Cat. No.: HY-12275

FR 180204

26 Cited Publications

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Based on 26 publication(s) in Google Scholar

FR 180204 is an ATP-competitive and selective ERK inhibitor. FR 180204 inhibits ERK1 and ERK2 with IC₅₀s of 0.51 μM (K_i=0.31 μM) and 0.33 μM (K_i=0.14 μM), respectively.

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Pureté: 99.91%
CAS No.: 865362-74-9
Formule: C₁₈H₁₃N₇
Masse moléculaire:327.34

Stockage:

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

FR 180204 Chemical Structure

CAS No.: 865362-74-9

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (26)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

ERK2

0.14 μM (Ki)

ERK1

0.31 μM (Ki)

ERK2

0.33 μM (IC₅₀)

ERK1

0.51 μM (IC₅₀)

Voir tous les produits spécifiques à Isoform ERK :

In Vitro

In AP-1-transfected cells, FR180204 dose-dependently inhibits AP-1 transactivation with IC₅₀ of 3.1 μM^[1]. FR 180204 inhibits spontaneous mesothelioma cell growth^[3].

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

In Vivo

FR180204 (100 mg/kg, i.p., b.i.d.) significantly decreases the severity of symptoms and body weight loss in collagen-induced arthritis mice^[2]. In a mouse model of dengue virus (DENV) infection, FR180204 limits hepatocyte apoptosis, reduces DENV-induced liver injury, and improves clinical parameters^[4].

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

Chemical Information

CAS No. 865362-74-9
Appearance Solid
Masse moléculaire 327.34
Formule C₁₈H₁₃N₇
Color Light yellow to yellow
SMILES

NC1=NNC2=NN=C(C3=C4C=CC=CN4N=C3C5=CC=CC=C5)C=C21
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Publications (26)

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Journal Impact Factor

Immunity

Neutrophil "plucking" on megakaryocytes drives platelet production and boosts cardiovascular disease. [Abstract]

2022 Dec 13;55(12):2285-2299.e7. PMID: 36272416
Autophagy

PBK-Loaded secretory autophagosomes drive radiotherapy-induced systemic adipose depletion via MAPK/ERK-PRKA/PKA-LIPE/HSL signaling: a therapeutic target for esophageal cancer cachexia. [Abstract]

2026 Apr 23:1-26. PMID: 41988986
Neuron

C5aR1+ microglia exacerbate neuroinflammation and cerebral edema in acute brain injury. [Abstract]

2025 Nov 18:S0896-6273(25)00803-7. PMID: 41260217
Adv Sci (Weinh)

Calhm6 Governs Macrophage Polarization Through Chp1-Camk4-Creb1 Axis and Ectosomal Delivery in Inflammatory Responses. [Abstract]

2025 Sep 26:e02395. PMID: 40999918
Cell Death Differ

c-Myc inhibits myoblast differentiation and promotes myoblast proliferation and muscle fibre hypertrophy by regulating the expression of its target genes, miRNAs and lincRNAs. [Abstract]

2019 Mar;26(3):426-442. PMID: 29786076

FR 180204 purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2019 Mar;26(3):426-442. [Abstract]

Chicken breast muscles are injected with FR180204 or control, and the protein levels of the ERK1 and p-ERK are analysed.
J Transl Med

Delineation of colorectal cancer ligand-receptor interactions and their roles in the tumor microenvironment and prognosis. [Abstract]

2021 Dec 7;19(1):497. PMID: 34876143
Int J Biol Macromol

Ginsenoside Rb1 inhibits porcine epidemic diarrhea virus replication through suppressing S1 protein mediated the MAPK/ERK pathway and reducing apoptosis. [Abstract]

2025 Feb 11:140937. PMID: 39947549
Antioxidants (Basel)

Canagliflozin Inhibits Palmitic Acid-Induced Vascular Cell Aging In Vitro through ROS/ERK and Ferroptosis Pathways. [Abstract]

2024 Jul 11;13(7):831. PMID: 39061899
Cell Mol Life Sci

Suppression of Skp2 contributes to sepsis-induced acute lung injury by enhancing ferroptosis through the ubiquitination of SLC3A2. [Abstract]

2024 Jul 30;81(1):325. PMID: 39079969
Inflammation

FGF-21 Elevated IL-10 Production to Correct LPS-Induced Inflammation. [Abstract]

