Non-selective histone lysine methyltransferase inhibitor (IC 50 values are 0.8, 2.5 and 3 μM for Suv39H1, G9a and DIM5 respectively). Competitive, selective thioredoxin substrate. Induces ROS generation and oxidative stress. Selectively induces apoptosis
Storage Temp
Store at 2-8°C
Shipped In
Wet ice
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of SUV39H1 histone lysine methyltransferase
Note
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description
Chaetocin, a natural product originally produced by Chaetomium species, is shown to have apoptotic effects on some cancer cells. Mechanistic studies show that chaetocin is taken up in the cells by a process that requires intact/unreduced disulfides for uptake. Once inside, this compound imposes oxidative stress and consequent apoptosis induction. Other studies have shown chaetocin to reduce lysine-specific histone methyltransferase effects of SUV39H, which play a key role in maintaining stable gene expression patterns during embryonic development and cellular differentiation. Additionally, this agent is reported to cause profound chromatin reorganization in fibroblast nuclei by inducing chromatin condensation/clustering. Consequentially, chaetocin impairs Trx (thioredoxin) systems, which are essential for deoxynucleotide synthesis and involved in a broad range of cellular functions. Chaetocin is an inhibitor of G9a, SUV39H1 and TrxR1.
1.Isham CR, Tibodeau JD, Jin W, Xu R, Timm MM, Bible KC. (2007) Chaetocin: a promising new antimyeloma agent with in vitro and in vivo activity mediated via imposition of oxidative stress.. Blood, 109 (6):(2579-88). [PMID:17090648]
2.Greiner D, Bonaldi T, Eskeland R, Roemer E, Imhof A. (2005) Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9.. Nat Chem Biol, 1 (3):(143-5). [PMID:16408017]
3.Chaib H, Nebbioso A, Prebet T, Castellano R, Garbit S, Restouin A, Vey N, Altucci L, Collette Y. (2012) Anti-leukemia activity of chaetocin via death receptor-dependent apoptosis and dual modulation of the histone methyl-transferase SUV39H1.. Leukemia, 26 (4):(662-74). [PMID:21979880]
4.Cherblanc FL, Chapman KL, Brown R, Fuchter MJ. (2013) Chaetocin is a nonspecific inhibitor of histone lysine methyltransferases.. Nat Chem Biol, 9 (3):(136-7). [PMID:23416387]
5.Liu Z et al.. (2021) A methyltransferase-like 14/miR-99a-5p/tribble 2 positive feedback circuit promotes cancer stem cell persistence and radioresistance via histone deacetylase 2-mediated epigenetic modulation in esophageal squamous cell carcinoma.. Clin Transl Med, 11 (9):(e545). [PMID:34586732]
6.Nakajima NI et al.. (2017) Inhibition of the HDAC/Suv39/G9a pathway restores the expression of DNA damage-dependent major histocompatibility complex class\xa0I-related chain\xa0A\xa0and\xa0B in cancer cells.. Oncol Rep, 38 (2):(693-702). [PMID:28677817]
7.Harro CM et al.. (2021) Methyltransferase inhibitors restore SATB1 protective activity against cutaneous T cell lymphoma in mice.. J Clin Invest, 131 (3):[PMID:33270606]
Solution Calculators
Molarity Calculator
Determine the necessary mass, volume, or concentration for preparing a solution.
Dilution Calculator
Determine the dilution needed to prepare a stock solution.
B2306622