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.
Chemical Formula: C16H16N2OS
Exact Mass: 284.09833
Molecular Weight: 284.38
Elemental Analysis: C, 67.58; H, 5.67; N, 9.85; O, 5.63; S, 11.28
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)
Appearance: White to beige solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life:>2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
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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