| Description | S130 is a high affinity, selectiveATG4B (a major cysteine protease) inhibitor (IC50 of 3.24 μM).It suppresses autophagy flux. |
| In vitro | S130 suppresses autophagy and activates apoptosis by inhibiting ATG4B, leads to enhanced cytotoxicity. S130 (0-25 μM; 48 hours) induces cell death through inhibiting the activity of ATG4B at a dose higher than 6.3 μM. And such cytotoxicity might not cause cell death through necroptosis. Nutrient deprivation enhances S130-induced cytotoxicity. S130 (0-10μM; 24 hours) suppresses approximately 79% of the cleavage of full-length LC3-GST at the 10 μM, while no substrates were processed in ATG4B KO cells. S130 displays obvious inhibitory effects on ATG4B. |
| In vivo | Tumor growth suppressed by S130 (20 mg/kg; i.p.; daily; 3 weeks), S130 shows an efficient in vivo antitumor effect with a sound safety on vital organs. |
| Target activity | ATG4B:3.24 µM |
| molecular weight | 387.47 |
| Molecular formula | C24H25N3O2 |
| CAS | 1160852-22-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 125 mg/mL (322.61 mM), Sonication is recommended. |
| References | 1. Fu Y, et al. Discovery of a small molecule targeting autophagy via ATG4B inhibition and cell death of colorectal cancer cells in vitro and in vivo. Autophagy. 2018 Sep 20:1-17. |