货号	规格	价格	上海	北京	珠海	重庆	武汉
S82712-5mg买3赠1	99.48%	￥280.00 S82712-5mg ￥280.00 现货（买3赠1）	202 >10	-	-	-	-
S82712-10mg买3赠1	≥98%	￥450.00 S82712-10mg ￥450.00 现货（买3赠1）	97 >10	-	-	-	-
S82712-25mg买3赠1	≥98%	￥952.00 S82712-25mg ￥952.00 现货（买3赠1）	39 >10	-	-	-	-
S82712-100mg	≥98%	￥1760.00 S82712-100mg ￥1760.00 现货	9 9	-	-	-	-

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产品描述：

Rhosin (G04) hydrochloride (HCl) 是RhoA亚家族 Rho GTPases 的强效特异性抑制剂，Kd值约为0.4 uM。Rhosin hydrochloride 可诱导细胞凋亡

靶点：

Rho(Cell-free assay):0.4 μM(Kd);Apoptosis; Rho; Ras

体外研究：

In cells Rhosin specifically inhibits RhoA activity and RhoA-mediated cellular function without affecting Cdc42 or Rac1 signaling activities. By suppressing RhoA or RhoC activity Rhosin can inhibit mammary sphere formation by breast cancer cells, suppress invasion of mammary epithelial cells, and induce neurite outgrowth of PC12 cells in synergy with NGF

体内研究：

Treatment with rhosin abrogates the lung metastasis of B16BL6 and 4T1 cells in vivo.

细胞实验：

Cell lines: NIH3T3 cells, MCF7 cells, HME cells Concentrations: 10 μM, 30 μM, 50 μM Incubation Time: 24 h Method: NIH3T3 cells, MCF7 cells, or HME cells are grown in log phase in a 10-cm dish or a sixwell dish, and are starved in serum-free medium in the presence or absence of G04 at indicated concentrations for 24 hours and are subsequently stimulated with 10% calf serum or fetal bovine serum for 15 min. Cells are lysed in a buffer containing 20 mM Tris-HCL, pH 7.6, 100 mM NaCl, 1% Triton X-100, 10 mM MgCl2, 2 mM NaF and protease inhibitors (2 mM PMSF, 10 μg/ml leupeptin, 10 μg/ml aprotinin). Lysates are clarified, the protein concentrations are normalized, and the GTP-bound RhoA, Rac1 or Cdc42 in the lysates are measured by respective anti-RhoA, Rac1 and Cdc42 Western blotting of the effector domain pull-downs.

动物实验：

Animal Models: 8-week-old female Balb/c mice, 8-week-old female C57BL/6J mice Dosages: 10 mg/kg, 30 mg/kg Administration: --

参考文献：

1. Xun Shang, et al. Rational design of small molecule inhibitors targeting RhoA subfamily Rho GTPases. Chem Biol. 2012 Jun 22;19(6):699-710. 2. Masanobu Tsubaki, et al. Rhosin Suppressed Tumor Cell Metastasis through Inhibition of Rho/YAP Pathway and Expression of RHAMM and CXCR4 in Melanoma and Breast Cancer Cells. Biomedicines. 2021 Jan 4;9(1):35.

溶解性：

Soluble in DMSO、H2O

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.533 ml	12.663 ml	25.326 ml
5 mM	0.507 ml	2.533 ml	5.065 ml
10 mM	0.253 ml	1.266 ml	2.533 ml
50 mM	0.051 ml	0.253 ml	0.507 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献(1篇)

1. [IF=7.2] Yuan Qingling et al."Pleckstrin homology and RhoGEF domain containing G4 (PLEKHG4) leads to the activation of RhoGTPases promoting the malignant phenotypes of thyroid cancer."APOPTOSIS.2023 Jun;:1-17

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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

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Rhosin (hydrochloride)