2. MAPK/ERK Pathway Stem Cell/Wnt
  3. ERK
  4. ERK-IN-4

ERK-IN-4 is an ERK inhibitor binds preferentially to ERK2 with a Kd of 5 μM. ERK-IN-4 specificity inhibits ERK Rsk-1 and Elk-1 phosphorylation. ERK-IN-4 has little effect on ERK protein phosphorylation by its upstream activator MEK1/2.

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ERK-IN-4 Chemical Structure

ERK-IN-4 Chemical Structure

CAS No. : 1049738-54-6

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1 mg USD 50 In-stock
5 mg USD 110 In-stock
10 mg USD 180 In-stock
25 mg USD 378 In-stock
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Based on 1 publication(s) in Google Scholar

ERK-IN-4 Related Antibodies

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ERK ERK1 ERK2 ERK5 ERK8

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Description

ERK-IN-4 is an ERK inhibitor binds preferentially to ERK2 with a Kd of 5 μM. ERK-IN-4 specificity inhibits ERK Rsk-1 and Elk-1 phosphorylation. ERK-IN-4 has little effect on ERK protein phosphorylation by its upstream activator MEK1/2[1].

IC50 & Target[1]

ERK2

5 μM (Kd)

In Vitro

ERK-IN-4 (Compound 76; 10-75 μM; 10 days) completely inhibits cell proliferation, and decreases number of cell colonies[1].
ERK-IN-4 (Compound 76; 100 μM) inhibits ERK-mediated phosphorylation of Rsk-1 on Thr573 and ERK-mediated Elk-1 phosphorylation in HeLa cells[1].

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

ERK-IN-4 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: HeLa, A549, or SUM-159 cells
Concentration: 10 µM, 20 µM, 30 µM, 40 µM, 150 µM for A549, or SUM-159 cells; 25 µM, 50 µM, 75 µM for HeLa cells
Incubation Time: 10 days
Result: Completely inhibited cell proliferation.
Molecular Weight

328.81

Formula

C14H17ClN2O3S
CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

O=C(N(CCN)C/1=O)SC1=C/C2=CC=C(OCC)C=C2.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (76.03 mM; ultrasonic and warming and heat to 80°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 3.0413 mL 15.2064 mL 30.4127 mL
5 mM 0.6083 mL 3.0413 mL 6.0825 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 (sealed storage, away from moisture). 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
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 (7.60 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    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% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (7.60 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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
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 (sealed storage, away from moisture). 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 3.0413 mL 15.2064 mL 30.4127 mL 76.0318 mL
5 mM 0.6083 mL 3.0413 mL 6.0825 mL 15.2064 mL
10 mM 0.3041 mL 1.5206 mL 3.0413 mL 7.6032 mL
15 mM 0.2028 mL 1.0138 mL 2.0275 mL 5.0688 mL
20 mM 0.1521 mL 0.7603 mL 1.5206 mL 3.8016 mL
25 mM 0.1217 mL 0.6083 mL 1.2165 mL 3.0413 mL
30 mM 0.1014 mL 0.5069 mL 1.0138 mL 2.5344 mL
40 mM 0.0760 mL 0.3802 mL 0.7603 mL 1.9008 mL
50 mM 0.0608 mL 0.3041 mL 0.6083 mL 1.5206 mL
60 mM 0.0507 mL 0.2534 mL 0.5069 mL 1.2672 mL
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ERK-IN-4 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:

ERK-IN-41049738-54-6ERKExtracellular signal regulated kinasesRsk-1Thr573Elk-1cell coloniesInhibitorinhibitorinhibit

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