Thymalfasin (Thymosin α1)是一种短链、高电荷且天然无序的免疫调节蛋白。
Cas No.:62304-98-7
Sample solution is provided at 25 µL, 10mM.
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Thymalfasin (Thymosin α1) is a short, highly charged, and inherently disordered protein with immunoregulatory effects[1]. Thymalfasin can increase the expression of major histocompatibility complex (MHC) antigens and β2 microglobulin on the cell surface, thereby increasing the expression of virus-specific antigens and inhibiting virus replication[2]. Thymalfasin has been widely used to inhibit tumor progression and alleviate inflammatory responses in cellular and animal models[3].
In vitro, Thymalfasin treatment for 24 hours inhibited SNK6 cell proliferation with an IC50 value of 1.334μmol/ml[4]. Treatment of HepG2 cells with 50μg/ml Thymalfasin for 12 hours induced cell cycle arrest and inhibited Akt phosphorylation at Ser473[5]. Treatment with 130μM Thymalfasin for 48h induced apoptosis and DNA damage in ZR-75-1 cells and MCF-7 cells[6].
In vivo, Thymalfasin, administered intraperitoneally at a dose of 0.6mg/kg/day for 5 consecutive days, improved survival and reduced tumor burden in MC38 cell-xenograft mouse models receiving hyperthermic intraperitoneal chemotherapy (HIPEC)[7]. In a mouse model of C. albicans infection, intraperitoneal injection of 200μg/kg/day Thymalfasin for 7 consecutive days alleviated C. albican-induced gastrointestinal inflammation, increased IL-22 levels, and reduced fungal growth in the liver[8].
References:
[1] Hoch K, Volk D E. Structures of thymosin proteins[J]. Vitamins and Hormones, 2016, 102: 1-24.
[2] Tao N, Xu X, Ying Y, et al. Thymosin α1 and its role in viral infectious diseases: the mechanism and clinical application[J]. Molecules, 2023, 28(8): 3539.
[3] Dominari A, Hathaway III D, Pandav K, et al. Thymosin alpha 1: a comprehensive review of the literature[J]. World journal of virology, 2020, 9(5): 67.
[4] Chen M, Jiang Y, Cai X, et al. Combination of Gemcitabine and Thymosin alpha 1 exhibit a better anti-tumor effect on nasal natural killer/T-cell lymphoma[J]. International Immunopharmacology, 2021, 98: 107829.
[5] Qin Y, Chen F D, Zhou L, et al. Proliferative and anti-proliferative effects of thymosin α1 on cells are associated with manipulation of cellular ROS levels[J]. Chemico-biological interactions, 2009, 180(3): 383-388.
[6] Guo Y, Chang H, Li J, et al. Thymosin alpha 1 suppresses proliferation and induces apoptosis in breast cancer cells through PTEN-mediated inhibition of PI3K/Akt/mTOR signaling pathway[J]. Apoptosis, 2015, 20(8): 1109-1121.
[7] Nevo N, Goldstein A L, Bar-David S, et al. Thymosin alpha 1 as an adjuvant to hyperthermic intraperitoneal chemotherapy in an experimental model of peritoneal metastases from colonic carcinoma[J]. International Immunopharmacology, 2022, 111: 109166.
[8] Bellet M M, Borghi M, Pariano M, et al. Thymosin alpha 1 exerts beneficial extrapulmonary effects in cystic fibrosis[J]. European Journal of Medicinal Chemistry, 2021, 209: 112921.
Thymalfasin (Thymosin α1)是一种短链、高电荷且天然无序的免疫调节蛋白[1]。Thymalfasin能增强细胞表面主要组织相容性复合体(MHC)抗原和β2微球蛋白的表达，从而提升病毒特异性抗原呈递效率并抑制病毒复制[2]。Thymalfasin已广泛应用于细胞和动物模型中抑制肿瘤进展及缓解炎症反应[3]。
在体外，Thymalfasin处理24小时可抑制SNK6细胞增殖，IC50值为1.334μmol/ml[4]。使用50μg/ml的Thymalfasin处理HepG2细胞12小时，能诱导细胞周期阻滞并抑制Akt蛋白Ser473位点的磷酸化[5]。以130μM的Thymalfasin处理ZR-75-1和MCF-7细胞48小时，可诱导细胞凋亡与DNA损伤[4]。
在体内，连续5日每日腹腔注射0.6mg/kg/day剂量的Thymalfasin，能提高接受腹腔热灌注化疗(HIPEC)的MC38移植瘤小鼠模型的生存率并减轻肿瘤负荷[7]。在白念珠菌感染小鼠模型中，连续7日每日腹腔注射200μg/kg/day剂量的Thymalfasin，可缓解白念珠菌诱导的胃肠道炎症，提升IL-22水平并减少肝脏中的真菌定植[8]。
| Cell experiment [1]: | |
Cell lines | MCF-7 cells |
Preparation Method | MCF-7 cells were routinely cultured in Dulbecco's modified Eagle's medium (DMEM), and supplemented with 10% (v/v) heat-inactivated fetal bovine serum (FBS), insulin (0.1units/ml), L-glutamine (2mM), sodium pyruvate (100mg/ml), nonessential amino acids (100µM), streptomycin (100mg/ml), and penicillin (100units/ml) in a humidified incubator at 37°C with 5% CO2. The cells were seeded in 96-well plates at an initial density of 5×10⁴ cells/well and cultured for 24h. After incubation, the cells were further cultured in medium containing different concentrations of Thymalfasin (40, 70, 100, 130, and 160μM) for 12, 24, 48, 72, and 96h, respectively. At the indicated time points (12, 24, 48, 72, and 96h), MTT was added to each well to a final concentration of 0.5mg/ml, which was then dissolved in 150μl dimethyl sulfoxide and measured at a wavelength of 490nm. |
Reaction Conditions | 40, 70, 100, 130, and 160μM; 12, 24, 48, 72, and 96h |
Applications | Baricitinib dose-dependently increased the viability of PDLSCs following lipopolysaccharide treatment. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice |
Preparation Method | Using an 18G 4cm-long plastic catheter, 1×108 C. albicans cells were dissolved in 200μl of physiological saline, and were intragastrically (ig) inoculated into C57BL/6 mice to establish a gastrointestinal infection model. Thymalfasin was administered intraperitoneally at a dose of 200μg/kg every day for 7 days. Samples from the mice's stomach and colon were collected for histopathological analysis. |
Dosage form | 200μg/kg/day for 7 days; i.p. |
Applications | Thymalfasin treatment significantly mitigated inflammation in the gastrointestinal tract of mice with C. albicans infection. |
References: | |
| Cas No. | 62304-98-7 | SDF | |
| 别名 | 胸腺法新; Thymosin α1 | ||
| Canonical SMILES | N-acetyl-Ser-Asp-Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val-Val-Glu-Glu-Ala-Glu-Asn | ||
| 分子式 | C129H215N33O55 | 分子量 | 3108.28 |
| 溶解度 | Water : 0.3 mg/mL (0.10 mM) | 储存条件 | Store at -20°C |
| 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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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 321.7 μL | 1.6086 mL | 3.2172 mL |
| 5 mM | 64.3 μL | 321.7 μL | 643.4 μL |
| 10 mM | 32.2 μL | 160.9 μL | 321.7 μL |
| 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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