Home MAPK ERK inhibitor DEL-22379

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DEL-22379 ERK inhibitor

Cat.No.S7921

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

Chemical Structure

Molecular Weight: 444.53

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 89 mg/mL (200.21 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 444.53 Formula

C26H28N4O3

 Storage (From the date of receipt)
CAS No. 181223-80-3 -- Storage of Stock Solutions

Synonyms N/A Smiles COC1=CC2=C(C=C1)NC=C2C=C3C4=C(C=CC(=C4)NC(=O)CCN5CCCCC5)NC3=O

Mechanism of Action

Targets/IC50/Ki
ERK
(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), this compound shows potent anti-proliferative effects, and induces apoptosis.
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 this compound. Western blotting, kinase assays, and luciferase assays are also performed. In silico docking of this compound is carried out with the modeling tools provided by the OpenEye package (v. 2.1).
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 this compound fails to prevent the formation of tumors in mice injected with CHL cells (WT/WT).
References

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