ERK5-IN-2

SKU: orb1301715

Description

ERK5-IN-2 is a selective, orally bioavailable ERK5 inhibitor with sub-micromolar potency, exhibiting IC50 values of 0.82 μM against ERK5 and 3 μM for the ERK5-MEF2D complex. This tool compound is used in biochemical and cellular assays to investigate the role of ERK5 signaling in cancer, inflammation, and cardiovascular disease research.

Research Area

Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1888305-96-1
• MW: 388.19
• Purity: 99.01% (May vary between batches)
• Formula: C₁₇H₁₁BrFN₃O₂
• SMILES: Fc1cccc(Br)c1C(=O)c1c[nH]c(c1)C(=O)Nc1cccnc1
• Target: ERK
• Solubility: DMSO:10 mg/mL (25.76 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.58 mM)

Bioactivity

• Target IC50:
  ERK5 MEF2D:3 μM|ERK5:0.82 μM
• In Vivo:
  ERK5-IN-2 (compound 46) (p.o.; 100 mg/kg; CD1 mice for 7 days and CD1 nude (nu/nu) mice for 10 days) has an anti-angiogenic effect and low concentrations of haemoglobin.ERK5-IN-2 (i.v. or p.o.; 10 mg/kg for 0.083-24 hours) exhibits low intrinsic clearance and has high flux and a low efflux ratio (ER) in a caco-2 cell permeability assay in both human and mouse.
  Read more...

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, ERK, ERK5IN2, ERK-5-IN-2, ERK5-IN-2, ERK5, ERK5 IN 2, Extracellular signal regulated kinases, Inhibitor

Compound Identifiers

PubChem CID

118959080