1. Epigenetics TGF-beta/Smad
  2. PKC
  3. NSC668394

NSC668394 is a potent ezrin (Thr567) phosphorylation inhibitor, with a Kd of 12.59 μM. NSC668394 inhibit ezrin T567 phosphorylation caused by PKCΙ primarily via their binding to ezrin. NSC668394 can be used to prevent tumor metastasis.

For research use only. We do not sell to patients.

NSC668394 Chemical Structure

NSC668394 Chemical Structure

CAS No. : 382605-72-3

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 132 In-stock
Solution
10 mM * 1 mL in DMSO USD 132 In-stock
Solid
5 mg USD 120 In-stock
10 mg USD 180 In-stock
25 mg USD 370 In-stock
50 mg USD 600 In-stock
100 mg USD 980 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of NSC668394:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE NSC668394

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

NSC668394 is a potent ezrin (Thr567) phosphorylation inhibitor, with a Kd of 12.59 μM. NSC668394 inhibit ezrin T567 phosphorylation caused by PKCΙ primarily via their binding to ezrin. NSC668394 can be used to prevent tumor metastasis[1][2][3].

In Vitro

NSC668394 (10 μM; pretreated for 15 min) inhibits ezrin T567 phosphorylation (IC50=8.1 μM) and actin binding in vitro[1].
NSC668394 (1-10 μM; 2-6 h) inhibits ezrin-mediated invasion by K7M2 osteosarcoma (OS) cells on the HUVEC monolayer[1].
NSC668394 (20 μM) causes significant decrease in growth in JM1 and JM2 rat hepatoma cell lines[2].
NSC668394 (10 μM) reduces cell motility phenotypes in zebrafish[1].

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

Western Blot Analysis[1]

Cell Line: K7M2 OS cells
Concentration: 10 μM
Incubation Time: 6 hours
Result: Inhibited T567 phosphorylation and actin binding of endogenous ezrin without altering cellular ezrin levels.
In Vivo

NSC668394 (0.226 mg/kg/day; i.p. 5-days a week) inhibits ezrin-dependent in vivo OS metastatic growth in mouse lung[1].

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

Animal Model: Female BALB/c and SCID/Beige mice were injected with K7M2 or MNNG-HOS tumor cells[1]
Dosage: 0.226 mg/kg/day
Administration: I.p. 5-days a week for 66 days
Result: Showed an increase in survival.
Decreased the number of the green fluorescent protein (GFP)-expressing metastatic foci in the lung tissues.
Molecular Weight

452.10

Formula

C17H12Br2N2O3

CAS No.
Appearance

Solid

Color

Orange to red

SMILES

O=C(C=C1NCCC2=CC(Br)=C(O)C(Br)=C2)C3=C(N=CC=C3)C1=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (110.60 mM; ultrasonic and warming and heat to 60°C; 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 2.2119 mL 11.0595 mL 22.1190 mL
5 mM 0.4424 mL 2.2119 mL 4.4238 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration
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Volume
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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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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

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 (5.53 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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 +
+
%
Tween-80 +
%
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: 99.80%

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2119 mL 11.0595 mL 22.1190 mL 55.2975 mL
5 mM 0.4424 mL 2.2119 mL 4.4238 mL 11.0595 mL
10 mM 0.2212 mL 1.1059 mL 2.2119 mL 5.5297 mL
15 mM 0.1475 mL 0.7373 mL 1.4746 mL 3.6865 mL
20 mM 0.1106 mL 0.5530 mL 1.1059 mL 2.7649 mL
25 mM 0.0885 mL 0.4424 mL 0.8848 mL 2.2119 mL
30 mM 0.0737 mL 0.3686 mL 0.7373 mL 1.8432 mL
40 mM 0.0553 mL 0.2765 mL 0.5530 mL 1.3824 mL
50 mM 0.0442 mL 0.2212 mL 0.4424 mL 1.1059 mL
60 mM 0.0369 mL 0.1843 mL 0.3686 mL 0.9216 mL
80 mM 0.0276 mL 0.1382 mL 0.2765 mL 0.6912 mL
100 mM 0.0221 mL 0.1106 mL 0.2212 mL 0.5530 mL
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NSC668394 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.

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NSC668394
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HY-115492
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