Home MAPK ERK inhibitor DEL-22379 For research use only.

DEL-22379

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

DEL-22379 Chemical Structure

DEL-22379 Chemical Structure

CAS: 181223-80-3

Selleck's DEL-22379 has been cited by 3 publications

Purity & Quality Control

Batch: S792101 DMSO] 89 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.94%
99.94

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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
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]
Kinase Assay 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 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.
In Vivo
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]
Animal Research Animal Models Nude mice bearing A375 (BRAF mutant), CHL (WT/WT) or HCT116 (KRAS mutant) tumors
Dosages 15 mg/kg, bid
Administration i.p.

Chemical lnformation & Solubility

Molecular Weight 444.53 Formula

C26H28N4O3
CAS No. 181223-80-3 SDF --
Smiles COC1=CC2=C(C=C1)NC=C2C=C3C4=C(C=CC(=C4)NC(=O)CCN5CCCCC5)NC3=O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 89 mg/mL ( (200.21 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

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

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