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ERK5-IN-2

ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively. ERK5-IN-2 does not interact with the BRD4 bromodomain. ERK5-IN-2 suppresses both tumor xenograft growth and basic fibroblast growth factor (bFGF) driven Matrigel plug angiogenesis[1].

Product Specifications

CAS Number

[1888305-96-1]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

ERK

Type

Reference compound

Related Pathways

MAPK/ERK Pathway; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/erk5-in-2.html

Purity

98.96

Solubility

DMSO : 250 mg/mL (ultrasonic)

Smiles

FC1=CC=CC(Br)=C1C(C2=CNC(C(NC3=CC=CN=C3)=O)=C2)=O

Molecular Formula

C17H11BrFN3O2

Molecular Weight

388.19

Precautions

H302, H315, H319, H335

References & Citations

[1]Myers SM, et al. Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38α and BRD4. Eur J Med Chem. 2019 May 25;178:530-543.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, protect from light)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

ERK5

Available Sizes

Curated Selection

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