Shelf life (days): 730.0
Formulation: A crystalline solid
Formal Name: 2,2',3S,3'S,5aR,5'aR,6,6'-octahydro-3,3'-bis(hydroxymethyl)-2,2'-dimethyl-[10bR,10'bR(11aS,11'aS)-bi-3,11a-epidithio-11aH-pyrazino[1',2':1,5]pyrrolo[2,3-b]indole]-1,1',4,4'-tetrone
Purity: ≥95%
Formula Markup: C30H28N6O6S4
Formula Weight: 696.8
CAS Number: 28097-03-2
Notes: The methylation of histones by histone methyltransferases (HMT) is an important mechanism by which gene expression is stably altered during cellular differentiation and embryonic development. Chaetocin is a fungal mycotoxin that inhibits the HMT SU(VAR)3-9 (IC50 = 0.8 μM).{18476} It inhibits other Lys9-specific HMTs, including G9a (IC50 = 2.5 μM) and DIM5 (IC50 = 3 μM).{18476} Selectivity for Lys9-HMTs is indicated by higher IC50 values (>90 μM) for Lys20-specific PRSET7, Lys27-specific EZH2, and Lys4-specific SET7/9. Chaetocin potently induces cellular oxidative stress, selectively killing cancer cells and rapidly-proliferating primary cells.{18475,18476} Chaetocin’s effects on oxidative stress are, at least in part, due to its capacity to act as a competitive and selective substrate for thioredoxin reductase-1 (Km = 4.6 μM).{18477} Chaetocin is useful both in epigenetic studies as an HMT inhibitor and in cancer research.{18398,17782,18480}
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