ZCL278
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mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
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Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
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Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
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Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
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SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
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Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
ZCL278是一种选择性的Cdc42抑制剂,Kd值为11.4 μM[1]。
细胞分裂调控蛋白42同源物(Cdc42)是一种小GTP酶,属于Rho家族,在调节多种细胞功能中起重要作用,包括细胞形态、细胞内吞作用、细胞迁移和细胞周期进程[2]。
ZCL278是一种有效的Cdc42抑制剂,与已报道的Cdc42抑制剂ML141具有不同的选择性。在人转移性前列腺癌PC-3细胞中,ZCL278对Rac/Cdc42的磷酸化和功能增加具有抑制作用。在皮层神经元,ZCL278以50 μM的剂量处理5或10分钟后抑制神经分枝数和生长锥运动。在Cdc42激活剂处理过的血清饥饿Swiss 3T3成纤维细胞中,ZCL278以50 μM的剂量处理1小时后显著减少GTP-Cdc42(接近80%),并扰乱活性Cdc42的核周分布[1]。在大鼠小脑颗粒神经元(CGNs)中,暴露于NaAsO2之前用ZCL278(20、50和100μM)预处理可剂量依赖性地增加细胞活力[3]。
参考文献:
[1]. Friesland, A., et al., Small molecule targeting Cdc42-intersectin interaction disrupts Golgi organization and suppresses cell motility. Proc Natl Acad Sci U S A, 2013. 110(4): p. 1261-6.
[2]. Selamat, W., et al., The Cdc42 Effector Kinase PAK4 Localizes to Cell-Cell Junctions and Contributes to Establishing Cell Polarity. PLoS One, 2015. 10(6): p. e0129634.
[3]. Liu, X., et al., Neuroglobin Plays a Protective Role in Arsenite-Induced Cytotoxicity by Inhibition of Cdc42 and Rac1GTPases in Rat Cerebellar Granule Neurons. Cell Physiol Biochem, 2015. 36(4): p. 1613-1627.
- 1. Fray MA, Charpentier JC, et al. "Vav2 lacks calcium entry-promoting scaffolding functions unique to Vav1 and inhibits T cell activation via Cdc42." J Cell Sci. 2020;jcs.238337. PMID:31974114
- 2. Yang Yang, Kaiyuan Zhang, et al. "SVCT2 Promotes Neural Stem/Progenitor Cells Migration Through Activating CDC42 After Ischemic Stroke." Front. Cell. Neurosci. 19 September 2019.
- 3. Ye Y, Li SL, et al. "Exosomal miR-141-3p regulates osteoblast activity to promote the osteoblastic metastasis of prostate cancer." Oncotarget. 2017 Oct 24;8(55):94834-94849. PMID:29212270
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 584.89 |
Cas No. | 587841-73-4 |
Formula | C21H19BrClN5O4S2 |
Solubility | ≥29.25 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
Chemical Name | 2-(4-bromo-2-chlorophenoxy)-N-[[4-[(4,6-dimethylpyrimidin-2-yl)sulfamoyl]phenyl]carbamothioyl]acetamide |
SDF | Download SDF |
Canonical SMILES | CC1=CC(=NC(=N1)NS(=O)(=O)C2=CC=C(C=C2)NC(=S)NC(=O)COC3=C(C=C(C=C3)Br)Cl)C |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
激酶实验 [1]: | |
p50RhoGAP/Cdc42GAP试验 |
采用p50RhoGAP/Cdc42GAP试验和吸光度检测法,测定无机磷酸盐产量,以评估GTP酶活性。将Cdc42与GTP或ZCL278预先混合,再将其加入反应缓冲液中,于37 °C孵育20分钟。再加入GAP,反应于37 °C继续孵育20分钟。加入CytoPhos试剂,将反应孵育10分钟,在650nm测定无机磷酸盐产量。 |
细胞实验 [1]: | |
细胞系 |
皮层神经元 |
制备方法 |
在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。 |
反应条件 |
50 μM;5和10分钟或2、4、6、8和10分钟 |
实验结果 |
在经ZCL278治疗的神经元中,神经元分支随时间推移而显着受抑。此外,ZCL278显着抑制Cdc42介导的生长锥运动。 |
References: [1]. Friesland, A., et al., Small molecule targeting Cdc42-intersectin interaction disrupts Golgi organization and suppresses cell motility. Proc Natl Acad Sci U S A, 2013. 110(4): p. 1261-6. |
描述 | ZCL278是一种选择性的Cdc42 GTPase抑制剂,Kd值为11.4 μM。 | |||||
靶点 | Cdc42 GTPase | |||||
IC50 | 11.4 μM(Kd) |
质量控制和MSDS
- 批次:
化学结构
![ZCL278](http://www.apexbt.com//media/diy/images/struct/A8300.png)
相关生物数据
![ZCL278 ZCL278](http://www.apexbio.cn/media/diy/images/wb/A8300_1.jpg)
相关生物数据
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