RG-108
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Cat.No：IR0790 Solarbio
CAS：48208-26-0
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Solid
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> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Epigenetics > RG-108
Product Information
| CAS | 48208-26-0 |
| Name | RG-108 |
| Molecular Formula | C19H14N2O4 |
| Molecular Weight | 334.33 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD08705332 |
| SMILES | O=C(N1[C@H](C(O)=O)CC2=CNC3=C2C=CC=C3)C4=CC=CC=C4C1=O |
| InChIKey | HPTXLHAHLXOAKV-INIZCTEOSA-N |
| InChI | InChI=1S/C19H14N2O4/c22-17-13-6-1-2-7-14(13)18(23)21(17)16(19(24)25)9-11-10-20-15-8-4-3-5-12(11)15/h1-8,10,16,20H,9H2,(H,24,25)/t16-/m0/s1 |
| PubChem CID | 702558 |
| Target Point | DNA Methyltransferase |
| Passage | Epigenetics |
| Background | RG-108 is a DNA methyltransferase inhibitor. |
| Biological Activity | RG108 是一种非核苷的 DNA 甲基转移酶 (DNA methyltransferase) 抑制剂，IC50 值为 115 nM。[1-3] |
| In Vitro | RG108在体外有效阻断DNA甲基转移酶，并且不会在人细胞系中引起共价酶捕获。用低微摩尔浓度的RG108孵育细胞导致基因组DNA的显著去甲基化而没有任何可检测的毒性。有趣的是，RG108引起肿瘤抑制基因的去甲基化和再激活，但它不影响着丝粒卫星序列的甲基化[1]。在另一项研究中，研究了生物素化RG108结合物的合成和体外分析，以评估与DNA甲基转移酶的相互作用[2]。在最近的一项研究中，显示与天然SM相比，RG108可以显著降低SM衍生的iPS细胞中的DNA甲基转移酶活性[3]。 |
| Kinase Experiment | 用于体外甲基化测定的底物DNA是来自人p16Ink4a基因的启动子区的798bp片段(相对于起始密码子为-423/+ 375)。甲基化反应含有350至400ng底物DNA和4单位M.SssI甲基化酶(0.5μM)，终体积为50μL。加入抑制剂至终浓度分别为10，100，200和500μM。反应在37℃下进行2小时。完成后，将反应在65℃下灭活15分钟，并使用PCR纯化试剂盒纯化DNA。将300纳克纯化的DNA在60℃下用30单位BstUI消化3小时，并在2％Tris-硼酸盐EDTA琼脂糖凝胶上分析。 |
| Data Literature Source | [1]. Brueckner B，et al. Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of human DNA methyltransferases. Cancer Res. 2005 Jul 15;65(14):6305-11. [2]. Schirrmacher E，et al. Synthesis and in vitro evaluation of biotinylated RG108: a high affinity compound for studying binding interactions with human DNA methyltransferases. Bioconjug Chem. 2006 Mar-Apr;17(2):261-6. [3]. Pasha Z，et al. Efficient non-viral reprogramming of myoblasts to stemness with a single small molecule to generate cardiac progenitor cells. PLoS One. 2011;6(8):e23667 |
| Unit | Bottle |
| Specification | 5mg 10mg |
是一种DNA methyltransferase抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
Note：
1. The products are all for scientific research use only. Do not use it for medical, clinical diagnosis or treatment, food and cosmetics, etc. Do not store them in ordinary residential areas.
2. For your safety and health, please wear laboratory clothes, disposable gloves and masks.
3. The experimental results may be affected by many factors, after-sale service is limited to the product itself and does not involve other compensation.
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