Description
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.
Product information
CAS Number: 2449093-46-1
Molecular Weight: 520.11
Formula: C29H26ClNO2S2
Chemical Name: 3-[({4-[(E)-2-(7-chloroquinolin-4-yl)ethenyl]phenyl}[(2-phenylethyl)sulfanyl]methyl)sulfanyl]propanoic acid
Smiles: OC(=O)CCSC(SCCC1C=CC=CC=1)C1C=CC(/C=C/C2C=CN=C3C=C(Cl)C=CC=23)=CC=1
InChiKey: PHENTWJNXGESKT-RMKNXTFCSA-N
InChi: InChI=1S/C29H26ClNO2S2/c30-25-12-13-26-23(14-17-31-27(26)20-25)9-6-22-7-10-24(11-8-22)29(35-19-16-28(32)33)34-18-15-21-4-2-1-3-5-21/h1-14,17,20,29H,15-16,18-19H2,(H,32,33)/b9-6+
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 135 mg/mL (259.56 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
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.
In Vivo:
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.
References:
- 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.
Products are for research use only. Not for human use.
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