化合物 T11896
- CAS号:2449093-46-1
- 英文名:Propanoic acid, 3-[[[4-[2-(7-chloro-4-quinolinyl)ethenyl]phenyl][(2-phenylethyl)thio]methyl]thio]-
- 中文名:化合物 T11896
- CBNumber:CB88250483
- 分子式:C29H26ClNO2S2
- 分子量:520.11
- MOL File:2449093-46-1.mol
- 沸点 :718.4±60.0 °C(Predicted)
- 密度 :1.317±0.06 g/cm3(Predicted)
- 储存条件 :Store at -20°C
- 溶解度 :DMSO : 135 mg/mL (259.56 mM; Need ultrasonic)
- 酸度系数(pKa) :4.28±0.10(Predicted)
- 形态 :Solid
- 颜色 :Light yellow to yellow
化合物 T11896性质、用途与生产工艺
- 生物活性 LV-320 是一种有效且非竞争性的 ATG4B 抑制剂，其 IC50 值为 24.5 μM，Kd 值为 16 μM。 LV-320 抑制 ATG4B 的酶促活性，阻断细胞自噬，并且在体内稳定，无毒且有活性。
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靶点
IC50: 24.5 µM (ATG4B); Kd: 16 μM (ATG4B)
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体外研究
LV-320 (0-120 µM; SKBR3, MCF7, JIMT1, and MDA-MB-231 cells) treatment results in a dose-dependent increase in endogenous LC3B-II and protein p62 levels in all four cell lines.
LV-320 (120 µM; 48 hours; MDA-MB-231 cells) treatment results in an increase in LC3B-II, indicating that LV-320 blocks autophagic flux.Western Blot Analysis
Cell Line: SKBR3, MCF7, JIMT1, and MDA-MB-231 cells Concentration: 0 µM, 25 µM, 50 µM, 75 µM, 100 µM, or 120 µM Incubation Time: Result: Resulted in a dose-dependent increase in endogenous LC3B-II and protein p62 levels in all four cell lines. Cell Autophagy Assay
Cell Line: MDA-MB-231 cells Concentration: 120 µM Incubation Time: 48 hours Result: Blocked autophagic flux. -
体内研究
LV-320 (100-200 mg/kg; oral gavage; three times over two days; GFP-LC3 mice) treatment results in a terminal blood level of 169 µM and a liver level of 104 µM. The expression of GFP-LC3 puncta is significantly greater accumulation in LV-320 treated animals compared to controls. LC3B-II protein is also increased in LV-320-treated animals. The treatment do not cause significant toxicity in mice at either dose.
Animal Model: GFP-LC3 mice (females, 9-14 weeks) Dosage: 100 mg/kg or 200 mg/kg Administration: Oral gavage; three times over two days (Pharmacokinetic study) Result: Terminal blood levels were 169 µM and liver levels were 104 µM. LC3B-II protein level was also increased.
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