ERK5-IN-1

Name: ERK5-IN-1
Brand: Tocris Bioscience
SKU: 5393

Tocris Bioscience, part of Bio-Techne | Catalog # 5393

Citations (1)

COA / SDS

Potent and selective ERK5 inhibitor

Key Product Details

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)
Molecular Weight:	638.8

View Full Technical Details for ERK5-IN-1

Technical Data
Citations

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 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.

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.

Elkins X-ray crystal structure of ERK5 (MAPK7) in complex with a specific inhibitor. J.Med.Chem. 2013 PMID: 23656407
Deng 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. 2013 PMID: 24239623