[CAS NO. 865362-74-9]  FR 180204

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PRODUCTS SPECIFICATIONS [865362-74-9]

Store
Catalog
SLK-S7524
Brand
Selleck
CAS
865362-74-9

DESCRIPTION [865362-74-9]

Overview

MDLMFCD14585805
Molecular Weight327.34
Molecular FormulaC18 H13 N7
SMILESNC1=NNC2=NN=C(C3=C4C=CC=CN4N=C3C5=CC=CC=C5)C=C21

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM3.0549 mL15.2746 mL30.5493 mL
5 mM0.6110 mL3.0549 mL6.1099 mL
10 mM0.3055 mL1.5275 mL3.0549 mL
50 mM0.0611 mL0.3055 mL0.6110 mL

Description

FR 180204 is an ATP-competitive, selective inhibitor with of 0.31 μM and 0.14 μM for ERK1 And ERK2, respectively. It is 30-fold less potent against the related kinase p38α and failed to inhibit any kinases(MEK1, MKK4, IKKα, PKCα, Src, Syc, and PDGFα) at less than 30 μM.

Features

ERK1/ERK2-selective inhibitor

Targets

ERK2 [1]
(Cell-free assay)
ERK1 [1]
( Cell-free assay)
0.14 μM(Ki)0.31 μM(Ki)

In vitro

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

In vivo

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