ERK5-IN-1

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Cat.No. 5393 - ERK5-IN-1 | C36H46N8O3 | CAS No. 1435488-37-1
Description: Potent and selective ERK5 inhibitor
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% (HPLC)
Datasheet
Citations
Literature
Pathways

Biological Activity

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.

Licensing Information

Sold under license from Dana-Farber Cancer Institute.

Compound Libraries

ERK5-IN-1 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 638.8
Formula C36H46N8O3
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1435488-37-1
PubChem ID 71604307
InChI Key XVBGRTMNFNMINE-UHFFFAOYSA-N
Smiles O=C2N(C)C3=C(N=C(NC5=CC=C(C(N6CCC(N7CCN(C)CC7)CC6)=O)C=C5OCC)N=C3)N(C4CCCC4)C1=CC=CC=C12

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 63.88 100
ethanol 63.88 100

Preparing Stock Solutions

The following data is based on the product molecular weight 638.8. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.57 mL 7.83 mL 15.65 mL
5 mM 0.31 mL 1.57 mL 3.13 mL
10 mM 0.16 mL 0.78 mL 1.57 mL
50 mM 0.03 mL 0.16 mL 0.31 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Deng et al (2013) 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. 70 758 PMID: 24239623

Elkins et al (2013) X-ray crystal structure of ERK5 (MAPK7) in complex with a specific inhibitor. J.Med.Chem. 56 4413 PMID: 23656407


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Keywords: ERK5-IN-1, supplier, potent, selective, ERK5, extracellular, regulated, kinases, MAPK7, inhibitors, inhibits, ERK, ERK, Tocris Bioscience

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MAPK Signaling

MAPK Signaling Scientific Review

MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.

Pathways for ERK5-IN-1

MAPK

MAPK Signaling Pathway

The mitogen-activated protein kinase pathway evokes an intracellular signaling cascade in response to extracellular stimuli such as heat and stress. It can influence cell division, metabolism and survival.