CK-869 has been used as an Arp2/3 complex inhibitor:
to treat cultured mammalian cells and study its in vitro and in vivo effects on microtubule assembly[1]
to induce membrane blebbing in HT1080 fibrosarcoma cells[2]
to treat KDM3A-null cells and study the relation between actin dynamics and ciliogenesis[3]
Biochem/physiol Actions
CK-0157869 (CK-869) prevents microtubule (MT) assembly, free of Arp2/3 complex.[1]
CK-869 is a cell-permeable inhibitor of actin assembly mediated by the actin-related protein Arp2/3 complex of human and bovine, but not yeast. The actin-related protein Arp2/3 complex plays a major role in the regulation of the actin cytoskeleton. Apparently the compound binds to the hydrophobic core of Arp3 and alters its conformation.
Biochemical and biophysical research communications, 496(3), 834-839 (2018-02-06)
Two types of Arp2/3 complex inhibitors, CK-666/636 and CK-548/869, are commonly used to study Arp2/3 complex-dependent actin assembly both in vitro and in vivo. However, we found that CK-548 and CK-869 directly suppress microtubule (MT) assembly independent of the actin cytoskeleton. Treatment
Polymerization of actin filaments directed by the actin-related protein (Arp)2/3 complex supports many types of cellular movements. However, questions remain regarding the relative contributions of Arp2/3 complex versus other mechanisms of actin filament nucleation to processes such as path finding
The Journal of cell biology, 218(2), 445-454 (2018-12-14)
Membrane blebbing accompanies various cellular processes, including cytokinesis, apoptosis, and cell migration, especially invasive migration of cancer cells. Blebs are extruded by intracellular pressure and are initially cytoskeleton-free, but they subsequently assemble the cytoskeleton, which can drive bleb retraction. Despite
The Journal of cell biology, 216(4), 999-1013 (2017-03-02)
Cilia assembly and disassembly are coupled to actin dynamics, ensuring a coherent cellular response during environmental change. How these processes are integrated remains undefined. The histone lysine demethylase KDM3A plays important roles in organismal homeostasis. Loss-of-function mouse models of
Contractile actomyosin networks are responsible for the production of intracellular forces. There is increasing evidence that bundles of actin filaments form interconnected and interconvertible structures with the rest of the network. In this study, we explored the mechanical impact of
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