39777-61-2
39777-61-2 结构式
基本信息
(1E,4E)-1,5(2 -甲氧基苯基)-1,4-戊二烯-3-酮
TFEB activator 1
Curcumin analog C1
Curcumin analog compound C1
Curcumin analog C1(TFEB activator 1 )
(1E,4E)-1,5-Bis(2-Methoxyphenyl)penta-1
1,5-Bis-(2-methoxy-phenyl)-penta-1,4-dien-3-one
(1E,4E)-1,5-Bis(2-Methoxyphenyl)penta-1,4-dien-3-one
(1E,4E)-1,5-Bis(2-methoxyphenyl)-1,4-pentadien-3-one
1,4-Pentadien-3-one, 1,5-bis(2-Methoxyphenyl)-, (1E,4E)-
物理化学性质
常见问题列表
| Target | Value |
|
TFEB
() |
TFEB activator 1 (Compound C1) activates TFEB (transcription factor EB) by directly binding to TFEB and promotes its entry into the nucleus, without affecting TFEB phosphorylation or inhibiting the activities of MTOR and MAPK1/ERK2-MAPK3/ERK1.
TFEB activator 1 (1 μM; for 12 h) significantly increases the levels of LC3B-II, the lipidated and phagophore- or autophagosome-associated form of MAP1LC3B/LC3B (microtubule-associated protein 1 light chain 3 β) in N2a cells.
TFEB activator 1 (0.2-1 μM) dose-dependently increases the levels of LC3-II and SQSTM1/p62 (sequestosome 1) in N2a cells.
Western Blot Analysis
| Cell Line: | N2a cells |
| Concentration: | 0, 0.2, 0.4, 0.6, 0.8 and 1 μM |
| Incubation Time: | 12 hours |
| Result: | Treatment dose-dependently increased the levels of LC3-II and SQSTM1/p62 (sequestosome 1). |
The medium lethal dose (LD
50
) value of TFEB activator 1 (Compound C1) is 175 mg/kg in the acute toxicity assay (single-dose i.v. tail vein injection; in rats) .
Short-term oral administration of TFEB activator 1 (low dosage 10 mg/kg and high dosage 25 mg/kg; for 24 h) dose-dependently increases the expression of LC3B-II and TFEB in the liver, frontal cortex and striatum of the brain.
Chronic administration of TFEB activator 1 (10 mg/kg per day; orally administered by gavage) activates TFEB and enhances autophagy in rat brains.
| Animal Model: | Adult male Sprague-Dawley (SD) rats weighing 350 to 400 g |
| Dosage: | 10 mg/kg and 25 mg/kg |
| Administration: | Short-term oral administration; for 24 hours |
| Result: | Activated TFEB and enhanced autophagy and lysosome biogenesis in rat brain. |
| Animal Model: | Adult male Sprague-Dawley (SD) rats weighing 350 to 400 g |
| Dosage: | 10 mg/kg |
| Administration: | Chronic oral administration; daily; for 21 days |
| Result: | Activated TFEB and enhanced autophagy in rat brains. |