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Purity: ≥98%
CK-869 is a small molecule inhibitor of human and bovine actin-related protein 2/3 (Arp2/3) complex which is a seven-subunit assembly that nucleates branched actin filaments. The mode of action of CK-869 is to bind to Arp2/3 complex and inhibit nucleation. CK-869 binds to a serendipitous pocket on Arp3 and allosterically destabilizes the short pitch Arp3-Arp2 interface. These results provide key insights into the relationship between conformation and activity in Arp2/3 complex and will be critical for interpreting the influence of the inhibitors on actin filament networks in vivo.
| ln Vitro |
CK-869 is an Actin-Related Protein 2/3 (ARP2/3) complex inhibitor, with an IC50 of 7 μM[1]. CK-869 strongly inhibits MT polymerization even at a dose of 25 μM[2].
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| References |
[1]. Hetrick B, et al. Small molecules CK-666 and CK-869 inhibit actin-related protein 2/3 complex by blocking an activating conformational change. Chem Biol. 2013 May 23;20(5):701-12.
[2]. Yamagishi Y, et al. Use of CK-548 and CK-869 as Arp2/3 complex inhibitors directly suppresses microtubule assembly both in vitro and in vivo. Biochem Biophys Res Commun. 2018 Feb 12;496(3):834-839. |
| Molecular Formula |
C17H16BRNO3S
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| Molecular Weight |
394.28
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| CAS # |
388592-44-7
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| SMILES |
BrC1=C([H])C([H])=C([H])C(=C1[H])C1([H])N(C(C([H])([H])S1)=O)C1C([H])=C([H])C(=C([H])C=1OC([H])([H])[H])OC([H])([H])[H]
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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 (6.34 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 (6.34 mM) (saturation unknown) 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. 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 (6.34 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 | 2.5363 mL | 12.6813 mL | 25.3627 mL | |
| 5 mM | 0.5073 mL | 2.5363 mL | 5.0725 mL | |
| 10 mM | 0.2536 mL | 1.2681 mL | 2.5363 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.
 CK-666 andCK-869bind to different sites on Arp2/3 complex.Chem Biol.2013 May 23;20(5):701-12. |
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 CK-869influences ATP-induced conformational changes in Arp3.Chem Biol.2013 May 23;20(5):701-12. |
 Cartoon showing proposed structural bases for inhibition of Arp2/3 complex byCK-869and CK-666.Chem Biol.2013 May 23;20(5):701-12. |
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