Shelf life (days): 1460.0
Formulation: A crystalline solid
Formal Name: N-2-pyridinyl-2-pyridinecarbothioamide
Purity: ≥98%
Formula Markup: C11H9N3S
Formula Weight: 215.3
CAS Number: 39122-38-8
Notes: NSC 185058 is an inhibitor of ATG4B, a cysteine protease that activates LC3B during the initiation of autophagy.{37384} It inhibits ATG4B cleavage of LC3B-GST (IC50 = 51 µM) and reduces LC3B lipidation induced by starvation in Saos-2 cells. NSC 185058 (100 µM) reduces starvation-induced autophagy and prevents autophagic vacuole formation in Saos-2 and MDA-MB-468 cells. It decreases phosphorylation of ribosomal protein S6 (RPS6) only marginally and does not affect phosphatidylinositol 3-kinase (PI3K) activity, indicating a direct role on ATG4B rather than through the mammalian target of rapamycin (mTOR) and PI3K signaling pathways. NSC 185058 (100 mg/kg) decreases autophagic vacuoles in vivo in mouse liver, inhibits tumor growth in an osteosarcoma nude mouse xenograft model, and decreases the number of autophagic vacuoles in osteosarcoma tumors.
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