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Sirt1/2-IN-3

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产品编号 T79564Cas号 301313-42-8

Sirt1/2-IN-3 (compound PS9) 作为SIRT1/2的双重抑制剂,其对SIRT1和SIRT2的IC50值分别为1.4 μM 和 2.0 μM。该化合物能够有效抑制p53脱乙酰化,并提升p53与α-微管蛋白的乙酰化水平。Sirt1/2-IN-3还能诱导细胞凋亡,并展现对人白血病细胞系的抗增殖效果。

Sirt1/2-IN-3

Sirt1/2-IN-3

Rating icon 还可以
产品编号 T79564Cas号 301313-42-8

Sirt1/2-IN-3 (compound PS9) 作为SIRT1/2的双重抑制剂,其对SIRT1和SIRT2的IC50值分别为1.4 μM 和 2.0 μM。该化合物能够有效抑制p53脱乙酰化,并提升p53与α-微管蛋白的乙酰化水平。Sirt1/2-IN-3还能诱导细胞凋亡,并展现对人白血病细胞系的抗增殖效果。

规格价格库存数量
5 mg
待询
8-10周
50 mg
待询
8-10周
大包装 & 定制
TargetMol 的所有产品仅用作科学研究或药证申报,不能被用于人体,我们不向个人提供产品和服务。请您遵守承诺用途,不得违反法律法规规定用于任何其他用途。
实验操作小课堂
常见问题解答
化合物带有盐酸盐离子、硫酸盐离子等是否和其本身有什么区别?盐形式和游离态有什么区别?
盐和非盐形式化合物的活性分子是一样的,在生物实验中起到的效果也一致,活性和使用方法都是一样的。只是由于呈盐不同,物理性质比如溶解度会有差异。建议您根据溶解、实验需求进行选择。
如何选择某个靶点的特异性或总的抑制剂?特异性和非特异性的区别是什么?
抑制剂按照特异性分为广谱 pan 和特异性 selective 两种。Pan 为某个靶点总的抑制剂,对所有亚型或整个家族的成员都有抑制作用。Selective 抑制剂针对某个蛋白激酶的某个亚型或家族中某个成员抑制率特别高或有特异性抑制作用。 一般评价一个抑制剂的抑制效率主要看 IC50 值,IC50 值越低,说明抑制剂效率越高。建议您根据以上几个特征进行综合选择,也可联系技术帮您推荐相关抑制剂。
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产品介绍

生物活性
产品描述
Sirt1/2-IN-3 (compound PS9) serves as a dual inhibitor of SIRT1/2, exhibiting IC50 values of 1.4 μM (SIRT1) and 2.0 μM (SIRT2), respectively. This compound effectively inhibits p53 deacetylation while simultaneously elevating p53 and α-tubulin acetylation levels. Additionally, Sirt1/2-IN-3 promotes apoptosis and exhibits antiproliferative effects on human leukemia cell lines [1].
体外活性
Sirt1/2-IN-3 (compound hsa55) (5 μM; 48 h) 在多种肿瘤细胞中引发凋亡,其半抑制浓度(IC 50)分别为:MV4-11细胞为6.5 μM、MOLM-13细胞为9.2 μM、THP1细胞为27.2 μM、Jurkat细胞为17.4 μM [1]。此外,Sirt1/2-IN-3在100 μM浓度和30分钟处理下可降低SIRT1及SIRT2蛋白的热稳定性,并能在25 μM及30 μM浓度,24小时处理后提高MOLM-13细胞中p53和α微管蛋白的乙酰化水平 [1]。
化学信息
分子量363.82
分子式C17H14ClNO4S
CAS No.301313-42-8
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

