Chaetocin

BML-GR349

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Methyltransferase inhibitor

Chaetocin, an antitumor antibiotic, is a thiodioxopiperazine natural product produced by Chaetomium species. Specific inhibitor of the lysine-specific methyltransferase SU (VAR)3-9 both in vitro and in vivo. It displays potent antimyeloma activity in IL-6-dependent myeloma cell lines. Its antimyeloma activity appears to be due to induction of oxidative stress and consequent apoptosis.

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Product Details

Appearance	White to off-white solid.
CAS	28097-03-2
Couple Target	Methyltransferase
Couple Type	Inhibitor
Formula	C₃₀H₂₈N₆O₆S₄
MW	696.9
Purity	≥98% (HPLC)
Solubility	Soluble in DMSO.
Source	Isolated from Chaetomium sp.

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended. Store, as supplied, at -20°C for up to 1 year. Store solutions at -20°C for up to 3 months.
Short Term Storage	-20°C
Shipping	Blue Ice

Regulatory Status	RUO – Research Use Only

The anticancer effect of chaetocin is enhanced by inhibition of autophagy: H. J. Jung, et al.; Cell Death Dis. 7, e2098 (2016), Application(s): Cell culture, Abstract
Arsenic silences hepatic PDK4 expression through activation of histone H3K9 methylatransferase G9a: X. Zhang, et al.; Toxicol. Appl. Pharmacol. 304, 42 (2016), Application(s): Cell culture, Abstract
Emerging role of linker histone variant H1x as a biomarker with prognostic value in astrocytic gliomas. A multivariate analysis including trimethylation of H3K9 and H4K20: Sepsa, A., Levidou, G., et al.; PLoS One 10, e0115101 (2015), Abstract
Chaetocin: a promising new antimyeloma agent with in vitro and in vivo activity mediated via imposition of oxidative stress: C.R. Isham, et al.; Blood 109, 2579 (2007), Abstract
Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9: D. Greiner, et al.; Nat. Chem. Biol. 1, 143 (2005), Abstract
[Isolation and configuration of Chaetocin]: D. Hauser, et al.; Helv. Chim. Acta. 53, 1061 (1970), (Article in German), Abstract

Last modified: May 29, 2024

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Chaetocin

BML-GR349

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