Atg4B-IN-2 是一种有效的竞争性Atg4B抑制剂，Ki为 3.1 μM，也具有降低PLA2的抑制能力，对 Atg4B 和 PLA2的IC50分别为 11 μM 和 3.5 μM。Atg4B-IN-2 通过细胞自噬 (Autophagy) 来增强抗去势抗性前列腺癌药物的抗癌活性。

Atg4B-IN-2 is a potent competitive Atg4B inhibitor with K i value of 3.1 μM, also possesses declining PLA 2 inhibitory potency, IC 50 s of 11 μM and 3.5 μM for Atg4B and PLA 2, respectively. Atg4B-IN-2 enhances the anticancer activity of anti-castration-resistant prostate cancer drugs via autophagy inhibition [1].

Atg4B-IN-2 (compound 21f) (1-10 μM; 2 hours) restores the p62 expression in cells treated with AF (amino acid-free) in a dose-dependent manner [1]. Atg4B-IN-2 (1 and 5 μM; 2 hours) decreases moderately autophagic vesicles at 1 μM, and almost completely inhibits autophagy at 5 μM [1]. Atg4B-IN-2 (5 μM; 2 hours) inhibits Abi-induced autophagy and significantly augments apoptotic cell death and sensitivity to Abi [1]. Western Blot Analysis Cell Line: LNCaP cells (incubated in AF medium) [1] Concentration: 1, 2, 5, 10 μM Incubation Time: 2 hours (then incubated in AFM for 24 or 3 hours) Result: Restored the p62 expression in cells treated with AF in a dose-dependent manner. Cell Autophagy Assay Cell Line: LNCaP cells (incubated in AF medium) [1] Concentration: 1 and 5 μM Incubation Time: 2 hours (then incubated in AFM for 24 or 3 hours) Result: Decreased moderately autophagic vesicles at 1 μM, and almost completely inhibited autophagy at 5 μM.

2765008-88-4

C21H30O3

330.46

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years