S130 是一种高亲和力、选择性的半胱氨酸蛋白酶 ATG4B 的抑制剂, IC₅₀ 值为 3.24 µM。S130 可以抑制自噬通量。

S130 is a high affinity, selective inhibitor of ATG4B (a major cysteine protease) with an IC 50 of 3.24 μM. S130 suppresses autophagy flux.

Solid

IC50: 3.24 μM (ATG4B)

S130 suppresses autophagy and activates apoptosis by inhibiting ATG4B, leads to enhanced cytotoxicity.
S130 (10 μM; 6 hours) suppresses autophagy at the early LC3 priming step or late autolysosome degradation stage.
S130 accumulates autolysosomes with more lipidated LC3.
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.
has not independently confirmed the accuracy of these methods. They are for refere

S130 (20 mg/kg; i.p.; daily; 3 weeks) suppresses tumor growth, and shows an efficient in vivo antitumor effect with a sound safety on vital organs.
has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : 125 mg/mL (322.61 mM; Need ultrasonic)配制储备液