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Chemical Structure| 865362-74-9 Chemical Structure| 865362-74-9

Structure of FR 180204
CAS No.: 865362-74-9

Chemical Structure| 865362-74-9

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FR 180204 is an ATP-competitive and selective ERK inhibitor, inhibiting ERK1 and ERK2 with IC50 values of 0.51 μM (Ki = 0.31 μM) and 0.33 μM (Ki = 0.14 μM), respectively.

Synonyms: ERK Inhibitor II

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Product Citations

Product Citations

Zhao, Bin ; Qiu, Xinjie ; Wang, Chong ; Wu, Shaobang ; Yin, Xin ; Zhang, Lina , et al.

Abstract: Oral ulcer (OU) is a highly prevalent mucosal disease characterized by persistent epithelial disruption. The primary challenge in its prolonged healing process is the disorder of re-epithelialization. This study develops a self-assembled hydrogel platform based on the natural small molecule rutin, which overcomes the re-epithelialization barrier through the synergistic effects of early growth response factor 1 (EGR1) gene programming and microenvironment remodeling. In this hydrogel, rutin formed supramolecular structures via hydrogen bonds and p–p interactions without structural modification. In vitro experiments confirm that rutin-based self-assembled hydrogel (RUTG) possesses excellent sustained-release properties and biocompatibility. Moreover, RUTG specifically regulates the transcriptional activation and translation of EGR1, thereby mediating the expression of re-epithelialization-related protein SOX9, and ultimately accelerating cell proliferation and migration as well as promoting re-epithelialization. Additionally, RUTG demonstrates beneficial anti-inflammatory and antioxidant properties, effectively remodeling the local microenvironment. In vivo studies using an oral ulcer model further confirm that RUTG could significantly accelerate the re-epithelialization process, shorten the ulcer healing cycle, and achieve functional tissue reconstruction. Collectively, this carrier-free hydrogel system, which integrates gene programming with microenvironment modulation to achieve efficient re-epithelialization, holds promise for introducing novel approaches to the treatment of oral ulcers.

Keywords: EGR1 ; oral ulcer ; re-epithelialization ; rutin ; self-assembly

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Product Details of FR 180204

CAS No. :865362-74-9
Formula : C18H13N7
M.W : 327.34
SMILES Code : NC1=NNC2=NN=C(C3=C4C=CC=CN4N=C3C5=CC=CC=C5)C=C21
Synonyms :
ERK Inhibitor II
MDL No. :MFCD14585805
InChI Key :XVECMUKVOMUNLE-UHFFFAOYSA-N
Pubchem ID :11493598

Safety of FR 180204

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P264-P270-P301+P312-P330-P501

Related Pathways of FR 180204

MAPK

Isoform Comparison

Biological Activity

Target
  • ERK2

    ERK2, Ki:0.14 μM

  • ERK1

    ERK1, Ki:0.31 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
KRAS-mutant NSCLC cells 10 μM 6 hours To investigate the effect of FR180204 on EREG expression, results showed that FR180204 significantly downregulated EREG expression PMC4451140
astrocytes 2 µg/mL 1 hour Inhibit the Erk pathway and reduce the expression of versican in inflaμMation-induced astrocytes PMC10479858
RAW 264.7 cells 50 µM 1 h and 24 h To investigate the effects of FR180204 on osteoclast hallmarks expression, results showed that FR180204 significantly reduced the expression of NFATc1, Acp5/TRAP, μMP9, and DC-STAMP. PMC7728313
NSTS-47 cells 1 µM 6 days FR180204 did not significantly affect the proliferative activity of NSTS-47 cells. PMC6163232

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice spinal cord injury model intraperitoneal injection 5 nmol Once every 2-3 days, for four times Inhibit the Erk pathway, reduce the expression of versican after spinal cord injury, and promote axonal regeneration PMC10479858
Lycopersicon esculentum, Vicia faba, Pisum sativum, Lupinus luteus Root meristem cells Immersion 10 mg/kg daily for 25 days To investigate the effect of FR180204 on mitosis in root meristem cells of different plant species. Results showed that FR180204 had the most significant effect on mitosis in Lycopersicon esculentum, leading to an increase in the number of prometaphase cells and a decrease in the number of telophase cells. PMC4427623
Mice Pak-1 knockout mice Intraperitoneal injection 30 µg/kg once every 2 days for 7 days FR180204, as a selective inhibitor of Erk1/2, attenuated ISO-induced cardiac hypertrophy in Pak-1-KO mice PMC3208757

Protocol

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1 mM

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3.05mL

0.61mL

0.31mL

15.27mL

3.05mL

1.53mL

30.55mL

6.11mL

3.05mL

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