产品
编 号：F618156
分子式：C29H26ClNO2S2
分子量：520.11
分子式：C29H26ClNO2S2
分子量：520.11
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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结构图
CAS No: 2449093-46-1
产品详情
生物活性：
LV-320 is a potent and uncompetitive ATG4B inhibitor with an IC50 of 24.5?μM and a Kd of 16?μM. LV-320 inhibits ATG4B enzymatic activity, blocks autophagic flux in cells, and is stable, non-toxic and active in vivo.
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. Thetreatment 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.
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.
LV-320 is a potent and uncompetitive ATG4B inhibitor with an IC50 of 24.5?μM and a Kd of 16?μM. LV-320 inhibits ATG4B enzymatic activity, blocks autophagic flux in cells, and is stable, non-toxic and active in vivo.
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. Thetreatment 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.
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.
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