ZCL278

Catalog No.S7293

ZCL278 is a selective Cdc42 GTPase inhibitor with Kd of 11.4 μM.

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ZCL278 Chemical Structure

ZCL278 Chemical Structure
Molecular Weight: 584.89

Validation & Quality Control

Quality Control & MSDS

Product Information

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Product Description

Biological Activity

Description ZCL278 is a selective Cdc42 GTPase inhibitor with Kd of 11.4 μM.
Targets Cdc42 GTPase [1]
IC50 11.4 μM(Kd)
In vitro ZCL278 inhibits Cdc42 GTPase activity by the competition with GTP and inhibits Rac/Cdc42 phosphorylation in a time-dependent manner. ZCL278 (50 μM) inhibits Cdc42-mediated microspike formation and disrupts GM130-docked Golgi structures in serum-starved Swiss 3T3 fibroblasts. In addition, ZCL278 also suppresses Cdc42-mediated neuronal branching and growth cone dynamics as well as actin-based motility and migration in a metastatic prostate cancer PC-3 cell line without cytotoxicity. [1]
In vivo
Features

Protocol(Only for Reference)

Kinase Assay:

[1]

p50RhoGAP or Cdc42GAP Assay Inorganic phosphate produced as a result of GTPase activity is measured by using a p50RhoGAP or Cdc42GAP assay (Cytoskeleton) and absorbance-based detection method. Briefly, Cdc42 is preloaded with GTP or ZCL278 and incubated in the reaction buffer (provided in the kit) for 20 min at 37 °C. GAP is then added for an additional 20 min at 37 °C. Following a 10-min incubation in CytoPhos reagent (Cytoskeleton), inorganic phosphate was detected at 650 nm.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Friesland A, et al. Proc Natl Acad Sci U S A. 2013, 110(4), 1261-1266.

Chemical Information

Download ZCL278 SDF
Molecular Weight (MW) 584.89
Formula

C21H19BrClN5O4S2

CAS No. 587841-73-4
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 100 mg/mL (170.97 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 2-(4-Bromo-2-chlorophenoxy)-N-[[[4-​[[(4,6-dimethyl-2-pyrimidinyl)amino]sulfonyl]pheny​l]amino]thioxomethyl]acetamide

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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