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Submit ReviewERK5-IN-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)
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.
Product Datasheets for ERK5-IN-1
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
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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
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
