ERK5-IN-1

SKU: orb1302017

Description

ERK5-IN-1 is a potent, dual-activity small molecule inhibitor, demonstrating high potency against ERK5 (IC50 = 87 nM) and the LRRK2[G2019S] mutant (IC50 = 26 nM). This compound is a valuable chemical probe for investigating the roles of these kinases in cancer and neurodegenerative disease research, both in cellular and biochemical studies.

Research Area

Signal Transduction

Key Properties

• CAS Number: 1234479-76-5
• MW: 459.54
• Purity: 99.42%
• Formula: C₂₅H₂₉N₇O₂
• SMILES: COc1cc(ccc1Nc1ncc2N(C)C(=O)c3ccccc3N(C)c2n1)N1CCN(C)CC1
• Target: ERK
• Solubility: DMSO:25 mg/mL (54.4 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.35 mM)

Bioactivity

• Target IC50:
  ERK5:87 nM (cell free)|LRRK2 (G2019S):26 nM
• In Vitro:
  ERK5-IN-1 (Compound 5) inhibits EGF-stimulated autophosphorylation of ERK5 in HeLa cells [EC50: 0.19 μM].
• Cell Research:
  HeLa cells were serum starved overnight followed by treatment with inhibitors for 1 h. Cells were then stimulated with EGF (20 ng/mL) for 17 min and harvested in RIPA buffer (1× PBS, 1% NP40, 0.5% sodium deoxycholate, 0.1% SDS, 0.1 mg/ml PMSF and 1 mM sodium orthovanadate). Proteins from total cell lysates were resolved by 6% sodium dodecyl sulfate (SDS)-poly-acrylamide gel electrophoresis (PAGE), transferred to nitrocellulose membrane, blocked in 5% nonfat milk, and blotted with anti-ERK5 antibody.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Extracellular signal regulated kinases, ERK, ERK5 IN 1, ERK5, ERK5IN1, ERK-5-IN-1, ERK5-IN-1, Inhibitor

Compound Identifiers

PubChem CID

46844147