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| 2-Fluoro-N-[2-(2-methyl-1H-indol-3-yl)ethyl]benzamide Basic information |
| 2-Fluoro-N-[2-(2-methyl-1H-indol-3-yl)ethyl]benzamide Chemical Properties |
| Boiling point | 528.2±50.0 °C(Predicted) | | density | 1.235±0.06 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | DMSO: ≥25mg/mL | | form | powder | | pka | 13.86±0.46(Predicted) | | color | white to tan | | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. |
| Hazard Codes | Xi | | Risk Statements | 36 | | Safety Statements | 26 | | WGK Germany | 3 |
| 2-Fluoro-N-[2-(2-methyl-1H-indol-3-yl)ethyl]benzamide Usage And Synthesis |
| Description | CK-666 (442633-00-3) is a potent, selective and reversible inhibitor of ARP2/3 complex (actin related proteins 2 and 3) with an IC50?= 4 μM for human ARP2/3.1?Blocks actin nucleation and radically alters lamellipodial actin architecture, suspended cell shape and the cell spreading process.2 CK-666 attenuates BBB dysfunction induced by methamphetamine.3?It is an important new tool for studying actin assembly and the diverse range of actin-related processes in normal4 and pathophysiology5. | | Uses | CK-666 may be used to study Arp2/3-mediated structural changes in cells. | | General Description | A cell-permeable indolyl-fluorobenzamide compound that selectively inhibits actin assembly mediated by actin-related protein Arp2/3 complex of human, bovine, fission yeast S. pombe, and budding yeast S. cerevisiae origin (IC50 = 4, 17, 5, and 12 μM, respectively), without affecting S. pombe formin domain Cdc12(FH2)-mediated or the spontaneous actin polymerization. Shown to inhibit the actin filament "comet tails" formation around intracellular Listeria in infected SKOV3 cells (IC50 = 7 μM) in a reversible manner. Structrual studies indicate that CK-666 targets a pocket formed between subdomain 4 of Arp2 and subdomain 1 of Arp3, preventing Arp2/3 from shifting into an active conformation upon N-WASP-VCA binding. CK-666 and CK-869 (Cat. No. 182516) exhibit different modes of binding, resulting in their different yeast cross-reactivities. CK-689 (Cat. No. 182517) can serve as a negative control. | | Biochem/physiol Actions | CK-666 binds to Arp2/3 complex, stabilizes the inactive state of the complex and prevents its movement into active conformation. | | References | 1) Nolan et al. (2009), Characterization of two classes of small molecule inhibitors of Arp2/3 complex; Nature, 460 1031
2) Henson et al. (2015), Arp2/3 complex inhibition radically alters lamellipodial actin architecture, suspended cell shape, and the cell spreading process; Mol. Biol. Cell, 26 887
3) Park et al. (2013), Methamphetamine-induced occluding endocytosis is mediated by the Arp2/3 complex-regulated actin rearrangement; J. Biol. Chem., 288 33324
4) Sun et al. (2013), Actin nucleator Arp2/3 complex is essential for mouse preimplantation embryo development; Reprod. Fertil. Dev., 25 617
5) Efremov et al. (2015), Distinct impact of targeted actin cytoskeleton reorganization on mechanical properties of normal and malignant cells; Biochim. Biophys. Acta, 1853 (11PtB) 3117 |
| 2-Fluoro-N-[2-(2-methyl-1H-indol-3-yl)ethyl]benzamide Preparation Products And Raw materials |
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![2-Fluoro-N-[2-(2-methyl-1H-indol-3-yl)ethyl]benzamide](/img/442633-00-3.jpg "2-Fluoro-N-[2-(2-methyl-1H-indol-3-yl)ethyl]benzamide")
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