Thiomyristoyl
别名: TM
Thiomyristoyl (TM)是一种有效的、特异性SIRT2抑制剂，IC50为28 nM。它抑制SIRT1的IC50值为98 μM，而在浓度高达200 μM时，对SIRT3没有抑制作用。
Thiomyristoyl Chemical Structure
CAS: 1429749-41-6
产品质控
批次：
S824501
DMSO]100 mg/mL]false]Ethanol]100 mg/mL]false]Water]Insoluble]false
纯度：
99.84%
99.84
Thiomyristoyl相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| HeLa | Cytotoxicity assay | 50 uM | 72 hrs | Cytotoxicity against human HeLa cells assessed as reduction in cell viability at 50 uM measured after 72 hrs by CCK8 assay | 31117516 |
| MCF7 | Growth inhibition assay | 15 uM | 72 hrs | Growth inhibition of human MCF7 cells at 15 uM measured after 72 hrs by AlamarBlue assay | 31144814 |
| Neuro2a | Function assay | 0.2 to 2 uM | 24 hrs | Induction of neurite outgrowth in mouse Neuro2a cells at 0.2 to 2 uM measured after 24 hrs by microscopic analysis | 31144814 |
| HCT116 | Function assay | 25 uM | 6 hrs | Inhibition of SIRT2 in human HCT116 cells assessed as increase in alpha-tubulin acetylation at 25 uM incubated for 6 hrs by DAPI staining-based laser scanning confocal microscopic analysis | 30986062 |
| HCT116 | Function assay | 50 uM | 6 hrs | Inhibition of SIRT2 in human HCT116 cells assessed as increase in alpha-tubulin acetylation at 50 uM incubated for 6 hrs by DAPI staining-based laser scanning confocal microscopic analysis | 30986062 |
| BxPC3 | Growth inhibition assay | 72 hrs | Growth inhibition of human BxPC3 cells after 72 hrs by CellTiter-Blue assay, GI50=13.3μM | 30986062 | |
| MDA-MB-468 | Growth inhibition assay | 72 hrs | Growth inhibition of human MDA-MB-468 cells after 72 hrs by CellTiter-Blue assay, GI50=15.7μM | 30986062 | |
| NCI-H23 | Growth inhibition assay | 72 hrs | Growth inhibition of human NCI-H23 cells after 72 hrs by CellTiter-Blue assay, GI50=16.4μM | 30986062 | |
| HCT116 | Function assay | 5 days | Inhibition of anchorage-independent cell growth in human HCT116 cells assessed as reduction in colony formation incubated for 5 days followed by compound re-addition and measured after 9 to 11 days by nitro blue tetrazolium chloride-based soft agar colony, GI50=16.7μM | 30986062 | |
| A549 | Growth inhibition assay | 72 hrs | Growth inhibition of human A549 cells after 72 hrs by CellTiter-Blue assay, GI50=17.3μM | 30986062 | |
| SW948 | Growth inhibition assay | 72 hrs | Growth inhibition of human SW948 cells after 72 hrs by CellTiter-Blue assay, GI50=19.2μM | 30986062 | |
| MCF7 | Growth inhibition assay | 72 hrs | Growth inhibition of human MCF7 cells after 72 hrs by CellTiter-Blue assay, GI50=37μM | 30986062 | |
| MDA-MB-231 | Growth inhibition assay | 72 hrs | Growth inhibition of human MDA-MB-231 cells after 72 hrs by CellTiter-Blue assay, GI50=42.8μM | 30986062 | |
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Thiomyristoyl (TM)是一种有效的、特异性SIRT2抑制剂，IC50为28 nM。它抑制SIRT1的IC50值为98 μM，而在浓度高达200 μM时，对SIRT3没有抑制作用。 | ||
|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Thiomyristoyl(TM)是一种具有高度选择性的SIRT2抑制剂。它不能有效地抑制SIRT3, SIRT5, SIRT6或SIRT7。在体外，它能显著地抑制细胞活性，其细胞毒性对癌细胞具有一定的选择性。TM在癌细胞中降低c-Myc肿瘤蛋白水平。在不同细胞系中，TM降低c-Myc丰度的能力与细胞系对TM的敏感性相关[1]。 | |||
|---|---|---|---|---|
| 细胞实验 | 细胞系 | 乳腺癌细胞系MCF-7 | ||
| 浓度 | 1, 5, 10, 25, 50 μM | |||
| 孵育时间 | 6 h | |||
| 方法 | 将人类MCF-7细胞培养在含10%（v/v）热灭活的FBS、1% penicillin-streptomycin的DMEM培养基中，用200 nM TSA处理6小时。通过western blot检测p53蛋白的乙酰化水平。 | |||
| 体内研究(In Vivo) | ||
| 体内研究活性 | TM的抗癌效果与它降低c-Myc水平的能力相关。TM对非癌细胞系和没有肿瘤的小鼠的效果非常有限[1]。 | |
|---|---|---|
| 动物实验 | Animal Models | 小鼠异种移植物模型 |
| Dosages | 1.5 mg/50 μL (IP); 0.75 mg/50 μL (IT) | |
| Administration | 腹腔注射或肿瘤内注射 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06147232 | Not yet recruiting | Nephropathy|Diabetic Nephropathies|Diabetes Mellitus Type 1|Albuminuria|Diabetic Complications Renal|Diabetic Complications Cardiovascular|Hypoxia |
Steno Diabetes Center Copenhagen|Juvenile Diabetes Research Foundation|King''s College London|Glostrup University Hospital Copenhagen |
August 2024 | Phase 4 |
| NCT06384157 | Not yet recruiting | Opioid Use Disorder |
Indivior Inc. |
May 2024 | Phase 2 |
化学信息&溶解度
| 分子量 | 581.85 | 分子式 | C34H51N3O3S |
| CAS号 | 1429749-41-6 | SDF | Download Thiomyristoyl SDF |
| Smiles | CCCCCCCCCCCCCC(=S)NCCCCC(C(=O)NC1=CC=CC=C1)NC(=O)OCC2=CC=CC=C2 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 100 mg/mL ( (171.86 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 100 mg/mL (171.86 mM) Water : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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