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Chaetocin

Cat. No. 4504 1 次引用 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： SUV39H1 inhibitor
化学名： (3S,3'S,5aR,5aR,10bR,10'bR,11aS,11'aS)-2,2',3,3',5a,5'a,6,6'-octahydro-3,3'-bis(hydroxymethyl)-2,2'-dimethyl-[10b,10'b(11H,11'H)-bi3,11a-epidithio-11aH-pyrazino[1',2':1,5]pyrrolo[2,3-b]indole]-1,1',4,4'-tetrone
纯度： ≥95% (HPLC)
说明书
引用文献 (1)
评论
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for Chaetocin

Chaetocin is a histone methyltransferase SUV39H1 inhibitor (IC50 values are 0.8, 2.5 and 3 μM for dSU(VAR)3-9, mouse G9a and Neurospora crassa DIM5, respectively). Induces apoptosis in myeloma cell lines in vitro; exhibits antiproliferative activity in a mouse myeloma model in vivo.

Chaetocin potently inhibits cell proliferation and colony formation in a wide range of cancer cell lines (IC50 of 2-10 nM) and inhibits tumor growth by deregulating HIF-1α-mediated angiogenesis. Sensitizes glioblastoma multiforme cells to pro-apoptotic agents.

Chaetocin is also an inhibitor of the oxidative stress remediation enzyme thioredoxin reductase (TrxR), and so induces oxidative stress.

In addition, Chaetocin promotes osteogenic differentiation through modulating Wnt/Beta-catenin signaling in mesenchymal stem cells. Chaetocin treatment increased osteogenic ability and reduced adipogenic ability.

技术数据 for Chaetocin

分子量 696.84
公式 C30H28N6O6S4
储存 Store at -20°C
纯度 ≥95% (HPLC)
CAS Number 28097-03-2
PubChem ID 161591
InChI Key PZPPOCZWRGNKIR-UHFFFAOYSA-N
Smiles [H][C@]12NC3=C(C=CC=C3)[C@]1(C[C@]13SS[C@](CO)(N(C)C1=O)C(=O)N23)[C@]12C[C@]34SS[C@](CO)(N(C)C3=O)C(=O)N4[C@@]1([H])NC1=C2C=CC=C1

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for Chaetocin

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 6.97 10

制备储备液 for Chaetocin

以下数据基于产品分子量 696.84。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
0.1 mM 14.35 mL 71.75 mL 143.5 mL
0.5 mM 2.87 mL 14.35 mL 28.7 mL
1 mM 1.44 mL 7.18 mL 14.35 mL
5 mM 0.29 mL 1.44 mL 2.87 mL

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产品说明书 for Chaetocin

分析证书/产品说明书
选择另一批次：
化学品安全技术说明书

参考文献 for Chaetocin

参考文献是支持产品生物活性的出版物。

Isham et al (2007) Chaetocin: a promising new antimyeloma agent with in vitro and in vivo activity mediated via imposition of oxidative stress. Blood 109 2579 PMID: 17090648

Greiner et al (2005) Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9. Nat.Chem.Biol. 1 143 PMID: 16408017

Cherblanc et al (2013) Chaetocin is a nonspecific inhibitor of histone lysine methyltransferases. Nat.Chem.Biol. 9 136 PMID: 23416387

Greiner et al (2013) Reply to "Chaetocin is a nonspecific inhibitor of histone lysine methyltransferases". Nat.Chem.Biol. 9 137 PMID: 23416388

Ozyerli-Goknar et al (2019) The fungal metabolite chaetocin is a sensitizer for pro-apoptotic therapies in glioblastoma. Cell Death Dis 10 894 PMID: 31772153

Liang et al (2021) Chaetocin Promotes Osteogenic Differentiation via Modulating Wnt/Beta-Catenin Signaling in Mesenchymal Stem Cells. Stem Cells Int. doi: 10.1155/2021/88 PMID: 33628276

Nakajima et al (2017) Inhibition of the HDAC/Suv39/G9a pathway restores the expression of DNA damage-dependent major histocompatibility complex class I-related chain A and B in cancer cells. Oncol Rep. 38 693 PMID: 28677817

If you know of a relevant reference for Chaetocin, please let us know.

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关键词: Chaetocin, Chaetocin supplier, histone, lysine, methyltransferase, HMTase, SUV39H1, su(var)3-9, epigenetics, inhibits, inhibitors, antiproliferative, myeloma, selective, G9a, glioblastoma, thioredoxin, reductases, bone, osteogenic, stem, cell, differentiation, Lysine, Methyltransferases, Other, Osteogenic, Stem, Cells, Thioredoxin, Reductases, 4504, Tocris Bioscience

1 篇 Chaetocin 的引用文献

引用文献是使用了 Tocris 产品的出版物。 Chaetocin 的部分引用包括：

Bjoern et al (2021) Topoisomerase I inhibition and peripheral nerve injury induce DNA breaks and ATF3-associated axon regeneration in sensory neurons. Cell Rep 36 109666 PMID: 34496254

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