Chemi-Verse™ MEK1 Kinase Assay Kit

Catalog #

82100

$750 *

Size: 96 reactions

Qty

Bulk/Custom

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*US Pricing only. For international pricing, please contact your local distributor.

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Description

The Chemi-Verse™ MEK1 Kinase Assay Kit is a luminescent assay designed to measure MEK1 (dual specificity mitogen-activated protein kinase kinase 1) kinase activity for screening and profiling applications using ADP-Glo™ as a detection reagent. The assay kit comes in a convenient 96-well format, with enough purified recombinant MEK1 kinase, kinase substrate, ATP, and kinase assay buffer for 100 enzyme reactions.

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Product Data Gallery

Inhibition of MEK1 kinase Activity by GDC-0623.

Product Info

Storage and Usage

Citations

Assay Kit Format

Luminescent

Materials Required But Not Supplied

ADP-Glo™ Kinase Assay (Promega #V6930)
DTT (Dithiothreitol), 1M, optional
Microplate reader capable of reading luminescence
Adjustable micropipettor and sterile tips
30°C incubator

Format

Catalog #	Name	Amount	Storage
40123	MEK1, GST-Tag*	2.5 µg	-80°C
79334	5x Kinase Buffer	1.5 ml	-20°C
79686	500 µM ATP	50 µl	-20°C
	CHKtide (1 mg/ml)	250 µl	-20°C
79696	White 96-well plate	1	Room Temp

*The concentration of the protein is lot-specific and will be indicated on the tube.

Background

MEK1, also known as dual specificity mitogen-activated protein kinase kinase 1 or MAP2K1, is part of dual-specificity protein kinase family. MEK1 activates ERKs (extracellular signal-regulated kinases or MAPs) in response to several extra- and intracellular signals, and it is thus involved in cell proliferation and differentiation via regulation of transcription. MEK1 can be seen as the gatekeeper of ERK1/2 activity, offering a unique opportunity for inhibitors to act on all the downstream members of the ERK pathway. MEK1/2 has a very unique hydrophobic pocket which allows for binding of non-ATP competitive allosteric inhibitors, disturbing the formation of RAF (proto-oncogene serine/threonine-protein kinase)-MEK complexes or MEK phosphorylation. Inhibitors for MEK1 are currently used in combination with B-RAF1 inhibitors for the treatment of B-RAF-mutant melanoma. Further studies are required to design inhibitors that act mainly in abnormal tissues, as MEK1 is also expressed in normal cells, and to bypass resistance mechanisms.

References

Caunt C., et al., 2015 Nature Reviews Cancer 15: 577-592.

Storage/Stability

This assay kit will perform optimally for up to 6 months from date of receipt when the materials are stored as directed.

Applications

Study enzyme kinetics and screen small molecule inhibitors for drug discovery and high throughput screening (HTS) applications.

Shipping Temperature

-80°C

Notes

Troubleshooting Guide
Visit bpsbioscience.com/assay-kits-faq for detailed troubleshooting instructions. For all further questions, please email [email protected]

Contraindications

The final concentration of DMSO in the assay should not exceed 1%.

Warnings

Avoid freeze/thaw cycles

Disclaimers and Limitations

BPS Bioscience assay kits are validated using the listed components according to our specific protocol. Any deviations to kit components or protocols, such as using different proteins, cell/tissue lysates, or buffers (including using the same component from other commercial sources) will void any warranties on the performance of the assay kit and is not recommended.

End-users should immediately report any issues to [email protected] upon receipt of the kit, such as missing components, damaged vials, no dry ice, etc.

Scientific Category

Kinases

Regulatory Status

Research Use Only

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Chemi-Verse™ MEK1 Kinase Assay Kit

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