CK-636 is a Arp2/3 complex inhibitor. CK-636 binds between Arp2 and Arp3, where it appears to block movement of Arp2 and Arp3 into their active conformation. CK-636 inserts into the hydrophobic core of Arp3 and alters its conformation. Polymerization of actin filaments directed by the actin-related protein (Arp)2/3 complex supports many types of cellular movements. CK-636 may be a powerful tool compound for studying the Arp2/3 complex in living cells.
CAS Number: 442632-72-6
Molecular Weight: 284.38
Chemical Name: N-[2-(2-Methyl-1H-indol-3-yl)ethyl]-2-thiophenecarboxamide
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO, not in water
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
CK-636 binds between Arp2 and Arp3, where it appears to block movement of Arp2 and Arp3 into their active conformation. CK-636 inserts into the hydrophobic core of Arp3 and alters its conformation. CK-636 prevents actin polymerization and the formation of actin filament comet tails by Listeria in infected SKOV3 cells (IC50=22 µM). Additionally, CK-636-treated T cells exhibits elongated morphology with sharp pseudopodia at the leading edges, while the breadth of the CK-636-treated T cells is about 30% less than that of DMSO-treated T cells.
- Kwon KW, Park H, Doh J. Migration of T cells on surfaces containing complex nanotopography. PLoS One. 2013 Sep 12;8(9):e73960. doi: 10.1371/journal.pone.0073960. eCollection 2013. PubMed PMID: 24069255; PubMed Central PMCID: PMC3771970.
- Zhou K, Muroyama A, Underwood J, Leylek R, Ray S, Soderling SH, Lechler T. Actin-related protein2/3 complex regulates tight junctions and terminal differentiation to promote epidermal barrier formation. Proc Natl Acad Sci U S A. 2013 Oct 1;110(40):E3820-9. doi: 10.1073/pnas.1308419110. Epub 2013 Sep 16. PubMed PMID: 24043783; PubMed Central PMCID: PMC3791730.
- Nolen BJ, Tomasevic N, Russell A, Pierce DW, Jia Z, McCormick CD, Hartman J, Sakowicz R, Pollard TD. Characterization of two classes of small molecule inhibitors of Arp2/3 complex. Nature. 2009 Aug 20;460(7258):1031-4. doi: 10.1038/nature08231. Epub 2009 Aug 2. PubMed PMID: 19648907; PubMed Central PMCID: PMC2780427.
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