ZCL278
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
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: