GlpBio

TFEB activator 1

目录号: GC39530纯度: >99.50%同义词: (1E,4E)-1,5-二(2-甲氧基)-1,4-二烯基-3-戊酮,Curcumin analog C1
TFEB activator 1是一种口服有效、不依赖mTOR的TFEB激活剂，能够显著促进Flag-TFEB的核易位，EC50值为2167nM。
TFEB activator 1
Cas No.: 39777-61-2
规格价格库存数量操作
5mg¥455.00现货
1
10mg¥700.00现货
1
25mg¥1,400.00现货
1
50mg¥2,450.00现货
1
100mg¥3,850.00现货
1
电话: 400-920-5774Email: sales@glpbio.cn

文献被引

本产品暂无引用记录;以下为 GlpBio 产品在 Nature / Cell / Science 等顶刊的客户引用样例
  • Nature cover
    Nature
    641, 529–536 (2025)
  • Nature cover
    Nature
    628, 630–638 (2024)
  • Nature cover
    Nature
    632, 686–694 (2024)
  • Nature cover
    Nature
    618, 1017–1023 (2023)
  • Nature cover
    Nature
    610, 366–372 (2022)
  • Cell cover
    Cell
    187(9):2288-2304 (2024)
  • Cell cover
    Cell
    183(7):1867-1883 (2020)
  • Science cover
    Science
    388(6745) (2025)
  • Science cover
    Science
    387(6739) (2025)
  • Science cover
    Science
    387(6734) (2025)
  • Cell Research cover
    Cell Research
    35, 97–116 (2025)
  • Cell Research cover
    Cell Research
    34, 683–706 (2024)
  • Cell Research cover
    Cell Research
    33, 273–287 (2023)
  • Cell Research cover
    Cell Research
    33, 546–561 (2023)
  • Cell Research cover
    Cell Research
    33, 904–922 (2023)
  • Cell Research cover
    Cell Research
    31, 1291–1307 (2021)

产品描述 Description

TFEB activator 1 is an orally effective, mTOR-independent activator of TFEB that significantly promotes the nuclear translocation of Flag-TFEB with an EC50 of 2167nM[1]. Transcription factor EB (TFEB) is a master regulator of lysosomal biogenesis and autophagy that coordinates cellular responses to nutrient availability and stress[2]. Once activated, TFEB induces lysosomal and autophagy gene expression, and enhances cellular clearance of aggregates and damaged organelles to maintain metabolic homeostasis[3]. TFEB activator 1 is commonly used in research on neurodegenerative diseases, such as Alzheimer's disease[4][5].

In vitro, TFEB activator 1 (1μM; 12h pretreatment; 15min co-treatment; 6h incubation) enhanced TFEB nuclear translocation, increased LC3B-II and SQSTM1/p62 protein levels, improved cell viability, prevented apoptosis, and promoted mitophagy in 6-OHDA/AA-treated SH-SY5Y cells[6].

References:
[1] Song JX, Sun YR, Peluso I, et al. A novel curcumin analog binds to and activates TFEB in vitro and in vivo independent of MTOR inhibition. Autophagy. 2016;12(8):1372-1389.
[2] Settembre C, Di Malta C, Polito VA, et al. TFEB links autophagy to lysosomal biogenesis. Science. 2011;332(6036):1429-1433.
[3] Franco-Juárez B, Coronel-Cruz C, Hernández-Ochoa B, et al. TFEB; Beyond Its Role as an Autophagy and Lysosomes Regulator. Cells. 2022;11(19):3153.
[4] Xie YQ, Zhu L, Wang XT.TFEB activator 1 enhances autophagic degradation of oligomeric amyloid-β in microglia. Sheng Li Xue Bao. 2024;76(3):365-375
[5] Perrone L, Squillaro T, Napolitano F, Terracciano C, Sampaolo S, Melone MAB. The Autophagy Signaling Pathway: A Potential Multifunctional Therapeutic Target of Curcumin in Neurological and Neuromuscular Diseases. Nutrients. 2019;11(8):1881.
[6] Zhuang XX, Wang SF, Tan Y, et al. Pharmacological enhancement of TFEB-mediated autophagy alleviated neuronal death in oxidative stress-induced Parkinson's disease models. Cell Death Dis. 2020;11(2):128.
[7] Song JX, Malampati S, Zeng Y, et al. A small molecule transcription factor EB activator ameliorates beta-amyloid precursor protein and Tau pathology in Alzheimer's disease models. Aging Cell. 2020;19(2):e13069.

