SGI-1027
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.
SGI-1027是一种DNMT抑制剂，对DNMT1、DNMT3A和DNMT3B的IC50值分别为12.5 μM、8 μM和7.5 μM。
SGI-1027在体外对哺乳动物的DNMTs和细菌的M.SssI都有抑制活性。无论是内源性还是重组DNMT都可以被SGI-1027抑制。
这种抑制作用的机制是SGI-1027与Ado-Met竞争，而非酶的辅因子结合位点处的底物DNA。SGI-1027通过直接抑制DNMTs活性 ，从而抑制DNA的甲基化[1]。
在癌细胞中，由于启动子区的CpG岛甲基化，许多TSGs基因是沉默的。SGI-1027可以使CpG岛去甲基化并且激活这些沉默的TSGs基因。在RKO细胞中，SGI-1027的延长处理可以诱导P16和TIMP3基因的表达。此外，SGI-1027通过蛋白酶体途径可以导致DNMT1的选择性降解[1]。
参考文献：
[1] Datta J, Ghoshal K, Denny WA, Gamage SA, Brooke DG, Phiasivongsa P, Redkar S, Jacob ST. A new class of quinoline-based DNA hypomethylating agents reactivates tumor suppressor genes by blocking DNA methyltransferase 1 activity and inducing its degradation. Cancer Res. 2009 May 15;69(10):4277-85.
- 1. Schwartz, Hannah, et al. "In vitro Methods to Better Evaluate Drug Responses in Cancer." UMass Chan Medical School. September 8, 2022.
- 2. Ryan Richards, Megan E. Honeywell, et al. "FLICK: an optimized plate reader-based assay to infer cell death kinetics." STAR Protoc. 2021 Feb 3;2(1):100327. PMID: 33659903
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 461.52 |
| Cas No. | 1020149-73-8 |
| Formula | C27H23N7O |
| Solubility | ≥22.25 mg/mL in DMSO with gentle warming; insoluble in H2O; insoluble in EtOH |
| Chemical Name | N-[4-[(2-amino-6-methylpyrimidin-4-yl)amino]phenyl]-4-(quinolin-4-ylamino)benzamide |
| SDF | Download SDF |
| Canonical SMILES | CC1=CC(=NC(=N1)N)NC2=CC=C(C=C2)NC(=O)C3=CC=C(C=C3)NC4=CC=NC5=CC=CC=C54 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 描述 | SGI-1027是一种DNMT抑制剂，对DNMT1、DNMT3A和DNMT3B的IC50值分别为6 μM、8 μM和7.5 μM。 | |||||
| 靶点 | DNMT1 | DNMT3B | DNMT3A | |||
| IC50 | 6 μM | 7.5 μM | 8 μM | |||
质量控制和MSDS
- 批次:
化学结构
相关生物数据
