Chemical Name: (3S,3'S,5aR,5aR,10bR,10'bR,11aS,11'aS)-2,2',3,3',5a,5'a,6,6'-octahydro-3,3'-bis(hydroxymethyl)-2,2'-dimethyl-[10b,10'b(11H,11'H)-bi3,11a-epidithio-11aH-pyrazino[1',2':1,5]pyrrolo[2,3-b]indole]-1,1',4,4'-tetrone
Chaetocin is a histone methyltransferase SUV39H1 inhibitor (IC50 values are 0.8, 2.5 and 3 μM for dSU(VAR)3-9, mouse G9a and Neurospora crassa DIM5, respectively). Induces apoptosis in myeloma cell lines in vitro; exhibits antiproliferative activity in a mouse myeloma model in vivo.
Chaetocin potently inhibits cell proliferation and colony formation in a wide range of cancer cell lines (IC50 of 2-10 nM) and inhibits tumor growth by deregulating HIF-1α-mediated angiogenesis. Sensitizes glioblastoma multiforme cells to pro-apoptotic agents.
Chaetocin is also an inhibitor of the oxidative stress remediation enzyme thioredoxin reductase (TrxR), and so induces oxidative stress.
In addition, Chaetocin promotes osteogenic differentiation through modulating Wnt/Beta-catenin signaling in mesenchymal stem cells. Chaetocin treatment increased osteogenic ability and reduced adipogenic ability.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9.
Greiner et al.
Chaetocin is a nonspecific inhibitor of histone lysine methyltransferases.
Cherblanc et al.
Reply to "Chaetocin is a nonspecific inhibitor of histone lysine methyltransferases".
Greiner et al.
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