TFEB activator 1是一种口服有效、不依赖mTOR的TFEB激活剂，能够显著促进Flag-TFEB的核易位，EC50值为2167nM[1]。转录因子EB（TFEB）是溶酶体生物发生和自噬的主要调控因子，可协调细胞对营养供应和应激的反应[2]。TFEB被激活后，可诱导溶酶体和自噬基因表达，增强细胞内聚物和受损细胞器的清除，从而维持代谢稳态[3]。TFEB activator 1常用于神经退行性疾病，如阿尔茨海默病的研究[4][5]。

在体外，TFEB activator 1（1μM；12小时预处理；15分钟共处理；6小时孵育）可增强6-OHDA/AA处理的SH-SY5Y细胞中TFEB的核易位，增加LC3B-II和SQSTM1/p62蛋白水平，提高细胞活力，抑制细胞凋亡，并促进线粒体自噬[6]。

在体内，TFEB activator 1（10mg/kg/天；灌胃；4个月）可减少5xFAD小鼠的全长APP、CTF-α/β和Aβ病理改变，增加TFEB核易位及自噬-溶酶体标志物（LC3B-II、LAMP1、CTSD），并恢复突触可塑性和记忆缺陷[7]。

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

SH-SY5Y cells

Preparation Method

SH-SY5Y cells were maintained in DMEM/F-12 Media containing 10% fetal bovine serum in a 5% CO2 atmosphere at 37℃. Mycoplasma contamination testing status was negative. The cells were pretreated with TFEB activator 1 for 12h, and then treated with 6-OHDA/AA in the presence or absence of TFEB activator 1 for 15min, after which the medium was removed and replaced with DMEM F12 with or without TFEB activator 1 for another 6h. Mitochondrial membrane potential was determined by flow cytometer. The intralysosomal PH was estimated using LysoSensor and LysoTracker. Cell viability was determined by CCK8 assay. The apoptosis of the SH-SY5Y cells was determined with Annexin V/propidium iodide (PI) staining kit by flow cytometry. Cells were collected for Western blot analysis.

Reaction Conditions

1μM; 12h pretreatment; 15min co-treatment; 6h incubation

Applications

TFEB activator 1 increased LC3B-II and SQSTM1/p62 protein levels, improved cell viability, and promoted mitophagy in 6-OHDA/AA-treated SH-SY5Y cells.
Animal experiment [2]:

Animal models

5xFAD mice

Preparation Method

5xFAD mice were maintained at 23±2°C and 60±15% relative humidity with free access to feed and water. Two-month-old 5xFAD mice (male and female, n=10-14 per group) were treated daily with vehicle (1% CMC-Na) or TFEB activator 1 (10mg/kg) in 1% CMC-Na by oral gavage for 4 months. Contextualfear conditioning (CFC) was used to evaluate the fear memory reconsolidation of 5xFAD mice after treatment. After decapitation, mouse brain was quickly dissected and placed in sucrose-substituted ice-cold artificial cerebrospinal fluid for Electrophysiological recordings with microelectrode array recording system. And half brain tissues were lysed for Western blotting analysis and fixed for Immunohistochemistry analysis.

Dosage form

10mg/kg/day;oral gavage; 4 months

Applications

TFEB activator 1 reduced full-length APP, CTF-α/β, and Aβ pathology, increased TFEB nuclear translocation and autophagy-lysosome markers (LC3B-II, LAMP1, CTSD), and restored synaptic plasticity and memory deficits in 5xFAD mice.

References:
[1] Zhuang XX, Wang SF, Tan Y, et al. Pharmacological enhancement of TFEB-mediated autophagy alleviated neuronal death in oxidative stress-induced Parkinson's disease models. Cell Death Dis. 2020;11(2):128.
[2] Song JX, Malampati S, Zeng Y, et al. A small molecule transcription factor EB activator ameliorates beta-amyloid precursor protein and Tau pathology in Alzheimer's disease models. Aging Cell. 2020;19(2):e13069.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
39777-61-2
同义词
(1E,4E)-1,5-二(2-甲氧基)-1,4-二烯基-3-戊酮,Curcumin analog C1
SMILES
O=C(/C=C/C1=CC=CC=C1OC)/C=C/C2=CC=CC=C2OC
分子式
C19H18O3
分子量
294.34 g/mol
溶解性
DMSO: 125 mg/mL (424.68 mM)
保存条件
Store at -20°C,unstable in solution, ready to use.
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°C，然后在超声波浴中震荡一段时间。
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。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol