ZCL278
目录号 : GC12470
A selective Cdc42 inhibitor
Cas No.:587841-73-4
Sample solution is provided at 25 µL, 10mM.
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ZCL278 is a selective inhibitor of Cdc42 with Kd value of 11.4 μM [1].
Cell division control protein 42 homolog (Cdc42) is a small GTPase that belongs to the Rho family and plays an important role in regulating diverse cellular functions including cell morphology, endocytosis, migration, and cell cycle progression [2].
ZCL278 is a potent Cdc42 inhibitor and has a different selectivity with the reported Cdc42 inhibitor ML141. When tested with human metastatic prostate cancer PC-3 cells, ZCL278 showed inhibitory function on Rac/Cdc42 phosphorylation and the function increasing as the more-treated time. In cortical neurons, ZCL278 treatment suppressed neuronal branch number and inhibited growth cone motility at the dose of 50 μM for 5 or 10 min. Treated serum-starved Swiss 3T3 fibroblasts Cdc42 activator following administration of ZCL278 at the dose of 50 μM for 1 h exhibited a significant decrease (nearly 80%) in GTP-Cdc42 and disrupted perinuclear distribution of active Cdc42. [1]. When tested with rat cerebellar granule neurons (CGNs), pre-treated with ZCL278 before exposed to NaAsO2 increased cell viability in a dose-dependent manner (20, 50 and 100μM) [3].
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.
[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.
| Kinase experiment [1]: | |
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p50RhoGAP or Cdc42GAP Assay |
Inorganic phosphate produced as a result of GTPase activity was measured by using a p50RhoGAP or Cdc42GAP assay and absorbance-based detection method. Briefly, Cdc42 was preloaded with GTP or ZCL278 and incubated in the reaction buffer for 20 mins at 37 °C. GAP was then added for an additional 20 mins at 37 °C. Following a 10-min incubation in CytoPhos reagent, inorganic phosphate was detected at 650 nm. |
| Cell experiment [1]: | |
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Cell lines |
Cortical neurons |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20 °C for several months. |
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Reaction Conditions |
50 μM; 5 and 10 mins or 2, 4, 6, 8 and 10 mins |
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Applications |
In ZCL278-treated neurons, neuronal branching was significantly suppressed over the time course. In addition, ZCL278 markedly inhibited Cdc42-mediated growth cone motility. |
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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. | |
| Cas No. | 587841-73-4 | SDF | |
| 化学名 | 2-(4-bromo-2-chlorophenoxy)-N-[[4-[(4,6-dimethylpyrimidin-2-yl)sulfamoyl]phenyl]carbamothioyl]acetamide | ||
| 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 | ||
| 分子式 | C21H19BrClN5O4S2 | 分子量 | 584.89 |
| 溶解度 | ≥ 29.25mg/mL in DMSO | 储存条件 | Please store the product under the recommended conditions in the Certificate of Analysis. |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7097 mL | 8.5486 mL | 17.0972 mL |
| 5 mM | 0.3419 mL | 1.7097 mL | 3.4194 mL |
| 10 mM | 0.171 mL | 0.8549 mL | 1.7097 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet