CK-636

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.

Product information

CAS Number: 442632-72-6

Molecular Weight: 284.38

Formula: C16H16N2OS

Synonym:

CK-0944636

CK636

CK 636

CK-636

CK0944636

CK 0944636

Chemical Name: N-[2-(2-Methyl-1H-indol-3-yl)ethyl]-2-thiophenecarboxamide

Smiles: CC1NC2=CC=CC=C2C=1CCNC(=O)C1=CC=CS1

InChiKey: ACAKNPKRLPMONU-UHFFFAOYSA-N

InChi: 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)

Technical Data

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: ≥12 months 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

In Vitro:

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.

References:

1. 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.
2. 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.
3. 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.

Products are for research use only. Not for human use.