- ML 141
| ZCL278Selective Cdc42 inhibitor |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
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- Purity = 97.00%
- COA (Certificate Of Analysis)
- MS (Retest)
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
Related Biological Data
| Description | ZCL278 is a selective inhibitor of Cdc42 GTPase with a Kd value of 11.4 μM. | |||||
| Targets | Cdc42 GTPase | |||||
| IC50 | 11.4 μM(Kd) | |||||
| Kinase experiment [1]: | |
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]: | |
Cell lines | Cortical neurons |
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. |
Reaction Conditions | 50 μM; 5 and 10 mins or 2, 4, 6, 8 and 10 mins |
Applications | In ZCL278-treated neurons, neuronal branching was significantly suppressed over the time course. In addition, ZCL278 markedly inhibited Cdc42-mediated growth cone motility. |
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. | |
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| Cas No. | 587841-73-4 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | 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 | ||
| Formula | C21H19BrClN5O4S2 | M.Wt | 584.89 |
| Solubility | ≥29.25mg/mL in DMSO | Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
