DEL-22379

SKU: orb1300438

Description

DEL-22379 is a cell-permeable, water-soluble small molecule that potently inhibits ERK dimerization with an IC50 of approximately 0.5 µM. It is a valuable research tool for studying MAPK/ERK signaling in cancer models, applicable in both cellular and in vivo studies to investigate pathways driving tumor proliferation.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 181223-80-3
• MW: 444.53
• Purity: >99.99% (May vary between batches)
• Formula: C₂₆H₂₈N₄O₃
• SMILES: COc1ccc2[nH]cc(C=C3C(=O)Nc4ccc(NC(=O)CCN5CCCCC5)cc34)c2c1
• Target: Apoptosis,ERK
• Solubility: DMSO:22.2 mg/mL (49.94 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.5 mM)

Bioactivity

• Target IC50:
  ERK:0.5 μM
• In Vivo:
  DEL-22379 (15 mg/kg, i.p.) prevents tumor growth and metastasis in mice bearing A375 (BRAF mutant) and HCT116 (KRAS mutant) tumors, but fails to prevent the formation of tumors in mice injected with CHL cells (WT/WT).
• In Vitro:
  DEL-22379 inhibits ERK dimerization without affecting its phosphorylation. In a panel of human cell lines harboring mutant BRAF (V600E) or RAS (Q61L or G12V), DEL-22379 shows potent anti-proliferative effects, and induces apoptosis.
• Cell Research:
  Cellular proliferation is analyzed by Alamar blue assays. Briefly, Cells are plated in 96-well plates at a density of 1000-2000 cells per well. Cells are treated with drug concentrations prepared by serial dilution ranging from 0.1 nM to 10 μM. 48 hr after drug treatment cells are exposed to Alamar Blue and the colorimetric change is measured at 570 and 600 nm. GI50 is estimated by nonlinear regression using GraphPad5 Prism Software.(Only for Reference)

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

DEL 22379, DEL22379, DEL-22379, Apoptosis, Inhibitor, inhibit, ERK, Extracellular signal regulated kinases

Compound Identifiers

PubChem CID

69726164