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LV-320 Sale

目录号 : GC65432

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。

LV-320 Chemical Structure

Cas No.:2449093-46-1

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥4,634.00
现货
5mg
¥4,050.00
现货
10mg
¥6,750.00
现货
50mg
¥20,250.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

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[1].

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[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].

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[1].

[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.

Chemical Properties

Cas No. 2449093-46-1 SDF Download SDF
分子式 C29H26ClNO2S2 分子量 520.11
溶解度 DMSO : 135 mg/mL (259.56 mM; Need ultrasonic) 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 1.9227 mL 9.6134 mL 19.2267 mL
5 mM 0.3845 mL 1.9227 mL 3.8453 mL
10 mM 0.1923 mL 0.9613 mL 1.9227 mL
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Research Update

A new quinoline-based chemical probe inhibits the autophagy-related cysteine protease ATG4B

Sci Rep 2018 Aug 3;8(1):11653.PMID:30076329DOI:PMC6076261

The cysteine protease ATG4B is a key component of the autophagy machinery, acting to proteolytically prime and recycle its substrate MAP1LC3B. The roles of ATG4B in cancer and other diseases appear to be context dependent but are still not well understood. To help further explore ATG4B functions and potential therapeutic applications, we employed a chemical biology approach to identify ATG4B inhibitors. Here, we describe the discovery of 4-28, a styrylquinoline identified by a combined computational modeling, in silico screening, high content cell-based screening and biochemical assay approach. A structure-activity relationship study led to the development of a more stable and potent compound LV-320. We demonstrated that 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.