Chaetocin CAS: 28097-03-2
MF: C30H28N6O6S4
MW: 696.84
A lysine-specific histone methyltransferase inhibitor.

Chaetocin (CAS 28097-03-2)

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Synonym: Methyltransferase inhibitor
Application A lysine-specific histone methyltransferase inhibitor
CAS 등록번호: 28097-03-2
순도: ≥98%
분자량: 696.84
분자식: C30H28N6O6S4
* 참조분석증명서대량의 측정 데이터(함수량포함).
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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.


References

1. Greiner, Dorothea., et al., 2005. Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9. Nature chemical biology. 1(3): 143-5. PMID: 16408017
2. Isham, Crescent R., et al., 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
3. Illner, Doris., et al., 2010. Remodeling of nuclear architecture by the thiodioxoxpiperazine metabolite chaetocin. Experimental cell research. 316(10): 1662-80. PMID: 20302859

Physical State :
Solid
에서 유래된 :
Chaetomium
용해도 :
Soluble in DMSO (~25 mg/ml), and ethanol (25 mg/ml).
저장 :
Store at -20° C
밀도 :
~1.9 g/cm3 (Predicted)
굴절률 :
n20D 1.93
IC50 :
HeLa cells: IC50 = 0.05 µg/ml; HMT SU(VAR)3-9: IC50 = 0.6 µm (Drosophila melanogaster); ortholog: IC50 = 0.8 µm (human); HMT SU(VAR)3-9 : IC50 = 0.8 µm; G9a: IC50 = 2.5 µm; DIM5: IC50 = 3 µm; Lys9-HMTs: IC50 = >90 µm
연구용으로만 사용가능합니다. 진단이나 치료용으로 사용불가합니다.
WGK Germany :
3
RTECS :
FM3032000
PubChem CID :
11657687
MDL Number :
MFCD00133163
SMILES :
CN1C(=O)[[email protected]@]23C[[email protected]]4([[email protected]@H](N2C(=O)[[email protected]@]1(SS3)CO)NC5=CC=CC=C54)[[email protected]]67C[[email protected]]89C(=O)N([[email protected]](C(=O)N8[[email protected]]6NC1=CC=CC=C71)(SS9)CO)C

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Chaetocin  논문정보

다른 사용자의 Chaetocin사용법보기. 클릭하여 PubMed entry보기 .

Citations 1 to 4 of {3} total

PMID: # 27141211  Rombo, R. et al. 2016. German medical science : GMS e-journal. 14: Doc04.

PMID: # 27924221  Liu, L. et al. 2016. Cell Discov. 2: 16036.

PMID: # 27467759  Das, S. et al. 2016. PLoS ONE. 11: e0160022.

PMID: # 31811153  Nat Commun. 10: 5594.

Citations 1 to 4 of {3} total
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