1383716-40-2
1383716-40-2 structure
- Name: Vps34-PIK-III
- Chemical Name: pik-iii
- CAS Number: 1383716-40-2
- Molecular Formula: C17H17N7
- Molecular Weight: 319.36400
- Catalog: Signaling Pathways Autophagy Autophagy
- Create Date: 2018-04-06 13:16:44
- Modify Date: 2024-01-04 15:39:41
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Vps34-PIK-III is a potent and selective inhibitor of VPS34 with an IC50 of 18 nM.
| Name | pik-iii |
|---|---|
| Synonyms |
4'-cyclopropylmethyl-N2-pyridin-4-yl-[4,5']bipyrimidinyl-2,2'-diamine
4'-cyclopropylmethyl-N2-pyridin-4-yl-[4,5'] bipyrimidinyl-2,2'-diamine Vps34-PIK-III |
| Description | Vps34-PIK-III is a potent and selective inhibitor of VPS34 with an IC50 of 18 nM. |
|---|---|
| Related Catalog | |
| Target |
Vps34:18 nM (IC50) PI(3)Kδ:1.2 μM (IC50) PI(3)Kγ:3.04 μM (IC50) PI(3)Kα:3.96 μM (IC50) Autophagy |
| In Vitro | PIK-III is a selective inhibitor of VPS34 that binds a unique hydrophobic pocket not present in related kinases such as PI3Kα. PIK-III is at least 100-fold-selective for VPS34 over related lipid kinases such as PI3K and the protein kinase mTOR. PIK-III acutely inhibits autophagy and de novo lipidation of LC3, and leads to the stabilization of autophagy substrates. In H4 cells expressing the mCherry-GFP-LC3 reporter PIK-III inhibits the formation of mCherry-positive autolysosomes and increases the cytosolic signal of LC3 under basal conditions and when autophagy is induced with the mTOR inhibitor AZD8055. PIK-III prevents the turnover of GFP-tagged p62 under basal conditions and when autophagy is activated. PIK-III treatment leadsto an increase in the levels of LC3-I in H4 and PSN1 cells[2]. |
| In Vivo | The DFX-induced NCOA4-dependent turnover of FTH1 and FTL is blocked with PIK-III suggesting an autophagy-dependent process[2]. |
| References |
| Molecular Formula | C17H17N7 |
|---|---|
| Molecular Weight | 319.36400 |
| Exact Mass | 319.15500 |
| PSA | 102.50000 |
| LogP | 3.26110 |
| Storage condition | -20℃ |