Thiomyristoyl

製品コードS8245 バッチS824501

印刷

化学情報

 Chemical Structure Synonyms TM Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C34H51N3O3S

分子量 581.85 CAS No. 1429749-41-6
Solubility (25°C)* 体外 DMSO 100 mg/mL (171.86 mM)
Ethanol (warmed with 50ºC water bath) 100 mg/mL (171.86 mM)
Water Insoluble
体内 (毎回新しく調製した物を用意してください)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 Thiomyristoyl (TM) is a potent and specific SIRT2 inhibitor with an IC50 of 28 nM. It inhibits SIRT1 with an IC50 value of 98 μM and does not inhibit SIRT3 even at 200 μM.
in vitro Thiomyristoyl(TM) is a highly selective SIRT2 inhibitor. It cannot efficiently inhibit SIRT3, SIRT5, SIRT6, or SIRT7. In vitro, it shows great inhibition of cell viability and its cytotoxicity is relatively selective toward cancer cells. TM decreases c-Myc oncoprotein level in cancer cells, the ability of TM to decrease c-Myc abundance in different cell lines correlates with the sensitivity of the cell lines to TM[1].
in vivo The anticancer effect of TM correlates with its ability to decrease c-Myc level. TM has limited effects on non-cancerous cells and tumor-free mice[1].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 breast cancer cell lines MCF-7
濃度 1, 5, 10, 25, 50 μM
反応時間 6 h
実験の流れ Human MCF-7 cells are grown in DMEM media contained 10% (vol/vol) heat-inactivated fetal bovine serum and 1% penicillin-streptomycin and treated with in the presence of 200 nM TSA for 6 hr. The acetylation level of p53 protein is determined by western blot using anti-acetyl-p53 (K382) antibody. β-actin serves as a loading control.
動物実験 動物モデル Mouse xenograft model
投薬量 1.5 mg/50 μL (IP); 0.75 mg/50 μL (IT)
投与方法 intraperitoneal (IP) or intra-tumor (IT) injections

参考

  • https://pubmed.ncbi.nlm.nih.gov/26977881/

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

Starvation-induced phosphorylation activates gasdermin A to initiate pyroptosis [ Cell Rep, 2024, 43(9):114728] PubMed: 39264808
VRK1 Kinase Activity Modulating Histone H4K16 Acetylation Inhibited by SIRT2 and VRK-IN-1 [ Int J Mol Sci, 2023, 24(5)4912] PubMed: 36902348
Effects of Dimerization on the Deacylase Activities of Human SIRT2 [ Biochemistry, 2023, 10.1021/acs.biochem.3c00381] PubMed: 37966275
Deacetylation of ATG4B promotes autophagy initiation under starvation [ Sci Adv, 2022, 8(31):eabo0412] PubMed: 35921421
Sirt2 Inhibition Enhances Metabolic Fitness and Effector Functions of Tumor-Reactive T Cells [ Cell Metab, 2020, 32(3):420-436.e12] PubMed: 32768387
SIRT1 inhibitors mitigate radiation-induced GI syndrome by enhancing intestinal-stem-cell survival [ Cancer Lett, 2020, 501:20-30] PubMed: 33359449
A novel role of SIRT2 in regulating gap junction communications via connexin-43 in bovine cumulus-oocyte complexes. [ J Cell Physiol, 2020, 10.1002] PubMed: 32039484

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。