An inhibitor of ATG4B; inhibits ATG4B cleavage of LC3B-GST (IC50 = 51 µM) and reduces LC3B lipidation induced by starvation in Saos-2 cells; reduces starvation-induced autophagy and prevents autophagic vacuole formation in Saos-2 and MDA-MB-468 cells (100 µM); decreases autophagy in vivo in mouse liver

NSC 185058 – 1 mg

Brand:
Cayman
CAS:
39122-38-8
Storage:
-20
UN-No:
Non-Hazardous - /

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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SKU: 23957 - 1 mg Category:

Description

An inhibitor of ATG4B; inhibits ATG4B cleavage of LC3B-GST (IC50 = 51 µM) and reduces LC3B lipidation induced by starvation in Saos-2 cells; reduces starvation-induced autophagy and prevents autophagic vacuole formation in Saos-2 and MDA-MB-468 cells (100 µM); decreases autophagy in vivo in mouse liver, inhibits tumor growth in mouse xenograft model, and decreases the number of autophagic vacuoles in osteosarcoma tumors (100 mg/kg)

Formal name: N-2-pyridinyl-2-pyridinecarbothioamide

Synonyms: 

Molecular weight: 215.3

CAS: 39122-38-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Research Area|Cancer|Autophagy||Research Area|Cell Biology|Endomembrane System & Vesicular Trafficking|Autophagy||Research Area|Cell Biology|Proteolysis|Cytosolic & Secreted Proteases

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