2. GPCR/G Protein Anti-infection MAPK/ERK Pathway
  3. Dengue Virus Ras VSV Arenavirus
  4. ZCL278

ZCL278 is a selective Cdc42 inhibitor with Kds of 6.4 μM in fluorescence titration and 11.4 μM in surface plasmon resonance (SPR) measurement. ZCL278 is able to disrupt the Cdc42-ITSN interaction as well as GTP/GDP binding. ZCL278 has inhibitory effects on various enveloped viruses, but is ineffective against non-enveloped viruses. ZCL278 can be used for the studies of arsenic neurotoxicity and HER2-positive gastric cancer (GC).

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ZCL278

ZCL278 Chemical Structure

CAS No. : 587841-73-4

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Based on 3 publication(s) in Google Scholar

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Description

ZCL278 is a selective Cdc42 inhibitor with Kds of 6.4 μM in fluorescence titration and 11.4 μM in surface plasmon resonance (SPR) measurement. ZCL278 is able to disrupt the Cdc42-ITSN interaction as well as GTP/GDP binding. ZCL278 has inhibitory effects on various enveloped viruses, but is ineffective against non-enveloped viruses. ZCL278 can be used for the studies of arsenic neurotoxicity and HER2-positive gastric cancer (GC)[1][2][3][4].

IC50 & Target

Kd: 11.4 μM (Cdc42)[1]
In Vitro

ZCL278 (5-50 μM, 24 h) impedes wound healing without disruption of cell viability in PC-3 cells[1].
ZCL278 (50 μM, 5-15 min) exhibits a time-dependent inhibition of Cdc42 activity in PC-3 cells[1].
ZCL278 (50 μM, 0-10 min) inhibits mice primary neurons branchingand growthconemotility[1].
ZCL278 (0.01-1000 μM, 0-18 h) does not interfere with Junin virus (JUNV) attachment to the cell surface or virus particle internalization into host cells, it prevents the release of JUNV ribonucleoprotein cores into the cytosol and decreases pH-mediated viral fusion with host membranes in Vero, SUM159, SVG-A, or A549 cells[2].
ZCL278 (50 μM, 6-24 h) significantly inhibits VSV, LCMV and DV2 infections, but has no effect on non-enveloped virus PV1 in Vero or Huh7 cells[2].
ZCL278 (20 μM, 25 h) improves the cytotoxicity of NaAsO2 in rat astrocytes[3].
ZCL278 reduces cholesterol levels in the plasma membrane and reverses collateral resistance between Trastuzumab (HY-P9907) and chemotherapy in TC cells[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

ZCL278 Related Antibodies

Cell Migration Assay [1]

Cell Line: PC-3 cells
Concentration: 5 and 50 μM
Incubation Time: 24 h
Result: Dose-dependently inhibited cell migration (50 μM inhibits by 92%), did not affect cell viability, and eliminated the interference of toxicity.

Western Blot Analysis[1]

Cell Line: PC-3 cells
Concentration: 50 μM
Incubation Time: 5, 10, 15 min
Result: Inhibited endogenous Rac/Cdc42 activities.
Inhibited Cdc42 activity.
In Vivo

ZCL278 (1-100 μg/kg, i.p., once daily for 4 days) inhibits JUNV replication in a mouse model, and no toxicity is detected[2].
ZCL278 (50 mg/kg, i.p., every four days for 33 days) effectively reduces cholesterol enrichment in the plasma membrane and reverses collateral resistance between Trastuzumab and chemotherapy in [4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: JUNV infection model established in C57BL/6 mice [2]
Dosage: 1, 10 and 100 μg/kg
Administration: Intraperitoneal injection (i.p.), once daily for 4 days
Result: Reduced the viral load in the spleen by more than 33 times.
Did not affect the weight of mice.
Animal Model: Trastuzumab-resistant model established in female nude mice aged 3–4 weeks[4]
Dosage: 50 mg/kg
Administration: Intraperitoneal injection (i.p.), every four days for 33 days
Result: Remarkably suppressed tumor growth, while PTX/DTX alone failed to exert anti-tumor efficacy.
Markedly decreased Cdc42-GTP activity and mem brane cholesterol contents.
Molecular Weight

584.89

Formula

C21H19BrClN5O4S2
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(NC(NC1=CC=C(S(=O)(NC2=NC(C)=CC(C)=N2)=O)C=C1)=S)COC3=CC=C(Br)C=C3Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (85.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7097 mL 8.5486 mL 17.0972 mL
5 mM 0.3419 mL 1.7097 mL 3.4194 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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C2

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V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.27 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.27 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
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%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.49%

SDS (597 KB)

COA (246 KB) HNMR (239 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7097 mL 8.5486 mL 17.0972 mL 42.7431 mL
5 mM 0.3419 mL 1.7097 mL 3.4194 mL 8.5486 mL
10 mM 0.1710 mL 0.8549 mL 1.7097 mL 4.2743 mL
15 mM 0.1140 mL 0.5699 mL 1.1398 mL 2.8495 mL
20 mM 0.0855 mL 0.4274 mL 0.8549 mL 2.1372 mL
25 mM 0.0684 mL 0.3419 mL 0.6839 mL 1.7097 mL
30 mM 0.0570 mL 0.2850 mL 0.5699 mL 1.4248 mL
40 mM 0.0427 mL 0.2137 mL 0.4274 mL 1.0686 mL
50 mM 0.0342 mL 0.1710 mL 0.3419 mL 0.8549 mL
60 mM 0.0285 mL 0.1425 mL 0.2850 mL 0.7124 mL
80 mM 0.0214 mL 0.1069 mL 0.2137 mL 0.5343 mL
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ZCL278 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ZCL278587841-73-4ZCL 278ZCL-278Dengue VirusRasVSVArenavirusDENVVesicular Stomatitis VirusCdc42Cdc42-ZCL278actin-basedcellularGolgiorganizationmotilitymetastaticprostatecancerInhibitorinhibitorinhibit

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