A specific inhibitor of Cdc42
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MLS-573151 is a specific and cell permeable inhibitor of Cdc42 [1].
Cdc42 is a small GTPase of the Rho family involved in regulating signaling pathways that control diverse cellular functions such as cell morphology, cell migration, cell cycle progression and endocytosis [2].
In vitro: MLS-573151 was a specific, cell permeable inhibitor of Cdc42 with an IC50 of 2 μM [1]. MLS-573151 showed no effect on other GTPases, including the related Rho family members RhoA, Rac1, and Rac2. MLS-573151 functioned by blocking the binding of GTP to Cdc42 [1]. In marrow-derived mesenchymal stem cells, MLS-573151 showed no effect on cell migration [3].
参考文献:
[1] Surviladze Z, Waller A, Wu Y, et al.? Identification of a small GTPase inhibitor using a high-throughput flow cytometry bead-based multiplex assay[J]. Journal of biomolecular screening, 2010, 15(1): 10-20.
[2] Qadir M I, Parveen A, Ali M.? Cdc42: Role in Cancer Management[J]. Chemical biology & drug design, 2015, 86(4): 432-439.
[3] Wang L, Yang L, Tian L, et al.? Cannabinoid Receptor 1 Mediates Homing of Bone Marrow‐Derived Mesenchymal Stem Cells Triggered by Chronic Liver Injury[J]. Journal of cellular physiology, 2017, 232(1): 110-121.
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