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Synonyms: α-methylene-γ-butyrolactone 3
Compound class: Synthetic organic
Comment: MB-3 is reported as a cell-permeable small-molecule inhibitor of the histone acetyltransferase enzyme, general control nonderepressible 5 (GCN5, gene symbol KAT2B) . In vitro, MB-3 has been shown to inhibit GCN5-driven acetylation of the chimeric oncoprotein E2A-PBX1 . E2A-PBX1 is a non-histone target of GCN5 .
A 2017 article by Dahlin et al. suggests that the thiol-reactivity of MB-3 brings in to question its activity as a selective HAT inhibitor .
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
|No information available.|
|Mechanism Of Action and Pharmacodynamic Effects|
|E2A-PBX1 (pre-B-cell leukemia transcription factor) is a fused oncoprotein which results from a t(1;19)(q23;q13) chromosomal translocation. E2A-PBX1 is found in more than 20% of patients with pediatric pre-B ALL (acute lymphoblastic leukemia) . GCN5-induced acetylation of E2A-PBX1 stablises the oncoprotein and leads to oncogenic transformation in B-cells. MB-3 inhibits this process and results in increased E2A-PBX1 degradation via a E3 ubiquitin ligase HDM2 mechanism .|