Rho
The Rho family of GTPases is a family of small (~21 kDa) signaling G proteins, and is a subfamily of the Ras superfamily. The members of the Rho GTPase family have been shown to regulate many aspects of intracellular actin dynamics, and are found in all eukaryotic kingdoms, including yeasts and some plants. Three members of the family have been studied in detail: Cdc42, Rac1, and RhoA. All G proteins are "molecular switches", and Rho proteins play a role in organelle development, cytoskeletal dynamics, cell movement, and other common cellular functions.
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EHop-016是Rac GTPase高效选择性抑制剂,在MDA-MB-435细胞中IC50值1.1uM。
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NSC 23766是一种RacGTPase抑制剂,通过鸟嘌呤核苷酸交换因子(GEFs),靶向激活Rac,IC50为50 μM。但不抑制与其相关的靶点Cdc42和RhoA。
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ZCL278是Cdc42调节剂,能直接与Cdc42结合,Kd为11.4 uM,能抑制Cdc42与intersectin的相互作用。
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ML141(CID-2950007)是Cdc42高效选择性抑制剂,IC50值为200nM,对其他Rho GTPase家族成员作用力弱。
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CCG-1423是一种新型的RhoA/C介导的基因转录抑制剂,能抑制细胞的转移前列腺癌PC-3细胞侵袭模型。
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