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NSC 23766 trihydrochloride

产品编号 T6342 CAS 1177865-17-6

别名: Rac1 Inhibitor, NSC 23766

NSC 23766 trihydrochloride (Rac1 Inhibitor) 是一种 Rac GTPase 抑制剂，靶向 GEF 对 Rac 的激活，IC50值约为 50 μM。

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NSC 23766 trihydrochloride Chemical Structure

NSC 23766 trihydrochloride, CAS 1177865-17-6

规格	价格/CNY	货期
1 mg	￥ 175	现货
5 mg	￥ 371	现货
10 mg	￥ 675	现货
25 mg	￥ 1,390	现货
50 mg	￥ 2,730	现货
100 mg	￥ 3,920	现货
1 mL * 10 mM (in DMSO)	￥ 438	现货

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其他形式的 NSC 23766 trihydrochloride:

NSC 23766
询价

选择批次

纯度: 99.54%

纯度: 99.35%

纯度: 96.48%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	NSC 23766 trihydrochloride (Rac1 Inhibitor) is an inhibitor of Rac GTPase targeting Rac activation by GEFs (IC50: ~50 μM); no inhibitory for the closely related targets, RhoA or Cdc42.
靶点活性	Rac GTPase:50 μM
体外活性	NSC23766 is identified to fit into a surface groove of Rac1 known to be critical for GEF specification. NSC23766 effectively inhibits Rac1 binding and activation by the Rac-specific GEF Trio or Tiam1 in a dose-dependent manner without interfering with the closely related Cdc42 or RhoA binding or activation by their respective GEFs or with Rac1 interaction with BcrGAP or effector PAK1. [1] NSC 23766 is active in regulating Rac GTPase functions on cytoskeleton and many cell functions including cell cycle, cell growth, adhesion, migration and gene transcription. NSC 23766 (50 μM) potently blocks serum or platelet-derived growth factor-induced Rac1 activation and lamellipodia formation without affecting the activity of endogenous Cdc42 or RhoA in NIH 3T3 cells. NSC 23766 reduces Trio or Tiam1 but not Vav, Lbc, Intersectin, or a constitutively active Rac1 mutant-stimulated NIH 3T3 cells growth and suppresses Trio, Tiam1, or Ras-induced cell transformation. NSC23766 dose-dependently inhibits PC-3 cells proliferation and anchorage-independent growth. 25 μM NSC23766 inhibits the PC-3 cell invasion through Matrigel by 85%. [1] 50 μM NSC 23766 inhibits thrombin-induced activation of Rac1 an d Rac2 in human platelets, as well as platelet aggregation. [2] NSC23766 prevents Aβ40 and Aβ42 production in swAPP-HEK293cells without affecting Notch and sAPPα. NSC23766 prevents γ-secretase activity in cell, but not act as a direct γ-secretase inhibitor. NSC23766 dose-dependently reduces levels of secreted and intracellular Aβ40 with IC50 of 48.94 μM. 50 μM NSC 23766 inhibits release of Aβ42 by 57.97%. [3]
体内活性	NSC23766 induces mobilization of hematopoietic stem cells/progenitors. Intraperitoneal administration of NSC23766 (2.5 mg/kg) into the ''poorly mobilizing '' C57Bl/6 mouse strain leads to a two-fold increase in circulating hematopoietic stem cells/progenitors 6 hr after injection. [2] NSC23766 alleviates lipopolysaccharide-induced acute pulmonary injury in mice. Treatment with NSC23766 at 1 or 3 mg/kg not only reduces the inflammatory cells infiltration and MPO activities, but also inhibits pro-inflammatory mediators, tumor necrosis factor-α and interleukin-1β, mRNA expression. NSC23766 also reduces Evans Blue and albumin accumulation in LPS-challenged lungs. [6]
激酶实验	Rho GTPase activity assay: Cells are grown in log phase in a 10-cm dish, and are starved in 0.5% serum medium or indicated otherwise for 24 h before lysis in a buffer containing 20 mM Tris HCl (pH 7.6), 100 mM NaCl, 10 mM MgCl2, 1% Nonidet P-40, 10% glycerol, and 1× protease inhibitor mixture. Lysates are clarified, the protein concentrations are normalized, and the GTP-bound Rac1 in the lysates is measured by an effector domain pull-down assay. For the His6-PAK1 PBD pull-down assay, cell lysates are incubated with Ni2+-agarose-immobilized His6-PAK1 PBD domain (～1 μg each) purified from E. coli for 30 min. The Ni2+-agarose co-precipitates are washed twice in the wash buffer and analyzed by immunoblotting with anti-Rac1 monoclonal antibody.
细胞实验	Cells (1.5 × 104/mL) are seeded in each well of 96-well tissue culture plates with 200 μL of medium. After 24 hours of plating, the medium is replaced with 200 μL of fresh medium containing NSC23766 at the indicated concentrations. At the end of the treatment period 20 μL of MTS solution are added to each well and incubated at 37 ℃ for 2 hours. Absorbance at 490 nm is read on a 96-well plate reader.(Only for Reference)

