| Name | ERK5-IN-1 |
| Description | ERK5-IN-1 is a potent ERK5 inhibitor (IC50: 87 nM) and also inhibits LRRK2[G2019S] (IC50: 26 nM). |
| Cell Research | HeLa cells were serum starved overnight followed by treatment with inhibitors for 1 h. Cells were then stimulated with EGF (20 ng/mL) for 17 min and harvested in RIPA buffer (1× PBS, 1% NP40, 0.5% sodium deoxycholate, 0.1% SDS, 0.1 mg/ml PMSF and 1 mM sodium orthovanadate). Proteins from total cell lysates were resolved by 6% sodium dodecyl sulfate (SDS)-poly-acrylamide gel electrophoresis (PAGE), transferred to nitrocellulose membrane, blocked in 5% nonfat milk, and blotted with anti-ERK5 antibody. |
| Kinase Assay | Kinase activity was determined in an assay volume of 40 μL in kinase buffer (50 mM Tris–HCl, pH 7.5, 0.1 mM EGTA, 1 mM 2-mercaptoethanol) containing 200 ng of pure active ERK5 and the indicated amount of inhibitor. Reaction started by adding 10 mM magnesium acetate, and 50 μM [γ-32P]-ATP (500 cpm/pmol) and 250 μM PIMtide (ARKKRRHPSGPPTA) as substrates. Assays were carried out for 20 min at 30 °C, terminated by applying the reaction mixture onto p81 paper and the incorporated radioactivity measured as described previously. |
| In vitro | ERK5-IN-1 (Compound 5) inhibits EGF-stimulated autophosphorylation of ERK5 in HeLa cells [EC50: 0.19 μM]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.35 mM), Sonication is recommended.
DMSO : 25 mg/mL (54.4 mM), Sonication is recommended.
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| Keywords | Inhibitor | inhibit | Extracellular signal regulated kinases | ERK5-IN-1 | ERK-5-IN-1 | ERK5IN1 | ERK5 IN 1 | ERK5 | ERK |
| Inhibitors Related | TBHQ | Urea | Gum arabic | L-Cysteine | β-Glycerophosphate disodium salt pentahydrate | 4-Methylbenzylidene camphor | Lactose | Astragaloside IV | Tauroursodeoxycholate | Propoxur | Gluconate Calcium | β-Glycerophosphate disodium salt hydrate |
| Related Compound Libraries | Anti-Colorectal Cancer Compound Library | Bioactive Compound Library | Pain-Related Compound Library | Kinase Inhibitor Library | Anti-Ovarian Cancer Compound Library | Inhibitor Library | Anti-Prostate Cancer Compound Library | Immunology/Inflammation Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Liver Cancer Compound Library |
United States
