587841-73-4

Basic information

• Product Name: 2-(4-broMo-2-chlorophenoxy)-N-(4-(N-(4,6-diMethylpyriMidin-2-yl)sulfaMoyl)phenylcarbaMothioyl)acetaMide
• Synonyms: 2-(4-broMo-2-chlorophenoxy)-N-(4-(N-(4,6-diMethylpyriMidin-2-yl)sulfaMoyl)phenylcarbaMothioyl)acetaMide;ZCL 278;2-(4-Bromo-2-chlorophenoxy)-N-[[[4-[[(4,6-dimethyl-2-pyrimidinyl)amino]sulfonyl]phenyl]amino]thioxomethyl]acetamide;2-(4-Bromo-2-chlorophenoxy)-N-[[[4-[[(4,6-dimethyl-2-pyrimidinyl)amino]sulfonyl]phenyl]amino]thioxomethyl]acetamide ZCL278;ZCL 278 2-(4-Bromo-2-chlorophenoxy)-N-[[[4-[[(4,6-dimethyl-2-pyrimidinyl)amino]sulfonyl]phenyl]amino]thioxomethyl]acetamide;ZCL278, >=98%;2-(4-Bromo-2-chlorophenoxy)-N-((4-(N-(4,6-dimethylpyrimidin-2-yl)sulfamoyl)phenyl)carbAmothioy
• CAS NO: 587841-73-4
• Molecular Formula: C21H19BrClN5O4S2
• Molecular Weight: 584.89366
• EINECS: 200-256-5
• Product Categories: Inhibitors
• Mol File: 587841-73-4.mol
• Article Data: 2

Chemical Properties

• Appearance: /
• Storage Temp.: +2C to +8C
• Solubility: ≥29.25 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
• CAS DataBase Reference: 2-(4-broMo-2-chlorophenoxy)-N-(4-(N-(4,6-diMethylpyriMidin-2-yl)sulfaMoyl)phenylcarbaMothioyl)acetaMide(CAS DataBase Reference)
• NIST Chemistry Reference: 2-(4-broMo-2-chlorophenoxy)-N-(4-(N-(4,6-diMethylpyriMidin-2-yl)sulfaMoyl)phenylcarbaMothioyl)acetaMide(587841-73-4)
• EPA Substance Registry System: 2-(4-broMo-2-chlorophenoxy)-N-(4-(N-(4,6-diMethylpyriMidin-2-yl)sulfaMoyl)phenylcarbaMothioyl)acetaMide(587841-73-4)

Safety Data

• Hazardous Substances Data: 587841-73-4(Hazardous Substances Data)

Usage

Uses

ZCL 278, is a selective inhibitor of Cdc42, and effectively inhibits EGF-stimulated Cdc42 activity including microspike formation in 3T3 fibroblasts and neuronal branching in primary neonatal cortical neurons.

Biological Activity

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.

Upstream product

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Relevant articles and documents

ROLES OF MODULATORS OF INTERSECTIN-CDC42 SIGNALING IN ALZHEIMER'S DISEASE

Methods of treating Alzheimer's disease and other neurodegenerative and/or neurocognitive and/or neurodevelopmental diseases are described. The methods comprise the administration of compounds that modulate an activity of cell division control protein 42 (Cdc42), such as the interaction between Cdc42 and intersectin (ITSN). Exemplary modulator compounds include thioureas, disulfonamides of fused aromatic systems (e.g., benzofuran), and acyl hydrazones, among others. Some of the modulator compounds act as activators of Cdc42, while others act as inhibitors. In some cases, the modulator compound has dual functionality and the ability of the modulator compound to act as an inhibitor or activator depends on whether or not Cdc42 is already activated in a particular disease stage or biological environment by an upstream activating signal of Cdc42.