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| 10mg |
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| 1g |
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Purity: ≥98%
CK-636 (also called CK636; CK-0944636; CK0944636) is a potent inhibitor of the actin-related protein (Arp2/3) complex with IC50 values of 4 μM, 24 μM and 32 μM for inhibition of actin polymerization induced by human, fission yeast and bovine Arp2/3 complex, respectively. CK-636 binds between Arp2 and Arp3 where it appears to block movement of Arp2 and Arp3 into their active conformation and inhibits Arp2/3 complex’s ability to nucleate actin filaments. In a concentration dependence way, CK-636 reduced the formation of actin filament comet tails by Listeria with IC50 value of 22 μM in infected SKOV3 cells.
| Targets |
CK-636 (CK-0944636) specifically targets the Arp2/3 complex, with an IC50 of 0.5 μM for inhibiting Arp2/3-mediated actin polymerization and a Ki of 0.3 μM for binding to the Arp2/3 complex [1]
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| ln Vitro |
Arp2 and Arp3 appear to be prevented from adopting their active conformations by CK-636, which binds between them. CK-636 modifies the conformation of Arp3 by inserting into its hydrophobic core. Infected SKOV3 cells (IC50=22 μM), CK-636 inhibits actin polymerization and Listeria monocytogenes' production of actin filament comet tails [1]. T cells treated with CK-636 also exhibited an elongated morphology with sharp pseudopodia at the leading edge, and their width was roughly 30% less than that of T cells treated with DMSO [2].
In human non-small cell lung cancer A549 cells and breast cancer MDA-MB-231 cells, CK-636 (1-5 μM) dose-dependently inhibited cell migration, reducing migration distance by 70% (A549) and 75% (MDA-MB-231) at 2 μM in scratch-wound assays [1] - CK-636 (0.5 μM) inhibited Arp2/3-mediated actin nucleation by 80% in vitro, reducing the formation of actin patches and lamellipodia in A549 cells [1] - In human T cells, CK-636 (2 μM) suppressed migration on complex nanotopographic surfaces by 65%, disrupting actin cytoskeleton reorganization required for directional movement [2] - CK-636 (1-3 μM) reduced migrasome formation in migrating NIH/3T3 fibroblasts by 72% at 2 μM, as migrasome biogenesis depends on Arp2/3-mediated actin assembly [3] - Immunofluorescence staining showed CK-636 (1 μM) disrupted the colocalization of Arp2/3 complex with actin filaments in lamellipodia of MDA-MB-231 cells [1] |
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| ln Vivo |
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| Enzyme Assay |
Arp2/3-mediated actin polymerization inhibition assay: Purified Arp2/3 complex (20 nM) was incubated with actin monomers (2 μM), WASP-VCA domain (100 nM), and serial concentrations of CK-636 (0.1-10 μM) in polymerization buffer at 25°C. Actin polymerization was monitored by measuring fluorescence intensity of pyrene-labeled actin over 30 minutes, and IC50 values were calculated from dose-response curves [1]
- Arp2/3 complex binding assay: Recombinant Arp2/3 complex was immobilized on a sensor chip, and serial concentrations of CK-636 (0.2-15 μM) were injected. Binding affinity was measured by surface plasmon resonance (SPR), and the dissociation constant (Ki) was derived as 0.3 μM [1] |
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| Cell Assay |
Cell migration assay: A549/MDA-MB-231 cells were seeded in 6-well plates and scratched with a pipette tip. CK-636 (0.5-5 μM) was added, and wound closure rate was quantified by imaging at 0 and 24 hours. For T cell migration, human T cells were seeded on nanotopographic surfaces and treated with CK-636 (1-3 μM), with migration tracks analyzed by time-lapse microscopy [1][2]
- Actin cytoskeleton visualization assay: A549/MDA-MB-231 cells were treated with CK-636 (0.5-2 μM) for 16 hours, fixed, and stained with fluorescently labeled phalloidin (for actin) and anti-Arp2 antibody (for Arp2/3 complex). Actin structures and Arp2/3 localization were visualized by confocal microscopy [1] - Migrasome detection assay: NIH/3T3 fibroblasts were treated with CK-636 (1-3 μM) for 24 hours, stained with DiI (a membrane dye), and migrasomes were observed and counted under a fluorescence microscope. Migrasome size and number were quantified relative to vehicle controls [3] |
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| Animal Protocol |
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| References |
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| Additional Infomation |
CK-636 is a small molecule Arp2/3 complex inhibitor, which is a key regulator of actin cytoskeleton dynamics[1]. Its mechanism of action is to bind to the Arp2/3 complex and block its ability to assemble nucleated actin filaments, thereby disrupting pseudopodia formation, cell migration, and migratory body biosynthesis[1][2][3]. CK-636 has been widely used as a research tool to study the role of Arp2/3-mediated actin dynamics in cell migration, immune cell function, and organelle biosynthesis (e.g., migratory bodies)[1][2][3]. At concentrations up to 5 μM, CK-636 can effectively and specifically inhibit Arp2/3 activity without significant cytotoxicity to normal or cancer cells[1].
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| Molecular Formula |
C16H16N2OS
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| Molecular Weight |
284.38
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| Exact Mass |
284.098
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| CAS # |
442632-72-6
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| Related CAS # |
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| PubChem CID |
588963
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
576.8±45.0 °C at 760 mmHg
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| Flash Point |
302.6±28.7 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.674
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| LogP |
3.1
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
20
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| Complexity |
349
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ACAKNPKRLPMONU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H16N2OS/c1-11-12(13-5-2-3-6-14(13)18-11)8-9-17-16(19)15-7-4-10-20-15/h2-7,10,18H,8-9H2,1H3,(H,17,19)
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| Chemical Name |
N-[2-(2-Methyl-1H-indol-3-yl)ethyl]-2-thiophenecarboxamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.79 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (8.79 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5164 mL | 17.5821 mL | 35.1642 mL | |
| 5 mM | 0.7033 mL | 3.5164 mL | 7.0328 mL | |
| 10 mM | 0.3516 mL | 1.7582 mL | 3.5164 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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