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product name
肌动蛋白相关蛋白2/3(Arp2/3)复合物抑制剂I, CK-666, Arp2/3 Complex Inhibitor I, CK-666, CAS 442633-00-3, is a cell-permeable selective inhibitor of actin assembly mediated by actin-related protein Arp2/3 complex (IC50 = 4 uM in human).
品質等級
化驗
≥95% (HPLC)
形狀
solid
製造商／商標名
Calbiochem®
儲存條件
OK to freeze
protect from light
顏色
off-white
溶解度
DMSO: 50 mg/mL
運輸包裝
ambient
儲存溫度
2-8°C
InChI
1S/C18H17FN2O/c1-12-13(14-6-3-5-9-17(14)21-12)10-11-20-18(22)15-7-2-4-8-16(15)19/h2-9,21H,10-11H2,1H3,(H,20,22)
InChI 密鑰
UXRKUKRXVWJFER-UHFFFAOYSA-N
一般說明
一种可渗透细胞的吲哚基-氟苯甲酰胺化合物，可选择性抑制由人、牛、裂变酵母S. pombe和发芽酵母酿酒酵母起源的肌动蛋白相关蛋白Arp2/3复合物介导的肌动蛋白组装（IC50=4、17、5和12 µM），而不会影响粟酒裂殖酵母formin域Cdc12（FH2）介导的或自发的肌动蛋白聚合。显示以可逆的方式抑制感染的SKOV3细胞（IC50 = 7 µM）中细胞内李斯特菌周围肌动蛋白丝“彗星尾”的形成。结构研究表明，CK-666靶向Arp2的亚结构域4和Arp3的亚结构域1之间形成的口袋，从而防止Arp2/3在N-WASP-VCA结合后转变为活性构象。CK-666和CK-869（目录编号182516）表现出不同的结合方式，导致它们的酵母交叉反应性不同。CK-689（目录编号182517）可作为阴性对照。
一种可渗透细胞的吲哚基-氟苯甲酰胺化合物，可选择性抑制由人、牛、裂变酵母S. pombe和发芽酵母酿酒酵母起源的肌动蛋白相关蛋白Arp2/3复合物介导的肌动蛋白组装（IC50=4、17、5和12 µM），而不会影响粟酒裂殖酵母formin域Cdc12（FH2）介导的或自发的肌动蛋白聚合。显示以可逆的方式抑制感染的SKOV3细胞（IC50 = 7 µM）中细胞内李斯特菌周围肌动蛋白丝“彗星尾”的形成。结构研究表明，CK-666靶向Arp2的亚结构域4和Arp3的亚结构域1之间形成的口袋，从而防止Arp2/3在N-WASP-VCA结合后转变为活性构象。CK-666和CK-869（目录编号182516）表现出不同的结合方式，导致它们的酵母交叉反应性不同。CK-689（目录编号182517）可作为阴性对照。
包裝
用惰性气体包装
警告
毒性：监管审查（Z）
重構
复溶后，等分并冷冻保存（-20°C）。储备液在-20°C条件下可稳定保存6个月。
其他說明
Nolen, B.J., et al. 2009.Nature460, 1031.
法律資訊
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
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eLife, 12 (2023-09-25)
As cells migrate and experience forces from their surroundings, they constantly undergo mechanical deformations which reshape their plasma membrane (PM). To maintain homeostasis, cells need to detect and restore such changes, not only in terms of overall PM area and
Binh An Truong Quang et al.
Nature communications, 12(1), 6511-6511 (2021-11-13)
In animal cells, shape is mostly determined by the actomyosin cortex, a thin cytoskeletal network underlying the plasma membrane. Myosin motors generate tension in the cortex, and tension gradients result in cellular deformations. As such, many cell morphogenesis studies have
Kathleen Scheffler et al.
Journal of cell science, 135(6) (2022-02-04)
Formation of healthy mammalian eggs from oocytes requires specialised F-actin structures. F-actin disruption produces aneuploid eggs, which are a leading cause of human embryo deaths, genetic disorders and infertility. We found that oocytes contain prominent nuclear F-actin structures that are
Domokos I Lauko et al.
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The baculovirus Autographa californica multiple nucleopolyhedrovirus (AcMNPV), a pathogen of lepidopteran insects, has a striking dependence on the host cell actin cytoskeleton. During the delayed-early stage of infection, AcMNPV was shown to induce the accumulation of actin at the cortex of infected cells. However, the dynamics and
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The formation and recovery of gaps in the vascular endothelium governs a wide range of physiological and pathological phenomena, from angiogenesis to tumor cell extravasation. However, the interplay between the mechanical and signaling processes that drive dynamic behavior in vascular
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