VPS34-IN1

Catalog No.S7980 Synonyms: Vps34-IN-1

VPS34-IN1 Chemical Structure

Molecular Weight(MW): 425.91

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.

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  • C. Lysosomal and endosomal inhibition selectively targets Tsc2−/− MEFs. Proliferation of Tsc2+/+ and Tsc2−/− MEFs treated with vehicle control (DMSO), CQ (5uM), Vps34 inhibitor (SAR405; 1uM) or the combination for 72 hours (crystal violet staining). D. Confirmation of selective growth inhibition using VPS34-IN1 inhibitor. Proliferation of Tsc2+/+ and Tsc2−/− MEFs treated with vehicle control (DMSO), CQ (5uM), VPS34-IN1 (500nM) or the combination for 72 hours (crystal violet staining). Two-sample t-test was carried out between CQ and SAR405 and each drug alone. Results are representative of three independent experiments. Bar graph represent means ±SD.

    Oncotarget, 2017, 8(24):38099-38112. VPS34-IN1 purchased from Selleck.

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Biological Activity

Description 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.
Targets
Vps34 [1]
(Cell-free assay)
25 nM
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].

Protocol

Solubility (25°C)

In vitro DMSO 85 mg/mL (199.57 mM)
Ethanol 85 mg/mL (199.57 mM)
Water 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.

Chemical Information

Molecular Weight 425.91
Formula

C21H24ClN7O

CAS No. 1383716-33-3
Storage powder
Synonyms Vps34-IN-1

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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PI3K Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID