (1μM) and monitored continuously for up to 12h. Values are expressed as mean resistance, measured in ohms, or normalized resistance compared to baseline values with the means of several wells pooled in each independent experiment. Baseline resistance in HLMVECs was calculated from three independent experiments with 2–4 repeats of each condition. The maximal change in HPAEC normalized resistance as well as the rate of change (normalized resistance/h) following S1P was calculated from seven independent experiments with each experiment composed of 2–4 repeats of each condition. The time to recovery of baseline barrier function following thrombin (measured in minutes) was calculated from nine independent experiments with each experiment composed of 2–4 repeats of each condition. |
Reaction Conditions | 50μM; 1h |
Applications | Pretreatment of human lung microvascular endothelial cells (HLMVEC) and pulmonary artery endothelial cells (HPAEC)with CK 666 (50μM) 1h before sphingosine-1-phosphate (S1P)-induction significantly reduced trans-endothelial electrical resistance (TER). |
| Animal experiment [2]: | |
Animal models | C57BL/6 WT mice |
Preparation Method | C57BL/6 WT mice were intraperitoneally injected with CK 666 (30mg/kg) 24h and 2h before surgery. The mice were anesthetized, and bilateral renal pedicles were clamped for 35min to induce renal ischemia-reperfusion injury, during which the body temperature of mice was maintained on a heat plate at 38°C. The mice in the Sham group underwent the same procedures as those in the renal I/R group except for drug administration and clamping. The mice were sacrificed 24h after surgery. Serum and tissue samples were collected for subsequent testing. |
Dosage form | 30mg/kg; i.p.; once 24h and once 2h before ischemia |
Applications | CK 666 markedly decreased serum creatinine and blood urea nitrogen levels, reduced renal malondialdehyde (MDA) content, attenuated tubular necrosis in a mouse renal ischemia–reperfusion injury model. |
References: | |
| Cas No. | 442633-00-3 | SDF | |
| Chemical Name | 2-fluoro-N-(2-(2-methyl-1H-indol-3-yl)ethyl)benzamide | ||
| Canonical SMILES | FC1=CC=CC=C1C(NCCC2=C(C)NC3=CC=CC=C23)=O | ||
| Formula | C18H17FN2O | M.Wt | 296.34 |
| الذوبان | <29.63mg/ml in DMSO; <29.63mg/ml in ethanol | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.3745 mL | 16.8725 mL | 33.745 mL |
| 5 mM | 674.9 μL | 3.3745 mL | 6.749 mL |
| 10 mM | 337.5 μL | 1.6873 mL | 3.3745 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *