货号:A370554 同义名: 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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快速发货 顺丰冷链运输,1-2 天到达
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技术支持
免费溶解
产品名称 | Autophagy ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
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SBI-0206965 |
+++
ULK2, IC50: 711 nM ULK1, IC50: 108 nM |
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Hydroxychloroquine sulfate | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Valproic acid sodium | ✔ | HDAC | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||
PFK-015 |
++
PFKFB3, IC50: 207 nM |
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MRT68921 hydrochloride |
++++
ULK2, IC50: 1.1 nM ULK1, IC50: 2.9 nM |
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ROC-325 | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Autophinib |
+++
Autophagy, IC50: 40 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Lys05 | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
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 (KD) 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]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.40mL 0.68mL 0.34mL |
16.99mL 3.40mL 1.70mL |
33.97mL 6.79mL 3.40mL |
CAS号 | 39777-61-2 |
分子式 | C19H18O3 |
分子量 | 294.344 |
别名 | Curcumin analog C1;GO-Y019;RPN77612 |
运输 | 蓝冰 |
存储条件 |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 120 mg/mL(407.69 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |