Powder: -20°C for 3 years | In solvent: -80°C for 1 year
ERK5-IN-1 is a potent ERK5 inhibitor (IC50: 87 nM). It also inhibits LRRK2[G2019S] (IC50: 26 nM).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 48.00 | |
5 mg | In stock | $ 122.00 | |
10 mg | In stock | $ 172.00 | |
25 mg | In stock | $ 297.00 | |
50 mg | In stock | $ 513.00 | |
100 mg | In stock | $ 728.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 123.00 |
Description | ERK5-IN-1 is a potent ERK5 inhibitor (IC50: 87 nM). It also inhibits LRRK2[G2019S] (IC50: 26 nM). |
Targets&IC50 | ERK5:87 nM (cell free) |
In vitro | ERK5-IN-1 (Compound 5) inhibits EGF-stimulated autophosphorylation of ERK5 in HeLa cells (EC50: 0.19 μM). |
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. |
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. |
Molecular Weight | 459.54 |
Formula | C25H29N7O2 |
CAS No. | 1234479-76-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 25 mg/mL (54.4 mM)
You can also refer to dose conversion for different animals. More
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ERK5-IN-1 1234479-76-5 MAPK ERK ERK5 IN 1 Inhibitor ERK-5-IN-1 Extracellular signal regulated kinases ERK5IN1 inhibit inhibitor