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
Assay:
≥93% (HPLC)
Form:
powder
Quality level:
Storage condition:
OK to freeze, protect from light
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.
storage temp.
2-8°C
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
Rational design of small molecule inhibitors targeting RhoA subfamily Rho GTPases
Shang X, et al.
Chemistry and Biology, 19(6), 699-710 (2012)
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)
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)
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)
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