CK-636

Names

[ Name ]:
CK-636

[Synonym ]:
N-[2-(2-Methyl-1H-indol-3-yl)ethyl]-2-thiophenecarboxamide
2-Thiophenecarboxamide, N-[2-(2-methyl-1H-indol-3-yl)ethyl]-

Biological Activity

[Description]:

CK-636 is a cell permeable inhibitor of Arp2/3 complex, that could inhibit actin polymerization, with IC50 values of 4 μM, 24 μM and 32 μM for human, fission yeast and bovine, respectively.

[Related Catalog]:

Signaling Pathways >> Cytoskeleton >> Arp2/3 Complex

Research Areas >> Cancer

Research Areas >> Inflammation/Immunology

[Target]

IC50: 4/24/32 uM (Human/fission yeast/bovine Arp2/3)[1].

[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)[1]. 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[2].

[References]

[1]. Nolen BJ, et al. Characterization of two classes of small molecule inhibitors of Arp2/3 complex. Nature. 2009 Aug 20;460(7258):1031-4.

[2]. Kwon KW, et al. Migration of T cells on surfaces containing complex nanotopography. PLoS One. 2013 Sep 12;8(9):e73960.

[Related Small Molecules]

Cytochalasin B | CK869

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
576.8±45.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₆H₁₆N₂OS

[ Molecular Weight ]:
284.376

[ Flash Point ]:
302.6±28.7 °C

[ Exact Mass ]:
284.098328

[ PSA ]:
73.13000

[ LogP ]:
3.10

[ Appearance of Characters ]:
peach to light tan

[ Vapour Pressure ]:
0.0±1.6 mmHg at 25°C

[ Index of Refraction ]:
1.674

[ Storage condition ]:
2-8°C

[ Water Solubility ]:
DMSO: ≥20mg/mL

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302

[ Hazard Codes ]:
Xn

[ Risk Phrases ]:
22

[ RIDADR ]:
NONH for all modes of transport

Articles

Discovery of the migrasome, an organelle mediating release of cytoplasmic contents during cell migration.

Cell Res. 25(1) , 24-38, (2015)

Cells communicate with each other through secreting and releasing proteins and vesicles. Many cells can migrate. In this study, we report the discovery of migracytosis, a cell migration-dependent mech...