Chaetocin

Key Product Details

Product Description

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.

Product Specifications for Chaetocin

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for Chaetocin

The following data is based on the product molecular weight 696.84.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

10 9 8 7 6 5 4 3 2 1 Recalculate

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	14.35 mL	71.75 mL	143.50 mL
0.5 mM	2.87 mL	14.35 mL	28.70 mL
1 mM	1.44 mL	7.18 mL	14.35 mL
5 mM	0.29 mL	1.44 mL	2.87 mL

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 9 publications citing the usage of this product.

• Liang Chaetocin Promotes Osteogenic Differentiation via Modulating Wnt/Beta-Catenin Signaling in Mesenchymal Stem Cells. Stem Cells Int. 2021 PMID: 33628276
• Nakajima Inhibition of the HDAC/Suv39/G9a pathway restores the expression of DNA damage-dependent major histocompatibility complex class I-related chain A and B in cancer cells. Oncol Rep. 2017 PMID: 28677817
• Ozyerli-Goknar The fungal metabolite chaetocin is a sensitizer for pro-apoptotic therapies in glioblastoma. Cell Death Dis 2019 PMID: 31772153
• Greiner Reply to "Chaetocin is a nonspecific inhibitor of histone lysine methyltransferases". Nat.Chem.Biol. 2013 PMID: 23416388
• Cherblanc Chaetocin is a nonspecific inhibitor of histone lysine methyltransferases. Nat.Chem.Biol. 2013 PMID: 23416387
• Greiner Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9. Nat.Chem.Biol. 2005 PMID: 16408017
• Isham Chaetocin: a promising new antimyeloma agent with in vitro and in vivo activity mediated via imposition of oxidative stress. Blood 2007 PMID: 17090648

Product Documents for Chaetocin