555460-M
Rhosin
≥93% (HPLC), powder, Rho inhibitor, Calbiochem®
别名:
Rho抑制剂，Rhosin, G04，(2R)-2-氨基-3-(1H-吲哚-3-基)-Nʹ-((1E)-喹喔啉-6-基亚甲基)丙烷酰肼
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关于此项目
经验公式（希尔记法）:
C20H18N6O
化学文摘社编号:
分子量:
358.40
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.28
产品名称
Rho抑制剂，Rhosin, Rho Inhibitor, Rhosin, CAS 1173671-63-0, is a cell-permeable compound that directly targets Rho GEF binding domain (Kd = 354 nM for RhoA), thereby prevents Rho from interacting with its GEFs.
assay
≥93% (HPLC)
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
orange-brown
solubility
DMSO: 10 mg/mL
Quality Level
General description
Rhosin由两个通过连接体连接的芳香环组成，并以亚微摩尔范围的Kd与RhoA的Trp58周围区域结合，有效抑制GEF催化的RhoA激活。该化合物对于研究RhoA亚家族GTP酶的生理作用和评估靶向Rho在病理状况下的治疗潜力具有价值。
此外，Rhosin可以通过靶向RhoA和RhoC来抑制YAP激活。它还可以通过抑制Rho/YAP通路和调节黑色素瘤和乳腺癌细胞中RHAMM和CXCR4的表达来抑制肿瘤细胞转移。它通过增强D1-MSN可塑性和减少过度兴奋性来促进应激恢复力。
此外，Rhosin可以通过靶向RhoA和RhoC来抑制YAP激活。它还可以通过抑制Rho/YAP通路和调节黑色素瘤和乳腺癌细胞中RHAMM和CXCR4的表达来抑制肿瘤细胞转移。它通过增强D1-MSN可塑性和减少过度兴奋性来促进应激恢复力。
Application
Rho抑制剂Rhosin已被用于处理单个乳腺肿瘤细胞以调节RhoA活性，并用Förster共振能量转移（FRET）生物传感器验证细胞系。
Biochem/physiol Actions
主靶
Rho GT酶
Rho GT酶
靶标Ki：RhoA为354 nM
Preparation Note
复溶后，等分并冷冻保存（-20°C）。贮备溶液在-20°C下可稳定保存至多6个月。
Other Notes
Shang, X., et al. 2012.Chem. Biol.19, 699.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
毒性：标准处理（A）
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Rhosin suppressed tumor cell metastasis through inhibition of Rho/YAP pathway and expression of RHAMM and CXCR4 in melanoma and breast cancer cells
Tsubaki M, et al.
Biomedicines, 9(1), 35-35 (2021)
Spatial and temporal dynamics of RhoA activities of single breast tumor cells in a 3D environment revealed by a machine learning-assisted FRET technique
Cheung BCH, et al.
Experimental Cell Research, 410(2), 112939-112939 (2022)
The selective RhoA inhibitor rhosin promotes stress resiliency through enhancing D1-medium spiny neuron plasticity and reducing hyperexcitability
Francis TC, et al.
Biological Psychiatry (2019)
Rational design of small molecule inhibitors targeting RhoA subfamily Rho GTPases
Shang X, et al.
Chemistry and Biology, 19(6), 699-710 (2012)
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