Cat. No.: HY-112287

ERK1/2 inhibitor 1

7 Cited Publications

Customer Review

Based on 7 publication(s) in Google Scholar

ERK1/2 inhibitor 1 is a potent, orally bioavailable ERK1/2 inhibitor, showing 60% inhibition at 1 nM and an IC₅₀ of 3.0 nM against ERK1 and ERK2, respectively.

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

Purity: 99.58%
CAS No.: 2095719-90-5
Formula: C₂₉H₃₂ClN₅O₄
Molecular Weight:550.05

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

ERK1/2 inhibitor 1 Chemical Structure

CAS No.: 2095719-90-5

Size

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (7)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

ERK1/2 inhibitor 1 is a potent, orally bioavailable ERK1/2 inhibitor, showing 60% inhibition at 1 nM and an IC₅₀ of 3.0 nM against ERK1 and ERK2, respectively^[1].

IC₅₀ & Target^[1]

ERK2

3.0 nM (IC₅₀)

ERK1

All ERK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	4.9 nM Compound: 27	Antiproliferative activity against human A375 cells harboring BRAF V600E mutant after 96 hrs by Alamar blue assay Antiproliferative activity against human A375 cells harboring BRAF V600E mutant after 96 hrs by Alamar blue assay	[PMID: 29775310]
A-375	IC₅₀	4.9 nM Compound: 7	Antiproliferative activity against human A-375 cells assessed as reduction in cell viability after 96 hrs by alamar blue assay Antiproliferative activity against human A-375 cells assessed as reduction in cell viability after 96 hrs by alamar blue assay	[PMID: 34387469]
COLO 205	IC₅₀	7.5 nM Compound: 27	Antiproliferative activity against human COLO205 cells harboring BRAF V600E mutant after 96 hrs by Alamar blue assay Antiproliferative activity against human COLO205 cells harboring BRAF V600E mutant after 96 hrs by Alamar blue assay	[PMID: 29775310]
COLO 205	IC₅₀	7.5 nM Compound: 7	Antiproliferative activity against human COLO 205 cells assessed as reduction in cell viability after 96 hrs by alamar blue assay Antiproliferative activity against human COLO 205 cells assessed as reduction in cell viability after 96 hrs by alamar blue assay	[PMID: 34387469]

In Vitro

ERK1/2 inhibitor 1 (Compound 27) shows excellent antiproliferative potency with IC₅₀s of 4.9 and 7.5 nM in A375 and Colo205 cells, respectively^[1].

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

Chemical Information

CAS No. 2095719-90-5
Appearance Solid
Molecular Weight 550.05
Formula C₂₉H₃₂ClN₅O₄
Color Off-white to light yellow
SMILES

ClC1=CN=C(NC2CCOCC2)N=C1C3=CC=C(CN([C@H](C)C(N[C@H](CO)C4=CC=CC(C)=C4)=O)C5=O)C5=C3
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

Publications (7)

All RT-PCRWBFlow CytometryCell Imaging/Staining

Sort by:

Journal Impact Factor

Cell Mol Immunol

Chaperone- and PTM-mediated activation of IRF1 tames radiation-induced cell death and the inflammatory response. [Abstract]

2024 Aug;21(8):856-872. PMID: 38849539
Cell Commun Signal

Neutrophil extracellular traps induced by the hypoxic microenvironment in gastric cancer augment tumour growth. [Abstract]

2023 May 1;21(1):86. PMID: 37127629

ERK1/2 inhibitor 1 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2023 May 1;21(1):86. [Abstract]

Neutrophils were pretreated with inhibitors of the ERK (HY-112287;ERK1/2 inhibitor 1), p38 MAPK (HY-12839; p38 MAPK-IN-1), and p65 NF-кB (HY-138537; NF-κB-IN-1) pathways prior to incubation with hypoxic-CM from GC cells. The protein levels of p-ERK, p-p38, and p-p65 in neutrophils were measured by western blotting.

ERK1/2 inhibitor 1 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2023 May 1;21(1):86. [Abstract]

Neutrophils were pretreated with inhibitors of the ERK (HY-112287;ERK1/2 inhibitor 1), p38 MAPK (HY-12839; p38 MAPK-IN-1), and p65 NF-кB (HY-138537; NF-κB-IN-1) pathways prior to incubation with hypoxic-CM from GC cells. The NET formation by neutrophils was evaluated with MPO and citH3 staining. Magnification: 20 × . Scale bars: 50 μm.
Int J Mol Sci

Mitochondrial-Derived Peptide MOTS-c Increases Adipose Thermogenic Activation to Promote Cold Adaptation. [Abstract]

2019 May 17;20(10):2456. PMID: 31109005

ERK1/2 inhibitor 1 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2019 May 17;20(10):2456. [Abstract]

The level of phospho-ERK1/2, PGC1α, and UCP1 in adipocytes treated with MOTS-c and ERK inhibitor (HY-112287; ERK1/2 inhibitor 1; 10 nM).

ERK1/2 inhibitor 1 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2019 May 17;20(10):2456. [Abstract]

The RNA level of thermogenic genes (PGC1α, UCP1, and Dio2) in adipocytes treated with MOTS-c and ERK inhibitor (HY-112287; ERK1/2 inhibitor 1; 10 nM).
Cancer Med

Proton pump inhibitors stabilize the expression of PD-L1 on cell membrane depending on the phosphorylation of GSK3β. [Abstract]

2024 May;13(10):e7083. PMID: 38752436

ERK1/2 inhibitor 1 purchased from MedChemExpress. Usage Cited in: Cancer Med. 2024 May;13(10):e7083. [Abstract]

FACS analysis was used to perform the MFI of cell membrane of PD‐L1 in H441 cells with control or multiply small molecular inhibitors (Seen in the Table 1, 24 h) (n = 3). AV412 (HY‐10346; 20, 50 nM), ERK1/2 inhibitor 1 (HY‐112287; 20, 50 nM), AR‐A014418 (HY‐10512; 100, 200 nM), Erlotinib (HY‐50896; 50, 100 nM).
Adv Biol (Weinh)

HMGB1 Derived from the Pyroptotic Microenvironment Promotes Macrophage Extracellular Traps in Hirschsprung-Associated Enterocolitis. [Abstract]

2025 Sep;9(9):e00761. PMID: 40464207

ERK1/2 inhibitor 1 purchased from MedChemExpress. Usage Cited in: Adv Biol (Weinh). 2025 Sep;9(9):e00761. [Abstract]

Macrophages were pretreated with inhibitors of the ERK (HY‐112287; ERK1/2 inhibitor 1), JNK (HY‐12041; SP600125), p38 MAPK (HY‐12839; p38 MAPK-IN-1), and p65 NF‐kB (HY‐138537; NF-κB-IN-1) pathways prior to incubation with pyroptotic‐CM for 4 h.The MET formation by macrophages was evaluated with SYTOX Green staining and detected by flow cytometry.

ERK1/2 inhibitor 1 purchased from MedChemExpress. Usage Cited in: Adv Biol (Weinh). 2025 Sep;9(9):e00761. [Abstract]

Macrophages were pretreated with inhibitors of the ERK (HY‐112287; ERK1/2 inhibitor 1), JNK (HY‐12041; SP600125), p38 MAPK (HY‐12839; p38 MAPK-IN-1), and p65 NF‐kB (HY‐138537; NF-κB-IN-1) pathways prior to incubation with pyroptotic‐CM for 4 h. The p‐p38 and p‐p65 levels in macrophages were measured by western blotting.
J Obstet Gynaecol Res

Exosomal microRNA-139-5p from mesenchymal stem cells accelerates trophoblast cell invasion and migration by motivation of the ERK/MMP-2 pathway via downregulation of protein tyrosine phosphatase. [Abstract]

2020 Dec;46(12):2561-2572. PMID: 32945060
Research Square Preprint

2022 May.

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL (454.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8180 mL

9.0901 mL

18.1802 mL

5 mM

0.3636 mL

1.8180 mL

3.6360 mL

10 mM

0.1818 mL

0.9090 mL

1.8180 mL

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.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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: ≥ 2.08 mg/mL (3.78 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (3.78 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.08 mg/mL (3.78 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Heightman TD, et al. Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2. J Med Chem. 2018 Jun 14;61(11):4978-4992. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	1.8180 mL	9.0901 mL	18.1802 mL	45.4504 mL
	5 mM	0.3636 mL	1.8180 mL	3.6360 mL	9.0901 mL
	10 mM	0.1818 mL	0.9090 mL	1.8180 mL	4.5450 mL
	15 mM	0.1212 mL	0.6060 mL	1.2120 mL	3.0300 mL
	20 mM	0.0909 mL	0.4545 mL	0.9090 mL	2.2725 mL
	25 mM	0.0727 mL	0.3636 mL	0.7272 mL	1.8180 mL
	30 mM	0.0606 mL	0.3030 mL	0.6060 mL	1.5150 mL
	40 mM	0.0455 mL	0.2273 mL	0.4545 mL	1.1363 mL
	50 mM	0.0364 mL	0.1818 mL	0.3636 mL	0.9090 mL
	60 mM	0.0303 mL	0.1515 mL	0.3030 mL	0.7575 mL
	80 mM	0.0227 mL	0.1136 mL	0.2273 mL	0.5681 mL
	100 mM	0.0182 mL	0.0909 mL	0.1818 mL	0.4545 mL

Keywords

ERK1/2 inhibitor 1

7 Cited Publications

100 mg Get Quote

Subscribe to the

MedChemExpress

Newsletter

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

ERK1/2 inhibitor 1

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) ERK1/2 inhibitor 1

All ERK Isoforms

Biological Activity

Chemical Information

Publications (7)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

ERK1/2 inhibitor 1

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) ERK1/2 inhibitor 1

All ERK Isoforms

Biological Activity

Chemical Information

Publications (7)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

ERK1/2 inhibitor 1 Related Classifications

HY-112287 Related Classifications