ERK5-IN-1
Chemical Name: 11-Cyclopentyl-2-[[2-ethoxy-4-[[4-(4-methyl-1-piperazinyl)-1-piperidinyl]carbonyl]phenyl]amino]-5,11-dihydro-5-methyl-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one
Purity: ≥98%
Biological Activity
ERK5-IN-1 is a potent and selective ERK5 inhibitor; inhibits EGFR-induced ERK5 autophosphorylation (EC50 = 90 nM) and ERK5 enzymatic activity (IC50 = 162 nM). Exhibits at least 30-fold selectivity for ERK5 over LRRK2 in a cell based assay. Also selective for ERK5 over a panel of other kinases. Orally bioavailable.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
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Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones.
Deng et al.
Eur.J.Med.Chem., 2013;70:758 -
X-ray crystal structure of ERK5 (MAPK7) in complex with a specific inhibitor.
Elkins et al.
J.Med.Chem., 2013;56:4413
Product Datasheets
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Citation for ERK5-IN-1
The citations listed below are publications that use Tocris products. Selected citations for ERK5-IN-1 include:
1 Citation: Showing 1 - 1
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Identification of Novel RAS Signaling Therapeutic Vulnerabilities in Diffuse Intrinsic Pontine Gliomas.
Authors: C David Et al.
Cancer Res 2019;79:4026-4041
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