SIRT1/2 Inhibitor IV
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.
SIRT1/2 Inhibitor IV是一种小分子SIRT1和SIRT2抑制剂,IC50值分别为56 µM和59 µM[1]。
Sirtuin 1 (SIRT1)和SIRT2是NAD依赖性的去乙酰化酶,是sirtuin家族蛋白的成员。SIRT1调节参与代谢、炎症和肿瘤发生的信号通路,而SIRT2作为微管蛋白的去乙酰化酶起作用[2]。
SIRT1/2 Inhibitor IV是一种细胞通透性的SIRT1和SIRT2抑制剂。SIRT1/2 Inhibitor IV抑制人SIRT1和SIRT2的NAD依赖性去乙酰化酶活性,IC50值分别为56和59 µmol/L。在NCI H460肺癌细胞系中,用SIRT1/2 Inhibitor IV和trichostatin A联合抑制SIRT2和HDAC6可导致微管蛋白的超乙酰化。SIRT1/2 Inhibitor IV也增加p53的乙酰化水平。在p53阳性肺癌细胞系NCI H460中,SIRT1/2 Inhibitor IV以p53非依赖的方式诱导对etoposide的剂量依赖性致敏[1]。
在小鼠异种移植模型中,SIRT1/2 Inhibitor IV (100 mg/kg)通过尾静脉注射或腹腔注射每天给药,给药2周(每周5次)可减少肿瘤生长[1]。在SIRT1/2 Inhibitor IV预处理2小时的小鼠中,暴露于6%的氧气中6小时,SIRT1/2 Inhibitor IV显著减少肾和肝脏中EPO mRNA的水平[2]。
参考文献:
Heltweg B, Gatbonton T, Schuler AD, et al. Antitumor activity of a small-molecule inhibitor of human silent information regulator 2 enzymes. Cancer Res. 2006 Apr 15;66(8):4368-77.
Laemmle A, Lechleiter A, Roh V, et al. Inhibition of SIRT1 impairs the accumulation and transcriptional activity of HIF-1α protein under hypoxic conditions. PLoS One. 2012;7(3):e33433.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 360.43 |
Cas No. | 14513-15-6 |
Formula | C21H16N2O2S |
Solubility | Soluble in DMSO |
Chemical Name | 5-((2-hydroxynaphthalen-1-yl)methyl)-2-mercapto-6-phenylpyrimidin-4-ol |
SDF | Download SDF |
Canonical SMILES | OC(C=CC1=CC=CC=C12)=C2CC(C(O)=NC(S)=N3)=C3C4=CC=CC=C4 |
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。 |