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VPS34-IN1 PI3K inhibitor

Name: VPS34-IN1
Brand: Selleck Chemicals
SKU: S7980
Availability: InStock
Rating: 5 (36 reviews)

Cat.No.S7980

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. This compound modulates autophagy.

Chemical Structure

Molecular Weight: 425.91

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.78%

99.78

Related Targets	Akt mTOR AMPK GSK-3 ATM/ATR DNA-PK PDPK1 PTEN PP2A PDK PI4K PIKfyve MELK
Related Products	LY294002 3-Methyladenine (3-MA) Dactolisib (BEZ235) Pictilisib (GDC-0941) Wortmannin (SL-2052) Buparlisib (BKM120) PI-103 TGX-221 ZSTK474 Omipalisib (GSK2126458) A66 PF-04691502 PIK-75 HCl IC-87114 740 Y-P (PDGFR 740Y-P) AS-605240 Taselisib (GDC 0032) SAR405 Apitolisib (GDC-0980) PIK-90 AZD6482 Gedatolisib (PKI-587) HS-173 AS-252424 Eganelisib (IPI-549) VS-5584 (SB2343) GSK2636771 AZD8186 GSK1059615 Pilaralisib (XL147)

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
VERO-E6	Function assay	48 hrs	Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of VERO-E6 cells after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging, IC50=0.4μM	ChEMBL
VERO-E6	Toxicity assay	48 hrs	Toxicity CC50 against VERO-E6 cells determined at 48 hours by high content imaging (same conditions as 2_LEY without exposure to 0.01 MOI SARS CoV-2 virus), CC50=26.83μM	ChEMBL
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	425.91	Formula	C₂₁H₂₄ClN₇O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1383716-33-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Vps34-IN-1			Smiles	CC(C)(CNC1=NC=C(C(=N1)CC2CC2)C3=NC(=NC=C3)NC4=CC(=NC=C4)Cl)O

Solubility

In vitro
Batch:

DMSO : 85 mg/mL ( (199.57 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 85 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.250mg/ml (9.98mM)	Taking the 1 mL working solution as an example, add 50 μL of 85 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.708mg/ml (1.66mM)	Taking the 1 mL working solution as an example, add 50 μL of 14.16 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	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. This compound has no inhibition to the SGK2 isoform that does not possess a PtdIns(3)P-binding PX domain^[1].
References	https://pubmed.ncbi.nlm.nih.gov/25177796/

Applications

Methods	Biomarkers	Images	PMID
Western blot	p-SGK3 / SGK3 Nanog / CD133		25177796
Growth inhibition assay	Cell viability		31515514

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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