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

Thiomyristoyl Chemical Structure

CAS: 1429749-41-6

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 2530.71 现货
2mg RMB 1204.74 现货
5mg RMB 2212.24 现货
25mg RMB 7125.37 现货
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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

Sirtuin抑制剂选择性比较

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
SIRT2 [1]
(Cell-free assay)
28 nM
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
NCT06133153 Not yet recruiting
Lip; Anomaly
Croma-Pharma GmbH|Proinnovera GmbH
March 2024 Not Applicable
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
February 2024 Phase 4
NCT05505643 Not yet recruiting
Breast Cancer|Breast Neoplasm
Washington University School of Medicine|The Foundation for Barnes-Jewish Hospital|Varian Medical Systems
February 28 2024 Not Applicable
NCT05134740 Recruiting
Hodgkins Lymphoma|Non Hodgkins Lymphoma
Baylor College of Medicine|Center for Cell and Gene Therapy Baylor College of Medicine
January 2024 Phase 1

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)

体外溶解度
批次:

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

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次:

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

摩尔浓度计算器

质量 浓度 体积 分子量

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

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,: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: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: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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