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
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Cell permeable: yes
Primary Target
CDC42
CDC42
Reversible: yes
Disclaimer
Toxicity: Standard Handling (A)
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).
Other Notes
Friesland, A., et al. 2013. Proc. Natl. Acad. Sci. USA110, 1261.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
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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