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Application: Study enzyme kinetics and screen small molecule inhibitors for drug discovery and high throughput screening (HTS) applications.
Background: MLK4 (mixed-lineage kinase 4) is a member of the serine/threonine kinase MLK family of proteins. It is involved in DNA damage, and it is often mutated or overexpressed in several types of cancer. It has been described as tumor suppressor and oncogene in different studies. In ovarian cancer it inhibits the MAPK (mitogen-activated protein kinase) signaling pathway and thus reduces the invasion potential of the cancer cells, while in melanoma it was described to phosphorylate MEK1 (MAP kinase kinase 1) and MKK4/7 (MAK kinase 4) and activate ERK and JNK (c-Jun N-terminal kinase) pathways. In triple negative breast cancer (TNBC) it can contribute to the development of drug resistance. In a cellular model and in a xenograft model, the knockdown of MLK4 increased the sensitivity of cells to doxorubicin and etoposide. The use of inhibitors in combinatory therapy may thus present a new avenue of cancer therapy.
Contraindications: The final concentration of DMSO in the assay should not exceed 1%.
Description: The Chemi-Verse™ MLK4 Kinase Assay Kit is designed to measure MLK4 (Mixed-Lineage Kinase 4) 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 MLK4, kinase substrate, ATP, and kinase assay buffer for 100 enzyme reactions.
Storage Stability: This assay kit will perform optimally for up to 6 months from date of receipt when the materials are stored as directed.
Uniprot: Q5TCX8
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
References: Mehlich D., et al., 2921 Cell Death Dis 12(12):1111.
Gong M., et al., 2023 PLoS One 18(8):e0290462.
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