别名	Rac1 Inhibitor, NSC 23766
分子量	530.96
分子式	C24H35N7·3HCl
CAS No.	1177865-17-6

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: 53.1 mg/mL (100 mM)

DMSO: 53.1 mg/mL (100 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
H2O / DMSO	1 mM	1.8834 mL	9.4169 mL	18.8338 mL	47.0845 mL
	5 mM	0.3767 mL	1.8834 mL	3.7668 mL	9.4169 mL
	10 mM	0.1883 mL	0.9417 mL	1.8834 mL	4.7085 mL
	20 mM	0.0942 mL	0.4708 mL	0.9417 mL	2.3542 mL
	50 mM	0.0377 mL	0.1883 mL	0.3767 mL	0.9417 mL
	100 mM	0.0188 mL	0.0942 mL	0.1883 mL	0.4708 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Gao Y, et al. Proc Natl Acad Sci U S A, 2004, 101(20), 7618-7623. 2. Akbar H, et al. Methods Enzymol, 2006, 406, 554-565. 3. Désiré L, et al. J Biol Chem, 2005, 280(45), 37516-3 4. Sawada N, et al. Circ Res, 2008, 103(4), 360-368. 5. Yoshida T, et al. Mol Cancer Ther, 2010, 9(6), 1657-1668. 6. Veluthakal R, et al. NSC23766, a Known Inhibitor of Tiam1-Rac1 Signaling Module, Prevents the Onset of Type 1 Diabetes in the NOD Mouse Model. Cell Physiol Biochem. 2016;39(2):760-7. 7. Song SJ, et al. Inhibition of Rac1 GTPase activity affects porcine oocyte maturation and early embryo development. Sci Rep. 2016 Oct 3;6:34415 8. Zhao L, et al. Rac1 modulates the formation of primordial follicles by facilitating STAT3-directed Jagged1, GDF9 and BMP15 transcription in mice. Sci Rep. 2016 Apr 6;6:23972 9. Wang Y, et al. Involvement of Rac1 signalling pathway in the development and maintenance of acute inflammatory pain induced by bee venom injection. Br J Pharmacol. 2016 Mar;173(5):937-50 10. Chen Z, Zhang S, Nie B, et al. Distinct roles of srGAP3‐Rac1 in the initiation and maintenance phases of neuropathic pain induced by paclitaxel[J]. The Journal of Physiology. 2020, 598(12): 2415-2430.

文献引用

1. Ma X, Tan X, Yu B, et al. DOCK2 regulates antifungal immunity by regulating RAC GTPase activity. Cellular & Molecular Immunology. 2022: 1-17. 2. Ma X, Tan X, Yu B, et al. DOCK2 regulates antifungal immunity by regulating RAC GTPase activity. Cellular & Molecular Immunology. 2022: 1-17. 3. Chen Z, Zhang S, Nie B, et al. Distinct roles of srGAP3‐Rac1 in the initiation and maintenance phases of neuropathic pain induced by paclitaxel. The Journal of Physiology. 2020, 598(12): 2415-2430. 4. Zhou T, Wang C H, Yan H, et al. Inhibition of the Rac1-WAVE2-Arp2/3 signaling pathway promotes radiosensitivity via downregulation of cofilin-1 in U251 human glioma cells. Molecular medicine reports. 2016 May;13(5):4414-20. 5. Chen M, Li H, Xu X, et al.Identification of RAC1 in promoting brain metastasis of lung adenocarcinoma using single-cell transcriptome sequencing.Cell Death & Disease.2023, 14(5): 330.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

NSC 23766 trihydrochloride 1177865-17-6 Apoptosis Cell Cycle/Checkpoint GPCR/G Protein MAPK Rho Ras Inhibitor NSC-23766 NSC-23766 Trihydrochloride Rac1 Inhibitor inhibit NSC23766 NSC 23766 Trihydrochloride NSC 23766 NSC23766 Trihydrochloride inhibitor

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NSC 23766 trihydrochloride

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords