ERK1/2 inhibitor 1

Name: ERK1/2 inhibitor 1
Brand: MedChemExpress
SKU: HY-112287
Rating: 5.0 (7 reviews)

Cat. No.: HY-112287 Purity: 99.58%: Data Sheet
COA

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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.

CAS No. : 2095719-90-5

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 7 publication(s) in Google Scholar

7 Publications Citing Use of MCE ERK1/2 inhibitor 1

•Research Square Preprint. 2022 May.

RT-PCR

Flow Cytometry

Cell Imaging/Staining

: ERK1/2 inhibitor 1 purchased from MedChemExpress. Usage Cited in: Adv Biol (Weinh). 2025 Jun 4: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 Jun 4: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.

: 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).

: 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.

: 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).

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Biological Activity
Purity & Documentation
References
Customer Review

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

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.

Molecular Weight

550.05

Formula

C₂₉H₃₂ClN₅O₄

CAS No.

2095719-90-5

Appearance

Solid

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

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 2.08 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.
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: ≥ 2.08 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.
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.
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

mg/kg

Animal weight
(per animal)

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: 99.58%

Select Batch:

Data Sheet (275 KB) SDS (251 KB)

COA (252 KB) HNMR (295 KB) LCMS (94 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]

Complete Stock Solution Preparation Table

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