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ERK5-IN-1

Cat. No. 5393 1 Citation Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
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 (1)
Reviews
Literature (1)
Pathways (1)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for ERK5-IN-1

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.

Licensing Information

Sold under license from Dana-Farber Cancer Institute.

Compound Libraries for ERK5-IN-1

ERK5-IN-1 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.

Technical Data for ERK5-IN-1

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for ERK5-IN-1

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

Preparing Stock Solutions for ERK5-IN-1

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

Select a batch to recalculate based on the batch molecular weight:
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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References for ERK5-IN-1

References are publications that support the biological activity of the product.

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

If you know of a relevant reference for ERK5-IN-1, please let us know.

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Keywords: ERK5-IN-1, ERK5-IN-1 supplier, potent, selective, ERK5, extracellular, regulated, kinases, MAPK7, inhibitors, inhibits, ERK, 5393, Tocris Bioscience

1 Citation for ERK5-IN-1

Citations are publications that use Tocris products. Selected citations for ERK5-IN-1 include:

C David et al (2019) Identification of Novel RAS Signaling Therapeutic Vulnerabilities in Diffuse Intrinsic Pontine Gliomas. Cancer Res 79 4026-4041 PMID: 31201162

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

MAPK Signaling Scientific Review

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 Signaling Pathway

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.