Chemi-Verse™ PIM1 Kinase Assay Kit

Catalog #

82525

$535 *

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™ PIM1 Kinase Assay Kit is designed to measure PIM1 (Proviral Integration of Molony murine leukemia virus 1) serine/threonine 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 PIM1, kinase substrate, ATP, and kinase assay buffer for 100 enzyme reactions.

Need us to run inhibitor screens or profile your compounds against PIM1? Check out our Kinase Screening and Profiling Service.

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Synonyms

serine/threonine-protein kinase PIM1, Proviral Integration of Molony murine leukemia virus 1

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Product Data Gallery

Inhibition of PIM1 kinase activity by AZD1208.

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
41107	PIM1, GST-Tag*	10 µg	-80°C
79334	5x Kinase Buffer 1	1.5 ml	-20°C
79686	500 µM ATP	50 µl	-20°C
79884	S6Ktide (10 mg/ml)	50 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.

UniProt #

P11309

Background

PIM kinases (Proviral Integration of Molony murine leukemia virus), PIM1, PIM2 and PIM3, are a family of serine/threonine protein kinases that play crucial roles in cell survival, proliferation, and drug resistance. PIM kinases are overexpressed in several tumors and promote growth and survival of malignant cells through cell cycle regulation and/or inhibition of apoptosis. PIM1 has two isoforms that differ in length and localization, with the short isoform being found in the nucleus and the longer one in the plasma membrane. This protein is constitutively active, stabilized by phosphorylation. It is normally found in the thymus, spleen, bone marrow, fetal liver, and lymphocytes. It sits at a crosspoint of multiple pathways, being the effector in response to several cytokine activated pathways and acting on several proteins. In T cells, PIM1 enables cells to bypass the TCR (T cell receptor) checkpoint and enhance NFAT (nuclear factor of activated T-cells) activity and IL-2 secretion. High levels of PIM1 can be found in many cancer types, such as hematological disorders and prostate cancer. In triple-negative breast cancer, PIM-1 is a coactivator of Myc, phosphorylates histone H3 leading to stimulation of RNA polymerase II binding, and increased c-Myc driven transcription. The use of PIM1 inhibitors in cancer treatment, as monotherapy, has focused on using ATP competitive or mimetic molecules. The development of new inhibitors to be used in mono- or combinatory therapy will continue to expand the repertoire of tools available in cancer therapy.

References

Arrouchi H., et al., 2019 Bioinformation 15(1): 40-45.
Liu Z., et al., 2020 Am J Cancer Res 10(12): 4085-4097.
Jeyapal G. P., et al., 2018 Anticancer Agents Med Chem, 18(8): 1100-1114.
Asati V., et al., 2019 Eur J Med Chem., 172: 95-108.

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

Cancer Therapy Target

Regulatory Status

Research Use Only

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Chemi-Verse™ PIM1 Kinase Assay Kit

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