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| | PIK-III Basic information |
| Product Name: | PIK-III | | Synonyms: | PIK-III;Vps34-PIK-III;4'-(Cyclopropylmethyl)-N2-4-pyridinyl[4,5'-bipyrimidine]-2,2'-diamine;Vps34 inhibitor PIK-III;[4,5'-Bipyrimidine]-2,2'-diamine, 4'-(cyclopropylmethyl)-N2-4-pyridinyl-;PI3K,Autophagy,Vps34 PIK III,Vps-34-PIK-III,Inhibitor,Phosphoinositide 3-kinase,Vps34PIKIII,inhibit;PIK-Ⅲ;4'-(Cyclopropylmethyl)-N2-(pyridin-4-yl)-[4,5'-bipyrimidine]-2,2'-diamine | | CAS: | 1383716-40-2 | | MF: | C17H17N7 | | MW: | 319.36 | | EINECS: | | | Product Categories: | | | Mol File: | 1383716-40-2.mol |  |
| | PIK-III Chemical Properties |
| Boiling point | 657.4±65.0 °C(Predicted) | | density | 1.380±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | ≥31.9 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH | | form | solid | | pka | 6.19±0.26(Predicted) | | color | White to off-white |
| | PIK-III Usage And Synthesis |
| Biological Activity | pik-iii is a vps34 inhibitor and is able to inhibit autophagy.vps34 kinase has been found to be responsible for synthesis and deposition of phosphatidylinositol-3-phosphate at autophagosome formation sites, resulting in the recruitment of ptdins(3)p-binding proteins. | | in vitro | in previous study, pik-iii was identified as a selective inhibitor of vps34 binding in a hydrophobic pocket. in addition, pik-iii could acutely inhibit the autophagy and lipidation of lc3, which led to the stabilization of autophagy substrates. moreover, substrates such as ncoa4 were identified by conducting ubiquitin-affinity proteomic assay on pik-iii-treated cells, which accumulated in cells with atg7 deficience and co-localized with autolysosomes. ncoa4 could bind ferritin heavy chain-1 directly to target the iron-binding ferritin complex following starvation or iron depletion [1]. | | in vivo | animal study showed that pik-iii-treated ncoa4-/- mice had a profound accumulation of iron in splenic macrophages that were important for iron reutilization from engulfed red blood cells. in summary, such in vivo results provided a novel mechanism for selective autophagy of ferritin and revealed a previously untouched role for autophagy and ncoa4 in the control of in-vivo iron homeostasis [1]. | | IC 50 | 18 nm for vps34 | | references | [1] dowdle we et al. selective vps34 inhibitor blocks autophagy and uncovers a role for ncoa4 in ferritin degradation and iron homeostasis in vivo. nat cell biol. 2014 nov;16(11):1069-79. |
| | PIK-III Preparation Products And Raw materials |
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