ERK5-IN-1

• Supplier: Tocris Bioscience
• Catalog: 3970
• Prices: $245.00, $1,005.00
• Sizes: 10 mg, 50 mg
• Function Type: Inhibitor
• Cas Number: 1435488-37-1
• 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
• Formula: C36H46N8O3
• Molecular Weight: 638.8
• Purity: >98 %
• Description: Potent and selective ERK5 inhibitor; inhibits EGFR-induced ERK5 autophosphorylation (EC 50 = 90 nM) and ERK5 enzymatic activity (IC 50 = 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.

Product References

Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 - Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2

Deng X, Elkins JM, Zhang J, Yang Q, Erazo T, Gomez N, Choi HG, Wang J, Dzamko N, Lee JD, Sim T, Kim N, Alessi DR, Lizcano JM, Knapp S, Gray NS. Eur J Med Chem. 2013;70:758-67.

X-ray crystal structure of ERK5 (MAPK7) in complex with a specific inhibitor. - X-ray crystal structure of ERK5 (MAPK7) in complex with a specific inhibitor.

Elkins JM, Wang J, Deng X, Pattison MJ, Arthur JS, Erazo T, Gomez N, Lizcano JM, Gray NS, Knapp S. J Med Chem. 2013 Jun 13;56(11):4413-21.