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DEL-22379

Catalog No. T6818 CAS 181223-80-3

Synonyms: DEL22379

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

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

DEL-22379, CAS 181223-80-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 30.00
2 mg	In stock	$ 43.00
5 mg	In stock	$ 68.00
10 mg	In stock	$ 126.00
25 mg	In stock	$ 230.00
50 mg	In stock	$ 369.00
100 mg	In stock	$ 549.00
1 mL * 10 mM (in DMSO)	In stock	$ 74.00

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Purity: 100%

Purity: 99.3%

Biological Description

Chemical Properties

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Description	DEL-22379 is a water-soluble ERK dimerization inhibitor with IC50 of ～0.5 μM.
Targets&IC50	ERK: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]
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	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)

Synonyms	DEL22379
Molecular Weight	444.53
Formula	C26H28N4O3
CAS No.	181223-80-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 22.2 mg/mL (50 mM)

References and Literature

1. Herrero A, et al. Cancer Cell. 2015, 28(2), 170-182.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Inhibitor Library Covalent Inhibitor Library Bioactive Compounds Library Max Anti-COVID-19 Compound Library Anti-Obesity Compound Library Anti-Prostate Cancer Compound Library Stem Cell Differentiation Compound Library Anti-Colorectal Cancer Compound Library Neural Regeneration Compound Library

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Keywords

DEL-22379 181223-80-3 Apoptosis MAPK ERK DEL22379 Inhibitor Extracellular signal regulated kinases inhibit DEL 22379 inhibitor

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