VPS34-IN1

製品コードS7980 バッチS798001

印刷

化学情報

Chemical Structure Synonyms Vps34-IN-1 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C21H24ClN7O
分子量 425.91 CAS No. 1383716-33-3
Solubility (25°C)* 体外 DMSO 85 mg/mL (199.57 mM)
Ethanol 85 mg/mL (199.57 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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生物活性

製品説明 Vps34-IN1 is a potent and highly selective Vps34 inhibitor with IC50 of 25 nM invitro,which does not significantly inhibit the isoforms of class I as well as class II PI3Ks. Vps34-IN1 modulates autophagy.
in vitro Administration of VPS34-IN1 to cells induces a rapid dose-dependent dispersal of a specific PtdIns(3)P-binding probe from endosome membranes, within 1min, without affecting the ability of class I PI3K to regulate Akt. It can also induce a rapid ~50-60% loss of SGK3 phosphorylation within 1min. VPS34-IN1 has no inhibition to the SGK2 isoform that does not possess a PtdIns(3)P-binding PX domain[1].

プロトコル(参考用のみ)

キナーゼアッセイ In vitro Vps34 PI3K assay
The PI3K activity of recombinant Vps34–Vps15 complex expressed in insect cells is assayed in vitro via a radioactive liposome kinase assay. Liposomes are formed by extrusion of crude liver PtdIns through a 100nm filter membrane and incubates with 50ng of recombinant Vps34/15 for 30min at 1000 rev./min and 4°C. Assay buffer is 20mM Tris/HCl, pH7.4, 67mM NaCl, 10mM MnCl2, 0.02% CHAPS and 1mM DTT in the presence of 5μM ATP and 3μCi [γ-32P]ATP per reaction. Reactions are terminated by the addition of 500μl of chloroform/methanol/HCl (100:200:3.5, by vol.) and subsequently 180μl of chloroform and 300μl of 0.1M HCl to phase split reactions. The lower lipid-containing phase is retained and dried before the addition of chloroform. Reactions are spotted on to a Silica 60 TLC plate [activated with 1% potassium oxalate, 5mM EDTA and 50% (v/v) methanol] and separated by a solvent comprising methanol/chloroform/water/ammonium bicarbonate (47:60:11.2:2, by vol.). Radioactive incorporation is analysed by Fujifilm Image reader FLA-2000 and quantified by AIDA image analysis, IC50 values are determined by non-linear regression using Prism software.

カスタマーフィードバック

Data from [Data independently produced by , , Oncotarget, 2017, 8(24):38099-38112]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

An evolutionary-conserved VPS34-PIKfyve-TRPML1-Myosin II axis regulates the speed of amoeboid cell migration [ bioRxiv, 2024, 10.1101/2024.01.22.575998] PubMed: none
Class 3 PI3K coactivates the circadian clock to promote rhythmic de novo purine synthesis [ Nat Cell Biol, 2023, 25(7):975-988] PubMed: 37414850
S-acylation of p62 promotes p62 droplet recruitment into autophagosomes in mammalian autophagy [ Mol Cell, 2023, 83(19):3485-3501.e11] PubMed: 37802024
Dihydroartemisinin-induced ferroptosis in acute myeloid leukemia: links to iron metabolism and metallothionein [ Cell Death Discov, 2023, 9(1):97] PubMed: 36928207
MEK inhibition overcomes chemoimmunotherapy resistance by inducing CXCL10 in cancer cells [ Cancer Cell, 2022, S1535-6108(21)00662-0] PubMed: 35051357
Inhibition of Vps34 and p110δ PI3K Impairs Migration, Invasion and Three-Dimensional Spheroid Growth in Breast Cancer Cells [ Int J Mol Sci, 2022, 23-169008] PubMed: 36012280
Bortezomib abrogates temozolomide-induced autophagic flux through an ATG5 dependent pathway [ Front Cell Dev Biol, 2022, 10:1022191] PubMed: 36619857
Inhibition of lipid kinase PIKfyve reveals a role for phosphatase Inpp4b in the regulation of PI(3)P-mediated lysosome dynamics through VPS34 activity [ J Biol Chem, 2022, 298(8):102187] PubMed: 35760104
ALFY localizes to early endosomes and cellular protrusions to facilitate directional cell migration [ J Cell Sci, 2022, jcs.259138] PubMed: 35099014
Dynamic glucose uptake, storage, and release by human microvascular endothelial cells [ Mol Biol Cell, 2022, 33(12):ar106] PubMed: 35921166

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。