Arp2/3 complex
An important set of actin regulators initiate formation of new actin filaments by a process that is called nucleation. Spontaneous nucleation is a kinetic hurdle in the process of actin polymerization, and, therefore, factors that can accelerate or bypass this step are important for efficient actin assembly in the cell. So far, three classes of protein have been identified that initiate new filament polymerization: the actin-related protein-2/3 (ARP2/3) complex, the formins and spire. The intact ARP2/3 complex was shown to consist of a stable assembly of seven polypeptides. Two of the subunits were actin-related proteins of the ARP2 and ARP3 subfamilies, giving the complex its name. The ARP2/3 complex possesses little biochemical activity on its own.The capability of nucleation-promoting factors (NPFs) to activate the actin-related protein-2/3 (ARP2/3) complex is regulated by signal-transduction pathways that involve Rho-family GTPases and lipid second messengers.
The mechanism of regulation has been well characterized for two class I NPFs, Wiskott–Aldrich syndrome protein (WASP and neural (N)-WASP) and SCAR (suppressor of cyclic AMP repressor; also known as WAVE (WASP-family verprolin-homologous protein)), and differs between the two protein families. Coordinated nucleation and branching by the ARP2/3 complex has an important role in several cellular processes including cell migration and adhesion, moving membranes and their cargoes.The ARP2/3 complex and its activators are therefore likely to be crucial participants in the process of tumour-cell invasion and metastasis, and might represent targets for therapeutic intervention.
References
1.Goley ED,et al. Nat Rev Mol Cell Biol. 2006 Oct;7(10):713-26.
The mechanism of regulation has been well characterized for two class I NPFs, Wiskott–Aldrich syndrome protein (WASP and neural (N)-WASP) and SCAR (suppressor of cyclic AMP repressor; also known as WAVE (WASP-family verprolin-homologous protein)), and differs between the two protein families. Coordinated nucleation and branching by the ARP2/3 complex has an important role in several cellular processes including cell migration and adhesion, moving membranes and their cargoes.The ARP2/3 complex and its activators are therefore likely to be crucial participants in the process of tumour-cell invasion and metastasis, and might represent targets for therapeutic intervention.
References
1.Goley ED,et al. Nat Rev Mol Cell Biol. 2006 Oct;7(10):713-26.
Cytoskeleton/Cell Adhesion Molecules
Arp2/3 complex
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Cytochalasin B
产品货号 : M36360
cas no: 14930-96-2
Cytochalasin B 是一种能透过细胞的真菌毒素,能够与肌动蛋白丝的有刺端结合,扰乱肌动蛋白聚合物的形成,对 F-actin 的 Kd 值为 1.4-2.2 nM。Cytochalasin B 抑制细胞迁移。 -
187-1, N-WASP inhibitor
产品货号 : M30611
cas no: 380488-27-7
Inhibits neural Wiskott-Aldrich syndrome protein (N-WASP) by stabilizing the autoinhibited state of the protein. Blocks phosphatidylinositol 4,5-bisphosphate (PIP2)-stimulated actin assembly (IC50 ~ 2 μM) but does not directly inhibit actin polymerization. -
CK 666
产品货号 : M14508
cas no: 442633-00-3
CK 666 (CK 0944666) 是一种小分子 Arp2/3 复合物抑制剂,IC50 为 4 uM。 -
CK-636
产品货号 : M14507
cas no: 442632-72-6
一种小分子 Arp2/3 复合物抑制剂,可抑制裂殖酵母 Arp2/3 复合物刺激的肌动蛋白聚合。 -
CK 869
产品货号 : M14339
cas no: 388592-44-7
CK 869 是人和牛肌动蛋白相关蛋白 2/3 (Arp2/3) 复合物的抑制剂,抑制肌动蛋白聚合 (IC50=11 uM)。