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PIK-III Sale

(Synonyms: Vacuolar Protein Sorting 34 Inhibitor 2, Vps34-IN2, Vps34 Inhibitor 2) 目录号 : GC14679

A selective inhibitor of Vps34

PIK-III Chemical Structure

Cas No.:1383716-40-2

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,107.00
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2mg
¥630.00
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5mg
¥1,170.00
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10mg
¥1,890.00
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25mg
¥4,230.00
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50mg
¥7,560.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

IC50: 18 nM for VPS34

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].

Clinical trial: Up to now, PIK-III is still in the preclinical development stage.

Reference:
[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.

Chemical Properties

Cas No. 1383716-40-2 SDF
别名 Vacuolar Protein Sorting 34 Inhibitor 2, Vps34-IN2, Vps34 Inhibitor 2
化学名 4'-(cyclopropylmethyl)-N2-(pyridin-4-yl)-[4,5'-bipyrimidine]-2,2'-diamine
Canonical SMILES NC1=NC=C(C2=NC(NC3=CC=NC=C3)=NC=C2)C(CC4CC4)=N1
分子式 C17H17N7 分子量 319.36
溶解度 ≥ 31.9mg/mL in DMSO 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 3.1313 mL 15.6563 mL 31.3126 mL
5 mM 0.6263 mL 3.1313 mL 6.2625 mL
10 mM 0.3131 mL 1.5656 mL 3.1313 mL
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