1. MAPK/ERK Pathway Stem Cell/Wnt
  2. ERK
  3. ZINC12409120

ZINC12409120 is a high selective ERK inhibitor. ZINC12409120 acts on disrupting FGF23:α-Klotho interaction to inhibit ERK activity with an IC50 of 5.0 μM.

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ZINC12409120

ZINC12409120 Chemical Structure

CAS No. : 1010888-06-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
In-stock
Solution
10 mM * 1 mL in DMSO In-stock
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Based on 1 publication(s) in Google Scholar

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Description

ZINC12409120 is a high selective ERK inhibitor. ZINC12409120 acts on disrupting FGF23:α-Klotho interaction to inhibit ERK activity with an IC50 of 5.0 μM[1].

IC50 & Target

ERK

5 μM (IC50)

In Vitro

FGF23 induces hypophosphatemia, mediated by ternary complex formed by FGF23, the FGF receptor (FGFR), and α-Klotho[1].
ZINC12409120 (1 nM-0.1 mM; 5 h) inhibits ERK reporter activities mediated by FGF23 (1 μM), with an IC50 of 5 μM[1].
ZINC12409120 (10 μM; 5 h) specificaly inhibits ERK activity mediated by FGF23:α-Klotho instead of EGF-mediated ERK activation, and exhibits no inhibitory effect on EGFR tyrosine kinase or EGF/EGFR interaction[1].
ZINC12409120 has an half-life of 8.4 h, predicted by pkCSM64 (http://biosig.unimelb.edu.au/pkcsm/)[1].

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

Cell Proliferation Assay[1]

Cell Line: Human embryonic kidney (HEK) 293T cells
Concentration: 1 nM-0.1 mM
Incubation Time: 5 hours
Result: Inhibited FGF23-mediated ERK reporter activity in a dose-dependent manner, with an IC50 of 5 μM. And reduced FGF23-mediated ERK activities by 70%, as well.
Molecular Weight

344.37

Formula

C20H16N4O2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1CC2=C(C=CC=C2)CC1)C3=NC(C4=CC=CC5=C4C=CN5)=NO3

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 (145.19 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 2.9039 mL 14.5193 mL 29.0385 mL
5 mM 0.5808 mL 2.9039 mL 5.8077 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 (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.26 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

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: 99.95%

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 2.9039 mL 14.5193 mL 29.0385 mL 72.5963 mL
5 mM 0.5808 mL 2.9039 mL 5.8077 mL 14.5193 mL
10 mM 0.2904 mL 1.4519 mL 2.9039 mL 7.2596 mL
15 mM 0.1936 mL 0.9680 mL 1.9359 mL 4.8398 mL
20 mM 0.1452 mL 0.7260 mL 1.4519 mL 3.6298 mL
25 mM 0.1162 mL 0.5808 mL 1.1615 mL 2.9039 mL
30 mM 0.0968 mL 0.4840 mL 0.9680 mL 2.4199 mL
40 mM 0.0726 mL 0.3630 mL 0.7260 mL 1.8149 mL
50 mM 0.0581 mL 0.2904 mL 0.5808 mL 1.4519 mL
60 mM 0.0484 mL 0.2420 mL 0.4840 mL 1.2099 mL
80 mM 0.0363 mL 0.1815 mL 0.3630 mL 0.9075 mL
100 mM 0.0290 mL 0.1452 mL 0.2904 mL 0.7260 mL
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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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Product Name:
ZINC12409120
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HY-150687
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