CK 869Arp2/3 inhibitor; inhibits actin polymerization CAS# 388592-44-7 |
- Narciclasine
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| Cas No. | 388592-44-7 | SDF | Download SDF |
| PubChem ID | 3574452 | Appearance | Powder |
| Formula | C17H16BrNO3S | M.Wt | 394.28 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | CK-0157869 | ||
| Solubility | DMS : 75 mg/mL (190.22 mM; Need ultrasonic) H2O : < 0.1 mg/mL (insoluble) | ||
| Chemical Name | 2-(3-bromophenyl)-3-(2,4-dimethoxyphenyl)-1,3-thiazolidin-4-one | ||
| SMILES | COC1=CC(=C(C=C1)N2C(SCC2=O)C3=CC(=CC=C3)Br)OC | ||
| Standard InChIKey | MVWNPZYLNLATCH-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C17H16BrNO3S/c1-21-13-6-7-14(15(9-13)22-2)19-16(20)10-23-17(19)11-4-3-5-12(18)8-11/h3-9,17H,10H2,1-2H3 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Inhibitor of human and bovine actin-related protein 2/3 (Arp2/3) complex. Inhibits actin polymerization (IC50= 11 μM). Does not inhibit budding or fission yeast Arp2/3 complexes. |
CK 869 Dilution Calculator
CK 869 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.5363 mL | 12.6813 mL | 25.3627 mL | 50.7254 mL | 63.4067 mL |
| 5 mM | 0.5073 mL | 2.5363 mL | 5.0725 mL | 10.1451 mL | 12.6813 mL |
| 10 mM | 0.2536 mL | 1.2681 mL | 2.5363 mL | 5.0725 mL | 6.3407 mL |
| 50 mM | 0.0507 mL | 0.2536 mL | 0.5073 mL | 1.0145 mL | 1.2681 mL |
| 100 mM | 0.0254 mL | 0.1268 mL | 0.2536 mL | 0.5073 mL | 0.6341 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Small molecules CK-666 and CK-869 inhibit actin-related protein 2/3 complex by blocking an activating conformational change.[Pubmed:23623350]
Chem Biol. 2013 May 23;20(5):701-12.
Actin-related protein 2/3 (Arp2/3) complex is a seven-subunit assembly that nucleates branched actin filaments. Small molecule inhibitors CK-666 and CK-869 bind to Arp2/3 complex and inhibit nucleation, but their modes of action are unknown. Here, we use biochemical and structural methods to determine the mechanism of each inhibitor. Our data indicate that CK-666 stabilizes the inactive state of the complex, blocking movement of the Arp2 and Arp3 subunits into the activated filament-like (short pitch) conformation, while 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.
Characterization of two classes of small molecule inhibitors of Arp2/3 complex.[Pubmed:19648907]
Nature. 2009 Aug 20;460(7258):1031-4.
Polymerization of actin filaments directed by the actin-related protein (Arp)2/3 complex supports many types of cellular movements. However, questions remain regarding the relative contributions of Arp2/3 complex versus other mechanisms of actin filament nucleation to processes such as path finding by neuronal growth cones; this is because of the lack of simple methods to inhibit Arp2/3 complex reversibly in living cells. Here we describe two classes of small molecules that bind to different sites on the Arp2/3 complex and inhibit its ability to nucleate actin filaments. CK-0944636 binds between Arp2 and Arp3, where it appears to block movement of Arp2 and Arp3 into their active conformation. CK-0993548 inserts into the hydrophobic core of Arp3 and alters its conformation. Both classes of compounds inhibit formation of actin filament comet tails by Listeria and podosomes by monocytes. Two inhibitors with different mechanisms of action provide a powerful approach for studying the Arp2/3 complex in living cells.
