1234479-76-5
1234479-76-5 structure
- Name: ERK5-IN-1
- Chemical Name: 2-{[2-Methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino}-5,11-dimeth yl-5,11-dihydro-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one
- CAS Number: 1234479-76-5
- Molecular Formula: C25H29N7O2
- Molecular Weight: 459.54300
- Catalog: Research Areas Cancer
- Create Date: 2016-11-17 06:57:13
- Modify Date: 2024-01-10 12:41:03
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ERK5-IN-1 is a potent ERK5 inhibitor with an IC50 of 87±7 nM. ERK5-IN-1 also inhibits LRRK2[G2019S] with an IC50 of 26 nM.
| Name | 2-{[2-Methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino}-5,11-dimeth yl-5,11-dihydro-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one |
|---|---|
| Synonyms |
lrrk2-in-1
ERK5-IN-1 |
| Description | ERK5-IN-1 is a potent ERK5 inhibitor with an IC50 of 87±7 nM. ERK5-IN-1 also inhibits LRRK2[G2019S] with an IC50 of 26 nM. |
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| Related Catalog | |
| Target |
ERK5:87 nM (IC50) LRRK2[G2019S]:26 nM (IC50) |
| In Vitro | ERK5-IN-1 (Compound 5) exhibits a cellular EC50 for inhibiting epidermal growth factor (EGF) induced ERK5 autophosphorylation of 0.19±0.04 μM[1]. |
| Kinase Assay | Kinase activity is 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 are carried out for 20 min at 30°C, terminated by applying the reaction mixture onto p81 paper and the incorporated radioactivity measured[1]. |
| References |
| Molecular Formula | C25H29N7O2 |
|---|---|
| Molecular Weight | 459.54300 |
| Exact Mass | 459.23800 |
| PSA | 80.45000 |
| LogP | 2.96230 |
| Storage condition | 2-8℃ |
| Precursor 4 | |
|---|---|
| DownStream 0 | |