| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| P421448-1ml |
1ml |
现货  |
|
| 英文别名 | VPS34-IN2[4,5'-Bipyrimidine]-2,2'-diamine,4'-(cyclopropylmethyl)-N2-4-pyridinyl- |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | PIK-III |
| 生化机理 | PIK-III (VPS34-IN2)是\u200bVPS34酶活性的选择性抑制剂，可抑制自噬和LC3的从头脂化，并导致自噬底物的稳定。VPS34 和 PI(3)Kδ 的 IC50 值分别为 0.018 μM 和 1.2 μM。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 磷脂酰肌醇 3-激酶催化亚基 3 型抑制剂 |
| 产品介绍 |
PIK-III (VPS34-IN2), 一种选择性VPS34酶活性的抑制剂，抑制细胞自噬以及LC3的重新脂化，稳定自噬底物。其对VPS34和 PI(3)Kδ的IC50值分别为0.018 μM和1.2 μM。 Information PIK-III (VPS34-IN2), which is a selective inhibitor of VPS34 enzymatic activity, inhibitsautophagyand de novo lipidation of LC3 and leads to the stabilization of autophagy substrates. The IC50 values for VPS34 and PI(3)Kδ are 0.018 μM and 1.2 μM respectively. Targets Vps34 (Cell-free assay); PI3Kδ (Cell-free assay) 0.018μM; 1.2μM In vitro VPS34 enzymatic function is essential for LC3 lipidation in mammalian cells and PIK-III is a robust inhibitor of autophagy and LC3 lipidation in mammalian cells.In H4 cells, PIK-III inhibits the formation of autolysosomes and increases the cytosolic signal of LC3 under basal conditions and when autophagy is induced with the mTOR inhibitor AZD8055.In a CCCP-induced mitophagy model, PIK-III inhibits the clearance of mitochondria.PIK-III treatment leads to an increase in the levels of LC3-I in H4 and PSN1 cells.In Panc10.05 cells, PIK-III increases the levels of LC3-II in parallel with LC3-I suggesting a cell type-specific response. Cell Research(from reference) Cell lines：H4 cells/ HeLa cells Concentrations：2.5μM in H4 cells/5μM in Hela cells Incubation Time：overnight for H4 cells/12h for Hela cells |
| IC50 | PI3Kδ, IC50: 1.2μM |
|---|---|
| ALogP | 2.2 |
| HBD Count | 2 |
| Rotatable Bond | 5 |
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
| 分子类型 | 小分子 |
|---|---|
| IIUPAC Name | 4-(cyclopropylmethyl)-5-[2-(pyridin-4-ylamino)pyrimidin-4-yl]pyrimidin-2-amine |
| INCHI | 1S/C17H17N7/c18-16-21-10-13(15(23-16)9-11-1-2-11)14-5-8-20-17(24-14)22-12-3-6-19-7-4-12/h3-8,10-11H,1-2,9H2,(H2,18,21,23)(H,19,20,22,24) |
| InChi Key | XXSDLQLNIVFIJI-UHFFFAOYSA-N |
| Smiles | C1CC1CC2=NC(=NC=C2C3=NC(=NC=C3)NC4=CC=NC=C4)N |
| Isomeric SMILES | C1CC1CC2=NC(=NC=C2C3=NC(=NC=C3)NC4=CC=NC=C4)N |
| PubChem CID | 67983123 |
| 分子量 | 319.36 |
| DMSO(mg / mL) Max Solubility | 63 |
|---|---|
| DMSO(mM) Max Solubility | 197.2695391 |
| Water(mg / mL) Max Solubility | ＜1 |
| 分子量 | 319.400 g/mol |
| XLogP3 | 2.000 |
| 氢键供体数Hydrogen Bond Donor Count | 2 |
| 氢键受体数Hydrogen Bond Acceptor Count | 7 |
| 可旋转键计数Rotatable Bond Count | 5 |
| 精确质量Exact Mass | 319.155 Da |
| 单同位素质量Monoisotopic Mass | 319.155 Da |
| 拓扑极表面积Topological Polar Surface Area | 103.000 Ų |
| 重原子数Heavy Atom Count | 24 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 396.000 |
| 同位素原子数Isotope Atom Count | 0 |
| 定义的原子立体中心计数Defined Atom Stereocenter Count | 0 |
| 未定义的原子立体中心计数Undefined Atom Stereocenter Count | 0 |
| 定义的键立体中心计数Defined Bond Stereocenter Count | 0 |
| 未定义的键立体中心计数Undefined Bond Stereocenter Count | 0 |
| 所有立体化学键的总数The total count of all stereochemical bonds | 0 |
| 共价键合单元计数Covalently-Bonded Unit Count | 1 |
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