DEL-22379

Catalog No.S7921

DEL-22379 Chemical Structure

Molecular Weight(MW): 444.53

DEL-22379 is a water-soluble ERK dimerization inhibitor with IC50 of ∼0.5 μM.

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Choose Selective ERK Inhibitors

Biological Activity

Description DEL-22379 is a water-soluble ERK dimerization inhibitor with IC50 of ∼0.5 μM.
Targets
ERK [1]
(in HEK293 cells)
0.5 μM
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. [1]

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). [1]

Protocol

Kinase Assay:[1]
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ERK dimerization assay:

Compound screening is performed in HEK293T cells treated with the potential inhibitors (10 μM) for 30 min before EGF stimulation. Cellular lysates are tested for ERK dimerization by native PAGE and p-ERK evaluation of the potential positives. In vitro ERK dimerization is assayed using GST-MEK1 ΔN EE purified from bacteria, bound to glutathione sepharose beads, and incubated with 25 μg/ml of purified His-ERK2 plus increasing concentrations of DEL-22379. Western blotting, kinase assays, and luciferase assays are also performed. In silico docking of the DEL-22379 compound is carried out with the modeling tools provided by the OpenEye package (v. 2.1).
Cell Research:[1]
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  • Cell lines: A panel of human cell lines harboring mutant BRAF (V600E) or RAS (Q61L or G12V)
  • Concentrations: ~10 μM
  • Incubation Time: 48 h
  • Method: 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)
Animal Research:[1]
+ Expand
  • Animal Models: Nude mice bearing A375 (BRAF mutant), CHL (WT/WT) or HCT116 (KRAS mutant) tumors
  • Formulation: 1% DMSO
  • Dosages: 15 mg/kg, bid
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 89 mg/mL (200.21 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 444.53
Formula

C26H28N4O3

CAS No. 181223-80-3
Storage powder
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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ERK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID