Thiomyristoyl
(Synonyms: TM) 目录号 : GC17724
Thiomyristoyl是一种高效且特异性的SIRT2抑制剂（IC50 = 28 nM）。
Cas No.:1429749-41-6
Sample solution is provided at 25 µL, 10mM.
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Thiomyristoyl is a highly potent and specific SIRT2 inhibitor (IC50 = 28 nM) [1]. Thiomyristoyl forms a strong interaction with the catalytic site of SIRT2, competitively blocking the binding of natural substrates to NAD⁺, thereby significantly reducing the deacetylation levels of SIRT2-catalyzed substrates such as α-tubulin, p53, and NF-κB, thus affecting cellular metabolic homeostasis, stress response, and cell cycle regulation [2-3]. Thiomyristoyl is commonly used for its effects in neurodegenerative diseases, oncology, and colitis [4].
In A375 cells, Thiomyristoyl (50μM; 72h) increased sensitivity to cisplatin and exhibited increased accumulation of γ-H2AX and reduced EGFR-AKT-RAF-ERK1/2 pathway signaling compared to control cells [5]. In LNCaP cells, Thiomyristoyl (0.1-100μM; 72h) inhibits the deacetylation activity of SIRT2, blocks its mediated G1/S cell cycle transition, weakens cell proliferation, and promotes tumor cell apoptosis [6].
In dextran sulfate sodium-induced colitis mice model, Thiomyristoyl (5mg/kg; ip; 21d) alleviates colitis inflammation and tissue damage by inhibiting SIRT2 activity, weakening Th17 cell differentiation and pro-inflammatory signals such as IL-17A, p-STAT3, and p-NF-κB, restoring LDHA acetylation, and upregulating IL-10 [7]. In dextran sulfate sodium-induced colitis mice model, Thiomyristoyl (50mg/kg; ip; 10d) significantly improves inflammatory damage and disease activity index by inhibiting the deacetylation activity of SIRT2, alleviating symptoms such as colon shortening, weight loss, and increased mortality in colitis mice [8].
References:
[1]. Jing H, Hu J, He B, et al. A SIRT2-selective inhibitor promotes c-Myc oncoprotein degradation and exhibits broad anticancer activity[J]. Cancer cell, 2016, 29(3): 297-310.
[2]. Li Y, Han L, Fu Y, et al. The role of SIRT2 in homeostatic medicine and aging intervention[J]. Oral Science and Homeostatic Medicine, 2025.
[3]. Shenk T, Kulp III J L, Chiang L W. Drugs Targeting Sirtuin 2 Exhibit Broad-Spectrum Anti-Infective Activity[J]. Pharmaceuticals, 2024, 17(10): 1298.
[4]. Akter R, Afrose A, Rahman M R, et al. A comprehensive analysis into the therapeutic application of natural products as SIRT6 modulators in Alzheimer’s disease, aging, cancer, inflammation, and diabetes[J]. International journal of molecular sciences, 2021, 22(8): 4180.
[5]. Karwaciak I, Sałkowska A, Karaś K, et al. Targeting SIRT2 sensitizes melanoma cells to cisplatin via an EGFR-dependent mechanism[J]. International Journal of Molecular Sciences, 2021, 22(9): 5034.
[6]. Lin R, Yang Y, Wu E, et al. SIRT2 promotes cell proliferation and migration through mediating ERK1/2 activation and lactosylceramide accumulation in prostate cancer[J]. The Prostate, 2023, 83(1): 71-81.
[7]. Xu Y, Cai R, Zhao Z, et al. Thiomyristoyl ameliorates colitis by blocking the differentiation of Th17 cells and inhibiting SIRT2-induced metabolic reprogramming[J]. International Immunopharmacology, 2021, 90: 107212.
[8]. Hou D, Yu T, Lu X, et al. Sirt2 inhibition improves gut epithelial barrier integrity and protects mice from colitis[J]. Proceedings of the National Academy of Sciences, 2024, 121(18): e2319833121.
Thiomyristoyl是一种高效且特异性的SIRT2抑制剂（IC50 = 28 nM） [1]。Thiomyristoyl与SIRT2的催化位点形成强相互作用，竞争性阻断天然底物与NAD⁺的结合，从而显著降低SIRT2催化底物（如α-微管蛋白、p53和NF-κB）的去乙酰化水平，进而影响细胞代谢稳态、应激反应和细胞周期调控 [2-3]。硫代肉豆蔻酰常用于治疗神经退行性疾病、肿瘤和结肠炎 [4]。
在A375细胞中，与对照组细胞相比，Thiomyristoyl（50μM；72h）可提高细胞对cisplatin的敏感性，并表现出γ-H2AX积累增加和EGFR-AKT-RAF-ERK1/2信号通路活性降低 [5]。在LNCaP细胞中，Thiomyristoyl（0.1-100μM；72h）抑制SIRT2的去乙酰化活性，阻断其介导的G1/S细胞周期转换，减弱细胞增殖，并促进肿瘤细胞凋亡 [6]。
在dextran sulfate sodium诱导的小鼠结肠炎模型中，Thiomyristoyl（5mg/kg；ip；21d）通过抑制SIRT2活性、减弱Th17细胞分化和IL-17A、p-STAT3和p-NF-κB等促炎信号、恢复LDHA乙酰化以及上调IL-10，减轻结肠炎炎症和组织损伤 [7]。在dextran sulfate sodium诱导的小鼠结肠炎模型中，Thiomyristoyl（50mg/kg；ip；10d）通过抑制SIRT2的脱乙酰化活性，显著改善炎症损伤和疾病活动指数，缓解结肠炎小鼠的结肠缩短、体重减轻和死亡率增加等症状 [8]。
| Cell experiment [1]: | |
Cell lines | A375 cells |
Preparation Method | A375 cells (control and pretreated with Thiomyristoyl, 50μM, 72h) were seeded on 6-well plates. On the following day, cells were treated with 1 and 2μM cisplatin for 48h. Afterwards, the cells were harvested and lysed, and Western blotting was performed to detect the amount of histone γ-H2AX using γ-H2AX antibody. |
Reaction Conditions | 50μM; 72h |
Applications | Thiomyristoyl increased sensitivity to cisplatin and exhibited increased accumulation of γ-H2AX and reduced EGFR-AKT-RAF-ERK1/2 pathway signaling compared to control cells. |
| Animal experiment [2]: | |
Animal models | Dextran sulfate sodium-induced colitis mice model |
Preparation Method | Male C57BL/6J mice were randomly divided into three groups (control group, colitis group, and Thiomyristoyl group), with seven mice in each group. C57BL/6J mice had free access to drinking water containing 2.5% dextran sulfate sodium. Simultaneously, mice in the Thiomyristoyl group received daily intraperitoneal injections of Thiomyristoyl (5mg/kg). Mice were sacrificed after anesthesia. Blood samples from the eyes and spleen were collected to detect cytokines and T cells. The distance from the cecum to the anus was measured. The spleen was harvested for T cell detection. The colon was fixed in 4% paraformaldehyde solution for pathological and immunohistochemical examination. |
Dosage form | 5mg/kg; ip; 21d |
Applications | Thiomyristoyl alleviates colitis inflammation and tissue damage by inhibiting SIRT2 activity, weakening Th17 cell differentiation and pro-inflammatory signals such as IL-17A, p-STAT3, and p-NF-κB, restoring LDHA acetylation, and upregulating IL-10. |
References: | |
| 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 | 344 μL | 1.7201 mL | 3.4401 mL |
| 10 mM | 172 μL | 860 μL | 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。
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Quality Control & SDS
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- Purity: >98.50%
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