Chaetocin
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Chaetocin，来源于球毛壳菌的天然硫基二氧代哌嗪产物，是一个赖氨酸特异性的组蛋白甲基转移酶抑制剂，可以减少SUV39H1的组蛋白甲基转移酶效应，IC50值为0.8 μM。
SUV39H1是组蛋白甲基转移酶，可以甲基化组蛋白H3的赖氨酸9，在许多过程中发挥着重要功能，包括对MYOD1刺激的分化的抑制、细胞周期的调节、细胞分化以及端粒长度的调节。
Chaetocin在一些癌细胞中具有凋亡效应。在患者的CD138 +骨髓瘤细胞中，chaetocin具有较强的抗骨髓瘤活性，这是通过对氧化还原酶硫氧还蛋白还原酶的抑制所诱导的活性氧（ROS）来发挥作用的[1]。Chaetocin减少HL-60和KG-1a细胞中H3K9和H3K27的甲基化[2]。
Chaetocin也被用在动物模型中来研究SUV39H1的作用。Chaetocin在小鼠骨髓瘤异种移植物模型表现出抗增殖活性和抗癌作用[3]。
参考文献：
1. Isham CR, Tibodeau JD, Jin W, Xu R, Timm MM, Bible KC. Chaetocin: a promising new antimyeloma agent with in vitro and in vivo activity mediated via imposition of oxidative stress. Blood 2007,109:2579-2588.
2.Lai YS, Chen JY, Tsai HJ, Chen TY, Hung WC. The SUV39H1 inhibitor chaetocin induces differentiation and shows synergistic cytotoxicity with other epigenetic drugs in acute myeloid leukemia cells. Blood Cancer J 2015,5:e313.
3.Isham CR, Tibodeau JD, Bossou AR, Merchan JR, Bible KC. The anticancer effects of chaetocin are independent of programmed cell death and hypoxia, and are associated with inhibition of endothelial cell proliferation. Br J Cancer 2012,106:314-323.
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 696.84 |
| Cas No. | 28097-03-2 |
| Formula | C30H28N6O6S4 |
| Solubility | Limited solubility, soluble in DMSO |
| Chemical Name | (3S,3'S,6R,6'R,14R,14'R,16S,16'S)-3,3'-bis(hydroxymethyl)-2,2'-dimethyl-2,2',3,3',6,6',7,7'-octahydro-1H,1'H-[14,14'-bi(3,11a-epidithiopyrazino[1',2':1,5]pyrrolo[2,3-b]indole)]-1,1',4,4'(15H,15'H)-tetraone |
| SDF | Download SDF |
| Canonical SMILES | O=C1[C@](CO)(SS2)N(C)C([C@]32N1[C@]4([H])[C@](C(C=CC=C5)=C5N4)([C@@]6(C(C=CC=C7)=C7N8)[C@@]8([H])N(C([C@](CO)(SS9)N%10C)=O)[C@]9(C6)C%10=O)C3)=O |
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化学结构
