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CAS No.: 39777-61-2

TFEB activator 1/姜黄素类似物C1 Catalog No. CSN25353

Synonyms: Curcumin analog compound C1;Curcumin analog C1;GO-Y019

TFEB activator 1 is an orally effective, mTOR-independent activator of TFEB. It significantly promotes the nuclear translocation of Flag-TFEB with an EC50 of 2167 nM and enhances autophagy without inhibiting the mTOR pathway and has the potential for neurodegenerative diseases treatment. It also shows cytotoxic effect on HeLa, K562, MCF-7 and MDA-MB-231 cancer cell lines.

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描述Activation of TFEB (transcription factor EB), a master regulator of autophagy and lysosomal biogenesis, can ameliorate neurotoxicity and rescue neurodegeneration in animal models. TFEB activator 1 is a novel MTOR-independent TFEB activator. It significantly promoted phosphorylation of RPS6KB1 and MTOR, indicating that C1 enhanced autophagy without inhibiting the MTOR pathway. TFEB activator 1 (1 μM; 12 h) potently induced nuclear translocation of endogenous TFEB in N2a cells and it significantly promoted the nuclear translocation of Flag-TFEB with an EC₅₀ value of 2167 nM. The dissociation constant (K_D) of C1 to TFEB was determined to be 2.53 μM. In HeLa cells stably expressing Flag-TFEB, the levels of YWHA coimmunoprecipitated with Flag-TFEB significantly decreased after TFEB activator 1 (1 μM; 12 h) treatment compared with the control, suggesting that TFEB activator 1 could reduce TFEB-YWHA interaction independently of MTOR activity. TFEB activator 1 treatment dose-dependently increases the levels of LC3-II and SQSTM1/p62 (sequestosome 1) in N2a cells, and the effects require at least 9 h of treatment. However, 6 h of TFEB activator 1 treatment was sufficient to significantly promote TFEB nuclear translocation, indicating a delayed autophagy response via TFEB activation. The protein level of SQSTM1 (a target gene of TFEB) was significantly decreased by TFEB activator 1 (1 μM; 12 h), indicating that it enhances autophagic degradation of SQSTM1. Short-term oral administration of TFEB activator 1 (10 mg/kg and 25 mg/kg) dose-dependently increased the expression of LC3B-II and TFEB in the liver, frontal cortex and striatum of the brain. Meanwhile, TFEB activator 1 treatment dose-dependently increased the expression of LAMP1 in the frontal cortex^[1].
作用机制The binding site of TFEB activator 1 is likely located at the N-terminal Gly and Ala-rich domain of TFEB^[1].
参考文献

[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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.3974 mL
- 16.9869 mL
- 33.9738 mL
- 5 mM
- 0.6795 mL
- 3.3974 mL
- 6.7948 mL
- 10 mM
- 0.3397 mL
- 1.6987 mL
- 3.3974 mL

技术信息

CAS号

39777-61-2

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H18O3

运输

蓝冰

分子量

294.34

别名

Curcumin analog compound C1;Curcumin analog C1;GO-Y019;TFEB Activator 1;RPN-77612

溶解度

DMSO	120.0 mg/mL (407.7 mM) warming

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