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Synonyms | Vps34-IN-1 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C21H24ClN7O |
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分子量 | 425.91 | CAS No. | 1383716-33-3 | ||||||||
Solubility (25°C)* | 体外 | DMSO | 85 mg/mL (199.57 mM) | ||||||||
Ethanol | 35 mg/mL (82.17 mM) | ||||||||||
Water | Insoluble | ||||||||||
体内 (毎回新しく調製した物を用意してください) |
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* <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. |
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. |
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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]. |
キナーゼアッセイ | In vitro Vps34 PI3K assay | |
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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. |
Data from [Data independently produced by , , Oncotarget, 2017, 8(24):38099-38112]
Non-vesicular phosphatidylinositol transfer plays critical roles in defining organelle lipid composition [ EMBO J, 2024, 10.1038/s44318-024-00096-3] | PubMed: 38627600 |
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 |
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。
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