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Applications: Study complex formation and screen compounds that block the binding of MLL1 to WDR5 for drug discovery and high throughput screening (HTS) applications.
Background: Protein Mixed Lineage Leukemia-1 (MLL1, also known as KMT2A) belongs to the SET1/MLL family which consists of six (MLL1-4/KMT2A-2D, SET1A/KMT2F, and SET1B/KMT2G) major methyltransferases in mammals. MLL1 is a histone-H3 lysine-4 (H3K4) methyltransferase that promotes H3K4 mono-/di-/tri-methylation, a conserved trait of euchromatin associated with transcriptional activation. MLL1 is a master regulator for the transcription of many important genes including homeobox (Hox), which has been implicated in hematopoiesis and embryonic development. MLL1 forms a complex with RbBP5 (retinoblastoma-binding protein 5), ASH2L (Absent, small, homeotic disks-2-like), WDR5 (WD40 repeat-containing protein 5), and DPY30 (DumPY protein 30) to catalyze tri-methylation of H3K4. WDR5 represents a therapeutically exploitable target for cancer treatment as it plays a crucial role in MLL1 complex assembly and disassembly. WDR5 has two protein interaction sites: the WDR5-interacting (WIN) binding site and the WDR5-binding-motif (WBM) site. MLL1 forms the complex via WIN binding site, while RbBP5 is bound to WBM site, which is also the site for MYC oncoproteins interaction. The addition of inhibitors that competitively bind to WIN or WBM sites has been shown to disrupt MLL activity as well as displace MYC from chromatin and therefore disabling its tumorigenic function.
Contraindications: The MLL1 (KMT2A): WDR5 Binding Chemiluminescent Assay Kit is compatible with up to 1% final DMSO concentration.
Description: The MLL1 (KMT2A): WDR5 Binding Chemiluminescent Assay Kit is an ELISA-based assay designed to measure the binding between MLL1 (mixed lineage leukemia protein-1, also known as KMT2A) and WDR5 (WD40 repeat-containing protein 5) for screening and profiling applications. The MLL1 (KMT2A): WDR5 Binding Chemiluminescent Assay Kit comes with enough purified MLL1 (amino acids 3745-end) and WDR5 proteins, primary and secondary antibody, assay buffer, and detection reagent for 100 enzyme reactions.A 96-well plate is coated with MLL1 protein. After coating and blocking, WDR5 is added in an optimized assay buffer. Unbound WDR5 is washed away, and the plate is incubated with a primary antibody followed by a secondary HRP-conjugated antibody. Finally, ELISA ECL substrate is added to produce chemiluminescence that can be measured using a chemiluminescence reader. The chemiluminescence signal is proportional to the efficacy of WDR5 binding to MLL1 (KMT2A).
Storage Stability: This assay kit will perform optimally for up to 6 months from date of receipt when the materials are stored as directed.
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
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