1. GPCR/G Protein MAPK/ERK Pathway Apoptosis
  2. Ras Apoptosis
  3. Rhosin

Rhosin 是一种有效的,特异性的 RhoA 亚家族 Rho GTPases 抑制剂,能特异性的结合 RhoA,抑制 RhoA-GEF 相互作用,Kd 值 ~ 0.4 uM,但不与 Cdc42 或 Rac1,GEF,LARG 相互作用。Rhosin 可诱导细胞凋亡 (apoptosis)。Rhosin 通过增强 D1 中棘神经元的可塑性和降低过度兴奋性来促进应激恢复。

在相同的摩尔浓度下,化合物盐形式与游离形式有相同的生物活性,但盐形式 Rhosin hydrochloride 通常具有更好的水溶性和稳定性。

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Rhosin Chemical Structure

Rhosin Chemical Structure

CAS No. : 1173671-63-0

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Other Forms of Rhosin:

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Rhosin is a potent, specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin induces cell apoptosis[1][2]. Rhosin promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability[3].

IC50 & Target

Kd: 0.4 uM (RhoA)[1]

体外研究
(In Vitro)

Rhosin dose-dependently reduces RhoA and p-MLC1 activities of MCF7 cell-derived mammospheres with an EC50 ~30-50 μM, and causes decreased size and reduced number of mammospheres in MCF7 cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Rhosin (40 mg/kg; i.p.) treatment prevents social avoidance caused by social defeat stress. Rhosin also blocks sucrose preference deficits induced by defeat in C57Bl6/J (Jackson) mice[1].
Rhosin (30 µM; bilateral, intra- Nucleus Accumbens (NAc) infusions) attenuates stress-induced social avoidance. Rhosin blocks stress-induced hyperexcitability in NAc dopamine 1 receptor medium spiny neurons (D1-MSNs). Rhosin prevents decreased excitatory transmission on NAc D1-MSNs. Rhosin enhances spine density in defeat mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: D1-GFP or D2-GFP hemizygote mice on a C57BL/6J background[3]
Dosage: 40 mg/kg
Administration: i.p.
Result: Rhosin was systemically administered 15 min prior to defeat to block RhoA activation. While defeat significantly reduced the time that experimental mice spent interacting with a novel mouse, Rhosin administration suppressed this effect without affecting locomotor behaviors.
分子量

358.40

Formula

C20H18N6O

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Rhosin
目录号:
HY-12646A
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