5.00503
CDC42 Inhibitor III, ZCL278
别名:
CDC42 Inhibitor III, ZCL278, CDC42 GTPase Inhibitor III, 4-(3-(2-(4-Bromo-2-chloro-phenoxy)-acetyl)-thioureido)-N-(4,6-dimethyl-pyrimidin-2-yl)-benzenesulfonamide, 2-(4-Bromo-2-chlorophenoxy)-N-((4-((4,6-dimethyl-2-pyrimidinyl)sulfamoyl)phenyl)carbamothioyl)acetamide
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关于此项目
经验公式（希尔记法）:
C21H19BrClN5O4S2
化学文摘社编号:
分子量:
584.89
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
SMILES string
[S](=O)(=O)(Nc3nc(cc(n3)C)C)c1ccc(cc1)NC(=S)NC(=O)COc2c(cc(cc2)Br)Cl
InChI
1S/C21H19BrClN5O4S2/c1-12-9-13(2)25-20(24-12)28-34(30,31)16-6-4-15(5-7-16)26-21(33)27-19(29)11-32-18-8-3-14(22)10-17(18)23/h3-10H,11H2,1-2H3,(H,24,25,28)(H2,26,27,29,33)
InChI key
XKZDWYDHEBCGCG-UHFFFAOYSA-N
assay
≥94% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
light beige
solubility
DMSO: 50 mg/mL
Quality Level
General description
A cell-permeable, non-cytotoxic, aqueous soluble (181 µM in PBS, pH 7.4, containing 0.33% DMSO) pyrimidinylthiourea compound that targets Cdc42 GEF ITSN/intersectin and adjacent GTP/GDP binding site (Kd = 6.4 and 11.4 µM by fluorescence titration and SPR, respectively) and effectively inhibits EGF-stimulated Cdc42 activity (by 100% with 1 h pretreatment of 50 µM ZCL278) and Cdc42-dependent microspike/filopodia formation in serum-starved Swiss 3T3 fibroblast cultures without affecting RhoA-dependent cellular processes or Rac1-dependent lamellipodia formation. Short-term ZCL278 exposure in 5 d-cultured primary neonatal cortical neurons from 1 d postnatal mice is shown to dramatically abolish neurite branching (Ave branches per neurite = 21, 7.8, and 6.4, respectively, with 0, 5, and 10 min exposure to 50 µM ZCL278).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
CDC42
CDC42
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze 9-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Friesland, A., et al. 2013. Proc. Natl. Acad. Sci. USA110, 1261.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
Wenjie Huang et al.
Cancer research, 80(13), 2804-2817 (2020-05-08)
Pancreatic ductal adenocarcinoma (PDAC) is an aggressive malignancy characterized by extensive local invasion and systemic spread. In this study, we employed a three-dimensional organoid model of human pancreatic cancer to characterize the molecular alterations critical for invasion. Time-lapse microscopy was
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