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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-Chaetocin
Chaetocin

Chemical Structure : Chaetocin

CAS No.: 28097-03-2

Chaetocin

货号: PC-62758Not For Human Use, Lab Use Only.

Chaetocin is a potent, specific, SAM-competitive inhibitor of histone H3K9 methyltransferase (HMT) SU(VAR)3-9 (SUV39H1) with IC50 of 0.6 uM, no actiivty against H4 Lys20-specific HMT PRSET7 and SET7/9.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Chaetocin is a potent, specific, SAM-competitive inhibitor of histone H3K9 methyltransferase (HMT) SU(VAR)3-9 (SUV39H1) with IC50 of 0.6 uM, no actiivty against H4 Lys20-specific HMT PRSET7 and SET7/9.
Chaetocin inhibits the human ortholog of dSU(VAR)3-9 with IC50 of 0.8 uM, also inhibits Lys9-specific HMTs such as mouse G9a and Neurospora crassa DIM5 (IC50=2.5 and 3 uM).
Chaetocin prolongs survival and restores mitochondrial dysfunction, improves prognosis in a rat model of high salt diet-induced heart failure。
Chaetocin induces cell cycle arrest and apoptosis in melanoma cells.

物理化学性质&存储条件

分子量 696.851
分子式 C30H28N6O6S4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

O=C([C@@](N1C)(SS2)CO)N3[C@](NC4=CC=CC=C54)([H])[C@]5([C@@]6(C7=CC=CC=C7N8)[C@@]8([H])N(C9=O)[C@](C%10=O)(SS[C@]9(CO)N%10C)C6)C[C@]32C1=O

参考文献

1. Greiner D, et al. Nat Chem Biol. 2005 Aug;1(3):143-5.

2. Vo MC, et al. Oncotarget. 2017 Jul 11;8(28):46047-46056.

3. Yang G, et al. Nat Commun. 2017 Mar 31;8:14941.

4. Ono T, et al. Sci Rep. 2017 Jan 4;7:39752.

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