剂量转换

对于不同动物的给药剂量换算,您也可以参考 更多

参考文献

1.Vigushin DM, et al. Trichostatin A is a histone deacetylase inhibitor with potent antitumor activity against breast cancer in vivo. Clin Cancer Res. 2001 Apr;7(4):971-6.2.Ma J, et al. Trichostatin A, a histone deacetylase inhibitor, suppresses proliferation and promotes apoptosis of esophageal squamous cell lines. Mol Med Rep. 2015 Jun;11(6):4525-31.3.Chan ST, et al. Quercetin enhances the antitumor activity of trichostatin A through upregulation of p53 protein expression in vitro and in vivo. PLoS One. 2013;8(1):e54255.4.Huang W, et al. J Biol Chem, 2005, 280(11), 120047-120054.5.Avila AM, et al. J Clin Invest, 2007, 117(3), 659-671.6.Li X, Pan L, Wang B, et al. The Histone Deacetylases HosA and HdaA Affect the Phenotype and Transcriptomic and Metabolic Profiles of Aspergillus niger[J]. Toxins. 2019, 11(9): 520.7.Meng Y, Qian X, Zhao L, et al. Trichostatin A downregulates bromodomain and extra-terminal proteins to suppress osimertinib resistant non-small cell lung carcinoma[J]. Cancer Cell International. 2021, 21(1): 1-12.8.Xu K, Sun G, Li M, et al. Glibenclamide Targets Sulfonylurea Receptor 1 to Inhibit p70S6K Activity and Upregulate KLF4 Expression to Suppress Non-Small Cell Lung Carcinoma[J]. Molecular cancer therapeutics. 2019, 18(11): 2085-2096.9.Su Q, Li T, He P F, et al. Trichostatin A ameliorates Alzheimer’s disease-related pathology and cognitive deficits by increasing albumin expression and Aβ clearance in APP/PS1 mice[J]. Alzheimer's Research & Therapy. 2021, 13(1): 1-15.

文献引用

1.Wang C, Huang M, Lin Y, et al.ENO2-derived phosphoenolpyruvate functions as an endogenous inhibitor of HDAC1 and confers resistance to antiangiogenic therapy.Nature Metabolism.2023: 1-22.2.Liang X L, Ouyang L, Yu N N, et al.Histone deacetylase inhibitor pracinostat suppresses colorectal cancer by inducing CDK5-Drp1 signaling-mediated peripheral mitofission.Journal of Pharmaceutical Analysis.20233.Guo Q, Jing Y, Gao Y, et al.The PIF1/PIF3‐MED25‐HDA19 transcriptional repression complex regulates phytochrome signaling in Arabidopsis.New Phytologist.20234.Su Q, Li T, He P F, et al. Trichostatin A ameliorates Alzheimer’s disease-related pathology and cognitive deficits by increasing albumin expression and Aβ clearance in APP/PS1 mice. Alzheimer's Research & Therapy. 2021 Jan 4;13(1):7. doi: 10.1186/s13195-020-00746-8.5.Yuting Meng,Xixi Qian,Li Zhao,Nan Li,Shengjie Wu,Baoan Chen,Tong Sun,Xuerong Wang Trichostatin A downregulates bromodomain and extra-terminal proteins to suppress osimertinib resistant non-small cell lung carcinoma. Cancer Cell International. 2021, 21(1): 1-12.6.Zhang L, Shi J, Du D, et al. Ketogenesis acts as an endogenous protective programme to restrain inflammatory macrophage activation during acute pancreatitis. eBioMedicine. 2022, 78: 103959.7.Li X, Pan L, Wang B, et al. The Histone Deacetylases HosA and HdaA Affect the Phenotype and Transcriptomic and Metabolic Profiles of Aspergillus niger. Toxins. 2019, 11(9): 520.8.Xu K, Sun G, Li M, et al. Glibenclamide Targets Sulfonylurea Receptor 1 to Inhibit p70S6K Activity and Upregulate KLF4 Expression to Suppress Non-Small Cell Lung Carcinoma. Molecular cancer therapeutics. 2019, 18(11): 2085-2096.9.Du T, Hu X, Hou Z, et al.Re-expression of epigenetically silenced PTPRR by histone acetylation sensitizes RAS-mutant lung adenocarcinoma to SHP2 inhibition.Cellular and Molecular Life Sciences.2024, 81(1): 1-14.10.Xu C, Zhao W, Peng L, et al.PRDM14 extinction enables the initiation of trophoblast stem cell formation.Cellular and Molecular Life Sciences.2024, 81(1): 208.11.Xu W, Wang Z, Liu T, et al.Eurycomanone inhibits osteosarcoma growth and metastasis by suppressing GRP78 expression.Journal of Ethnopharmacology.2024: 118709.

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