2018 Jun;41(3):751-759. PMID: 29427162

FR 180204 purchased from MedChemExpress. Usage Cited in: Inflammation. 2018 Jun;41(3):751-759. [Abstract]

ERK1/2-specific inhibitor (FR 180204) is responsible for the inhibition of FGF21-induced IL-10 expression without affecting the viability of the THP-1 cells.
Cell Signal

A novel role of follicular fluid chemokine CCL21 in promoting porcine oocyte in vitro maturation through activating ERK1/2 signaling pathway. [Abstract]

2026 Jun:142:112431. PMID: 41720327
Cell Signal

Paeoniflorin-6'-O-benzene sulfonate inhibits keratinocyte proliferation by restoring GRK2-JAK1 colocalization in mouse model of psoriasis. [Abstract]

2025 Jul:131:111706. PMID: 40037425
J Pharmacol Exp Ther

Fluvastatin Induces Apoptosis in Primary and Transformed Mast Cells. [Abstract]

2020 Jul;374(1):104-112. PMID: 32434944
Mater Technol (N Y N Y)

2025 Jun 17.
Vet Res

The CD2v protein of African swine fever virus inhibits macrophage migration and inflammatory cytokines expression by downregulating EGR1 expression through dampening ERK1/2 activity. [Abstract]

2023 Nov 15;54(1):106. PMID: 37968713
Am J Cancer Res

SHMT2 promotes tumor growth through VEGF and MAPK signaling pathway in breast cancer. [Abstract]

2022 Jul 15;12(7):3405-3421. PMID: 35968337
Microbes Infect

Suppressive effects of toll-like receptor 2, toll-like receptor 4, and toll-like receptor 7 on protective responses to Mycobacterium bovis BCG from epithelial cells. [Abstract]

2025 Feb;27(2):105428. PMID: 39368609
Vet Microbiol

AS-IV exhibits anti-SADS-CoV effects through the inhibition of the MAPK/JNK signaling pathway mediated by the S1 protein. [Abstract]

2025 Dec 29:313:110858. PMID: 41477941
J Cardiovasc Transl Res

Foam Cell-Derived CXCL14 Muti-Functionally Promotes Atherogenesis and Is a Potent Therapeutic Target in Atherosclerosis. [Abstract]

2020 Apr;13(2):215-224. PMID: 31728901
Onco Targets Ther

18β-Glycyrrhetinic Acid Has Anti-Cancer Effects via Inducing Apoptosis and G2/M Cell Cycle Arrest, and Inhibiting Migration of A549 Lung Cancer Cells. [Abstract]

2021 Oct 22;14:5131-5144. PMID: 34712051
Research Square Preprint

2023 Apr 10.
Research Square Print

2023 Feb 1.
Biomed Pharmacother

NT157 inhibits cell proliferation and sensitizes glioma cells to TRAIL-induced apoptosis by up-regulating DR5 expression. [Abstract]

2022 Sep:153:113502. PMID: 36076591
Research Square Preprint

2021 Nov.
Environ Toxicol

Molecular mechanisms of quinalizarin induces apoptosis and G0/G1 cell cycle of human esophageal cancer HCE-4 cells depends on MAPK, STAT3, and NF-κB signaling pathways. [Abstract]

2021 Feb;36(2):276-286. PMID: 33030807
ACS Comb Sci

Benzimidazolyl-pyrazolo[3,4- b]pyridinones, Selective Inhibitors of MOLT-4 Leukemia Cell Growth and Sea Urchin Embryo Spiculogenesis: Target Quest. [Abstract]

2019 Dec 9;21(12):805-816. PMID: 31689077

Solvant et solubilité

In Vitro:

DMSO : ≥ 50 mg/mL (152.75 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

3.0549 mL

15.2746 mL

30.5493 mL

5 mM

0.6110 mL

3.0549 mL

6.1099 mL

10 mM

0.3055 mL

1.5275 mL

3.0549 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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: ≥ 2.5 mg/mL (7.64 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.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (7.64 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 900 μL 20% SBE-β-CD in Saline, 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

Protocole

Kinase Assay^[1]

