Chaetocin

製品コードS8068 バッチS806801

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₃₀H₂₈N₆O₆S₄
	分子量	696.84	CAS No.	28097-03-2
Solubility (25°C)*	体外	DMSO	100 mg/mL warmed with 50ºC water bath (143.5 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Chaetocin, a natural product from Chaetomium species, is a histone methyltransferase inhibitor with IC50 of 0.8 μM, 2.5 μM and 3 μM for dSU(VAR)3-9, mouse G9a and Neurospora crassa DIM5, respectively. Chaetocin is an anticancer agent and inhibitor of thioredoxin reductase (TrxR).
in vitro	In SL-2 Drosophila tissue culture cells, Chaetocin causes the inhibition of SU(VAR)3-9 and the number of H3 molecules dimethylated at Lys9, and also inhibits cell growth. ^[1] In HepG2, Hep3B, and Huh7 human hepatoma cells, Chaetocin inhibits HIF-1-Mediated hypoxic responses. ^[2] Chaetocin also potently inhibits proliferation and colony formation in a broad range of cancer cell lines with IC50 of 2-10 nM. ^[3]
in vivo	In Hepa 1c1c-7 tumor-bearing mice, Chaetocin (0.25 mg/kg, i.p.) inhibits tumor growth by deregulating HIF-1[alpha]-mediated angiogenesis. ^[2] In SKOV3 tumor-bearing nude mice, chaetocin treatment (0.25 mg/kg, i.p.) significantly delays the tumor growth with minimal evidence of toxicities. ^[3]

製品説明

Chaetocin, a natural product from Chaetomium species, is a histone methyltransferase inhibitor with IC50 of 0.8 μM, 2.5 μM and 3 μM for dSU(VAR)3-9, mouse G9a and Neurospora crassa DIM5, respectively. Chaetocin is an anticancer agent and inhibitor of thioredoxin reductase (TrxR).

in vitro

In SL-2 Drosophila tissue culture cells, Chaetocin causes the inhibition of SU(VAR)3-9 and the number of H3 molecules dimethylated at Lys9, and also inhibits cell growth. ^[1]

In HepG2, Hep3B, and Huh7 human hepatoma cells, Chaetocin inhibits HIF-1-Mediated hypoxic responses. ^[2]

Chaetocin also potently inhibits proliferation and colony formation in a broad range of cancer cell lines with IC50 of 2-10 nM. ^[3]

in vivo

In Hepa 1c1c-7 tumor-bearing mice, Chaetocin (0.25 mg/kg, i.p.) inhibits tumor growth by deregulating HIF-1[alpha]-mediated angiogenesis. ^[2]

In SKOV3 tumor-bearing nude mice, chaetocin treatment (0.25 mg/kg, i.p.) significantly delays the tumor growth with minimal evidence of toxicities. ^[3]

プロトコル(参考用のみ)

キナーゼアッセイ	Methylation assays
キナーゼアッセイ	Unless otherwise stated, reactions are performed as followed: 1 g of purified enzyme (dSU(VAR)3-9 213; GST-hSUV39H1(82-412); GST-ncDIM5(19-318) and GSTmG9a(621-1000); dPRSET7(1-691); His-SET7/9(109-366) or enzyme complex expressed in a baculoviral expression system (dE(z), dSU(Z)12, dp55, dESC) were incubated for 30 minutes with 1 g of a peptide containing the first 19 amino acids of H3 plus an additional cystein residue (ARTKQTARKSTGGKAPRKQC) in a total volume of 40μl in BC25 (10mM HEPES pH7.6, 25mM NaCl, 1mM EDTA, 10%glycerol). All enzymes except for the E(z) complex had a similar specific activity between 5-10 nmole/min/mg. For the E(z) complex, the specific activity is approximately 5-10 fold lower, which is probably due to an incomplete formation of the full complex that is required for the highest activity. As a methyl donor S-Adenosyl [methyl-3H] methionine (SAM) is present in the reaction at a final concentration of 40 M with a specific activity of 0.3Ci/mmole. Reactions are stopped by adding 1/10 volume of 100% acetic acid and the incorporation of radioactivity is measured by spotting 30 l of the reaction on P81 filter paper and subsequent scintillation counting. For the inhibitor screening, 1 l of inhibitor with a concentration of 10 g/l is added to each reaction. In the cases where PRSET7 or the E(z) complex is used as enzyme either recombinant nucleosomes (1 g) or recombinant H3 (1 g) respectively replaced the H3 peptide as a substrate.
細胞アッセイ	細胞株	HEK293T
	濃度	125 nM
	反応時間	24 h
	実験の流れ	Cells were treated with chaetocin (125 nM) or DMSO for 24 h.
動物実験	動物モデル	Hur7 tumor-bearing mice, Hepa 1c1c-7 tumor-bearing mice
	投薬量	0.25 mg/kg
	投与方法	i.p.

参考

[4] Siddaway R, et al. Acta Neuropathol. 2022 Nov;144(5):1027-1048.

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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Methionine restriction promotes cGAS activation and chromatin untethering through demethylation to enhance antitumor immunity [ Cancer Cell, 2023, 41(6):1118-1133.e12]	PubMed: 37267951
GalNAc-conjugated siRNA targeting the DNAJB1-PRKACA fusion junction in Fibrolamellar Hepatocellular Carcinoma [ Mol Ther, 2023, 10.1016/j.ymthe.2023.11.012]	PubMed: 37980543
Oncogenic Addiction of Fibrolamellar Hepatocellular Carcinoma to the Fusion Kinase DNAJB1-PRKACA [ Clin Cancer Res, 2023, 29(1):271-278]	PubMed: 36302174
Priming therapy by targeting enhancer-initiated pathways in patient-derived pancreatic cancer cells [ EBioMedicine, 2023, 92:104602]	PubMed: 37148583
Telomere dysfunction promotes cholangiocyte senescence and biliary fibrosis in primary sclerosing cholangitis [ JCI Insight, 2023, 10.1172/jci.insight.170320]	PubMed: 37707950
Exposure to high-sugar diet induces transgenerational changes in sweet sensitivity and feeding behavior via H3K27me3 reprogramming [ Elife, 2023, 12e85365]	PubMed: 37698486
SUV39H1 is a novel biomarker targeting oxidative phosphorylation in hepatitis B virus-associated hepatocellular carcinoma [ BMC Cancer, 2023, 23(1):1159]	PubMed: 38017386
SUV39H1 Inhibits Angiogenesis in Limb Ischemia of Mice [ Cell Transplant, 2023, 32:9636897231198167]	PubMed: 37811706
SUV39H1 Inhibits Angiogenesis in Limb Ischemia of Mice [ Cell Transplant, 2023, 32:9636897231198167]	PubMed: 37811706
Oncohistone interactome profiling uncovers contrasting oncogenic mechanisms and identifies potential therapeutic targets in high grade glioma [ Acta Neuropathol, 2022, 144(5):1027-1048]	PubMed: 36070144

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人間や獣医の診断であるか治療的な使用のためにでない。

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