In Vivo (Add solvents to the product individually and in order.)
Homogeneous suspension
CMC-NA
≥5mg/ml
Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
Biological Activity
Description
DEL-22379 is a water-soluble ERK dimerization inhibitor with an IC50 of ~0.5 μM.
Targets
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 harbouring mutant BRAF (V600E) or RAS (Q61L or G12V), this compound shows potent anti-proliferative effects, and induces apoptosis.
In Vivo
DEL-22379 (15 mg/kg, i.p.) prevents tumour growth and metastasis in mice bearing A375 (BRAF mutant) and HCT116 (KRAS mutant) tumours, but this compound fails to prevent the formation of tumours in mice injected with CHL cells (WT/WT).
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 modelling tools provided by the OpenEye package (v. 2.1).
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.
ERK phosphorylation disrupts the intramolecular interaction of capicua to promote cytoplasmic translocation of capicua and tumor growth
[ Front Mol Biosci, 2022, 9:1030725]
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
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