Nunc-Immuno MaxiSorp plates are coated with 20 μg/mL MBP solution in phosphate-buffered saline (PBS). After washing with PBS containing 0.05% Tween 20 (T-PBS), blocking buffer (T-PBS containing 3% BSA) is added to each well and the plates are incubated for 10 min at room temperature. After washing with T-PBS, chemical compounds, ATP and recombinant ERK2 diluted in assay dilution buffer (20 mM Mops, pH 7.2, 25 mM β-glycerol phosphate, 5 mM EGTA, 1 mM sodium orthovanadate, 1 mM dithiothreitol, and 50 μg/mL BSA) and are added to each well. Vehicle groups (containing 0.1% DMSO) and kinase-withdrawal groups are used for the control and basal determinations. After incubation for 1 h at room temperature, plates are washed twice with T-PBS. Anti-phospho MBP antibody (0.2 μg/mL) is added to each well, and the plates are incubated for 1 h at room temperature. After washing, anti-mouse HRP-conjugated polyclonal antibodies are added and the plates are incubated for 30 min.

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

Animal Administration^[2]

In brief, mice are randomized and grouped by body weight immediately before treatment. Bovine CII is dissolved in 0.1mol/Lacetic acid at the concentration of 10 mg/mL and then emulsified in an equal volume of Freund’s complete adjuvant H37Rv. Apart from a naive group, each mouse is immunized with 25 μL of the CII emulsion into the tail base, followed by a boost injection 3 weeks after primary injection (day 0). FR180204 and methylprednisolone are ground and suspended in 0.1% methylcellulose solution to a volume of 5 mL/kg. Drugs are given by twice daily intraperitoneal injection from days 0 to 12 in accordance with pharmacokinetic studies with superior area under the curve and Cmax values of i.p. versus s.c. or p.o. administration. The initial administration is 30 min before the boost CII injection. The clinical score of arthritis is obtained by summing the visual severity grade of each limb, scored as follows: 0, no arthritis; 1, one swollen digit; 2, two or more swollen digits or swelling of the entire paw without ankylosis; 3, gross swelling with ankylosis of the paw. Body weight is measured on day 12.

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (287 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 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)
Instruction de manipulation (2659 KB)

Références

[1]. Ohori M, et al. Identification of a selective ERK inhibitor and structural determination of the inhibitor-ERK2 complex. Biochem Biophys Res Commun. 2005 Oct 14;336(1):357-63. [Content Brief]

[2]. Ohori M, et al. FR180204, a novel and selective inhibitor of extracellular signal-regulated kinase, ameliorates collagen-induced arthritis in mice. Naunyn Schmiedebergs Arch Pharmacol. 2007 Jan;374(4):311-6. [Content Brief]

[3]. Honda M, et al. Mesothelioma cell proliferation through autocrine activation of PDGF-ββ receptor. Cell Physiol Biochem. 2012;29(5-6):667-74 [Content Brief]

[4]. Sreekanth GP, et al. Role of ERK1/2 signaling in dengue virus-induced liver injury. Virus Res. 2014 Aug 8;188:15-26 [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	3.0549 mL	15.2746 mL	30.5493 mL	76.3732 mL
	5 mM	0.6110 mL	3.0549 mL	6.1099 mL	15.2746 mL
	10 mM	0.3055 mL	1.5275 mL	3.0549 mL	7.6373 mL
	15 mM	0.2037 mL	1.0183 mL	2.0366 mL	5.0915 mL
	20 mM	0.1527 mL	0.7637 mL	1.5275 mL	3.8187 mL
	25 mM	0.1222 mL	0.6110 mL	1.2220 mL	3.0549 mL
	30 mM	0.1018 mL	0.5092 mL	1.0183 mL	2.5458 mL
	40 mM	0.0764 mL	0.3819 mL	0.7637 mL	1.9093 mL
	50 mM	0.0611 mL	0.3055 mL	0.6110 mL	1.5275 mL
	60 mM	0.0509 mL	0.2546 mL	0.5092 mL	1.2729 mL
	80 mM	0.0382 mL	0.1909 mL	0.3819 mL	0.9547 mL
	100 mM	0.0305 mL	0.1527 mL	0.3055 mL	0.7637 mL

Keywords

FR 180204

26 Cited Publications

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FR 180204

Anti-Infection Compound Library

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Antiviral Compound Library

Anti-Aging Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Glutamine Metabolism Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) FR 180204

Voir tous les produits spécifiques à Isoform ERK

Activité biologique

Chemical Information

Publications (26)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

FR 180204 Related Classifications

HY-12275 Related Classifications