Butyrolactone 3, also called MB-3 is an inhibitor of Histone acetyltransferase GCN5 (general control of amino-acid synthesis 5). Gcn5 HAT activity is required to acetylate histone H3 lysine 9 (K9) and K14, which allows transcription elongation by relaxing nucleosomes. Butyrolactone 3 specifically inhibits Gcn5's HAT activity. It has been shown to display anti-inflammatory and anti-carcinogenic effects.
1. Mai, Antonello., et al., 2006. Small-molecule inhibitors of histone acetyltransferase activity: identification and biological properties. Journal of medicinal chemistry. 49(23): 6897-907. PMID: 17154519 2. Holmlund, T., et al., 2013. GCN5 acetylates and regulates the stability of the oncoprotein E2A-PBX1 in acute lymphoblastic leukemia. Leukemia. 27(3): 578-85. PMID: 23044487
Soluble in DMSO, and methanol.
Store at -20° C
386.21° C at 760 mmHg (Predicted)
1.20 g/cm3 (Predicted)
n20D 1.50 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
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Holmlund et alHolmlund et al. (PubMed ID 23044487) found that Butyrolactone 3 inhibited GCN5 and decreased E2A-PBX1 acetylation and E2A-PBX1 protein levels in leukemic cells. -SCBT Publication Review
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