Thiomyristoyl
(Synonyms: TM) 目录号 : GC17724
A potent and selective SIRT2 inhibitor
Cas No.:1429749-41-6
Sample solution is provided at 25 µL, 10mM.
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Thiomyristoyl is a potent and specific SIRT2 inhibitor with an IC50 of 28 nM.
Thiomyristoyl (TM) is a potent SIRT2-specific inhibitor with broad anticancer activity but little effect on non-cancerous cells. SIRT2-inhibition promotes c-Myc ubiquitination and degradation, suggesting the therapeutic potential of TM to target certain c-Myc-driven cancers. TM could inhibit SIRT2 with an IC50 of 28 nM, but inhibits SIRT1 with an IC50 value of 98 μM and does not inhibit SIRT3 even at 200 μM. TM inhibits three human breast cancer cell lines, MCF-7, MDA-MB-468, and MDA-MB-231[1].
TM inhibits tumor growth in mouse models of breast cancer. TM does not cause significant toxicity in mice and no significant weight loss is observed in TM-treated mice. S5H, the acetyl-a-tubulin level is moderately but statistically significantly increased in tumors from TM-treated mice compared with those from vehicle-treated mice, suggesting that TM indeed inhibits SIRT2 in vivo[1].
References:
[1]. Jing H, et al. A SIRT2-Selective Inhibitor Promotes c-Myc Oncoprotein Degradation and Exhibits Broad Anticancer Activity. Cancer Cell. 2016 Mar 14;29(3):297-310.
Cell experiment: | Cells are seeded into 96-well plates at 3,000–4,000 cells per well. After 24 hr, test compounds (Thiomyristoyl) are added to cells to final concentrations ranging from 1 to 50 μM. Cells are then incubated for 72 hr and cell viability is measured using the CellTiter-Blue viability assay. Relative cell viability in the presence of test compounds is normalized to the vehicle-treated controls after background subtraction. GraphPad Prism software is used to determine the IC50 values. Knockdown of SIRT1-7 in various cell lines is achieved by lentiviral infection[1]. |
References: [1]. Jing H, et al. A SIRT2-Selective Inhibitor Promotes c-Myc Oncoprotein Degradation and Exhibits Broad Anticancer Activity. Cancer Cell. 2016 Mar 14;29(3):297-310. | |
| Cas No. | 1429749-41-6 | SDF | |
| 别名 | TM | ||
| 化学名 | (S)-benzyl (1-oxo-1-(phenylamino)-6-tetradecanethioamidohexan-2-yl)carbamate | ||
| Canonical SMILES | O=C(N[C@H](C(NC1=CC=CC=C1)=O)CCCCNC(CCCCCCCCCCCCC)=S)OCC2=CC=CC=C2 | ||
| 分子式 | C34H51N3O3S | 分子量 | 581.37 |
| 溶解度 | ≥ 163mg/mL in DMSO | 储存条件 | Room temperature |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7201 mL | 8.6004 mL | 17.2007 mL |
| 5 mM | 0.344 mL | 1.7201 mL | 3.4401 mL |
| 10 mM | 0.172 mL | 0.86 mL | 1.7201 mL |
| 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） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 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GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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，
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 saline，混匀澄清。
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet