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LV-320

Catalog No. T11896   CAS 2449093-46-1

LV-320 is a potent and uncompetitive ATG4B inhibitor with an IC 50 of 24.5 μM and a K d of 16 μM. LV-320 inhibits ATG4B enzymatic activity, blocks autophagic flux in cells, and is stable, non-toxic and active in vivo. These findings suggest that LV-320 will serve as a relevant chemical tool to study the various roles of ATG4B in cancer and other contexts [1].

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LV-320 Chemical Structure
LV-320, CAS 2449093-46-1
Pack Size Availability Price/USD Quantity
25 mg 6-8 weeks $ 1,430.00
50 mg 6-8 weeks $ 1,860.00
100 mg 6-8 weeks $ 2,675.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description LV-320 is a potent and uncompetitive ATG4B inhibitor with an IC 50 of 24.5 μM and a K d of 16 μM. LV-320 inhibits ATG4B enzymatic activity, blocks autophagic flux in cells, and is stable, non-toxic and active in vivo. These findings suggest that LV-320 will serve as a relevant chemical tool to study the various roles of ATG4B in cancer and other contexts [1].
Targets&IC50 ATG4B:(kd)16 μM , ATG4B:24.5 µM
In vitro LV-320 (0-120 μM; SKBR3, MCF7, JIMT1, and MDA-MB-231 cells) treatment leads to a dose-dependent increase in endogenous LC3B-II and protein p62 levels in all four cell lines [1]. 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 [1]. Western Blot Analysis [1] 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 [1] Cell Line: MDA-MB-231 cells Concentration: 120 μM Incubation Time: 48 hours Result: Blocked autophagic flux.
In vivo Administering LV-320 (100-200 mg/kg; oral gavage; three times over two days; GFP-LC3 mice) resulted in terminal blood and liver concentrations of 169 μM and 104 μM, respectively. This treatment significantly increased the accumulation of GFP-LC3 puncta and elevated LC3B-II protein levels in treated animals compared to controls, without causing notable toxicity at either dose [1]. The study utilized female GFP-LC3 mice aged 9-14 weeks [1], exploring the pharmacokinetics and the biological impact of LV-320 on autophagy-related markers.
Molecular Weight 520.11
Formula C29H26ClNO2S2
CAS No. 2449093-46-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 135 mg/mL (259.56 mM), Sonification is recommended.

TargetMolReferences and Literature

1. Bosc D, et al. A new quinoline-based chemical probe inhibits the autophagy-related cysteine protease ATG4B. Sci Rep. 2018 Aug 3;8(1):11653. doi: 10.1038/s41598-018-29900-x.

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Keywords

LV-320 2449093-46-1 Proteases/Proteasome Cysteine Protease LV 320 LV320 inhibitor inhibit

 

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