An inhibitor of ATG4B
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NSC 185058

Item No. 23957

Technical Information
Formal Name
N-2-pyridinyl-2-pyridinecarbothioamide
CAS Number
39122-38-8
Molecular Formula
C11H9N3S
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 2.5 mg/ml
λmax
234, 294, 340 nm
SMILES
S=C(C1=NC=CC=C1)NC2=NC=CC=C2
InChi Code
InChI=1S/C11H9N3S/c15-11(9-5-1-3-7-12-9)14-10-6-2-4-8-13-10/h1-8H,(H,13,14,15)
InChi Key
UGWOJXZJIZUKDP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    NSC 185058 is an inhibitor of ATG4B, a cysteine protease that activates LC3B during the initiation of autophagy.1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Akin, D., Wang, S.K., Habibzadegah-Tari, P., et alA novel ATG4B antagonist inhibits autophagy and has a negative impact on osteosarcoma tumors. Autophagy 10(11), 2021-2035 (2014).