ERK5-IN-1

Modify Date: 2024-01-10 12:41:03

ERK5-IN-1 Structure
ERK5-IN-1 structure
Common Name ERK5-IN-1
CAS Number 1234479-76-5 Molecular Weight 459.54300
Density N/A Boiling Point N/A
Molecular Formula C25H29N7O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of ERK5-IN-1


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.

 Names

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
Synonym More Synonyms

 ERK5-IN-1 Biological Activity

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.
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

[1]. Deng X, et al. Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones. Eur J Med Chem. 2013;70:758-767.

 Chemical & Physical Properties

Molecular Formula C25H29N7O2
Molecular Weight 459.54300
Exact Mass 459.23800
PSA 80.45000
LogP 2.96230
Storage condition 2-8℃

 Synonyms

lrrk2-in-1
ERK5-IN-1
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