PI4KIIIbeta-IN-10

Name: PI4KIIIbeta-IN-10
Brand: MedChemExpress
SKU: HY-100198
Rating: 5.0 (16 reviews)

Cat. No.: HY-100198 Purity: 99.84%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

PI4KIIIbeta-IN-10 is a potent PI4KIIIβ inhibitor with an IC₅₀ of 3.6 nM.

For research use only. We do not sell to patients.

PI4KIIIbeta-IN-10 Chemical Structure

CAS No. : 1881233-39-1

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 356	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 356	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 340	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 540	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 900	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1260	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Customer Review

Based on 16 publication(s) in Google Scholar

13 Publications Citing Use of MCE PI4KIIIbeta-IN-10

Proliferation Assay

: PI4KIIIbeta-IN-10 purchased from MedChemExpress. Usage Cited in: Autophagy. 2019 Jul;15(7):1214-1233. [Abstract]; Control or VAPA/B siRNA-transfected HEK293T cells are treated with DMSO or PI4KIIIbeta-IN-10 for 18 h and treated with bafilomycin A1 for 4 h. WBs probed with LC3.

: PI4KIIIbeta-IN-10 purchased from MedChemExpress. Usage Cited in: Autophagy. 2019 Jul;15(7):1214-1233. [Abstract]; Control or VAPA/B siRNA-transfected HEK293T cells are treated with DMSO or PI4KIIIbeta-IN-10 for 4 h. WB probed for TFEB and CTSB.

: PI4KIIIbeta-IN-10 purchased from MedChemExpress. Usage Cited in: Elife. 2017 Nov 1;6:e29388. [Abstract]; Inhibition of PI4KIIIβ by its specific inhibitor IN-10 for 20 min undocks EGFP-CHIP-K30A, but not farnesylated EGFP (EGFP-F) from cellular membranes.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

PI4KIIIbeta-IN-10 is a potent PI4KIIIβ inhibitor with an IC₅₀ of 3.6 nM.

IC₅₀ & Target^[1]

PI4KIIIβ

3.6 nM (IC₅₀)

PI4KIIIα

3 μM (IC₅₀)

PI3Kδ

720 nM (IC₅₀)

PI3KC2γ

1 μM (IC₅₀)

PI3Kα

10 μM (IC₅₀)

PI3Kγ

20 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
Huh-7	IC₅₀	1300 nM Compound: 10	Antiviral activity against HCV genotype 2a J6/JFH1 infected in human Huh7.5 cells after 3 days by gaussia luciferase assay Antiviral activity against HCV genotype 2a J6/JFH1 infected in human Huh7.5 cells after 3 days by gaussia luciferase assay	[PMID: 26885694]
Huh-7	CC₅₀	32000 nM Compound: 10	Cytotoxicity against human Huh7.5 cells after 3 days by presto blue assay Cytotoxicity against human Huh7.5 cells after 3 days by presto blue assay	[PMID: 26885694]

In Vitro

PI4KIIIbeta-IN-10 (Compound 10) is a potent PI4KIIIβ inhibitor with very minor off-target inhibition of PI4KIIIβ related lipid kinases. PI4KIIIbeta-IN-10 shows weak inhibition of PI3KC2γ (IC₅₀ ~1 μM), PI3Kα (~10 μM), and PI4KIIIα (~3 μM), and <20% inhibition at concentrations up to 20 μM for PI4K2α, PI4K2β, and PI3Kβ^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

475.58

Formula

C₂₂H₂₅N₃O₅S₂

CAS No.

1881233-39-1

Appearance

Solid

Color

White to off-white

SMILES

COC1=CC=C(C2=C(C)N=C(NC(C(C)(C)C)=O)S2)C=C1S(NC3=CC=C(O)C=C3)(=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (262.84 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1027 mL	10.5135 mL	21.0270 mL
5 mM	0.4205 mL	2.1027 mL	4.2054 mL
10 mM	0.2103 mL	1.0513 mL	2.1027 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.26 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.26 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.26 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.84%

Select Batch:

Data Sheet (278 KB) SDS (393 KB)

COA (252 KB) HNMR (293 KB) LCMS (131 KB)

Handling Instructions (2659 KB)

References

[1]. Rutaganira FU, et al. Design and Structural Characterization of Potent and Selective Inhibitors of Phosphatidylinositol 4 Kinase IIIβ. J Med Chem. 2016 Mar 10;59(5):1830-9. [Content Brief]

Kinase Assay
^[1]

Lipid kinase assays are preformed using recombinant enzyme, phosphoinositides and γ³²P-ATP in a membrane capture assay. Each inhibitor (e.g., PI4KIIIbeta-IN-10) is diluted into 10% DMSO and kinase assay buffer. Upon completion of the reaction, 4 µL is spotted onto 0.2 µm nitrocellulose. The membrane is dried for 5 minutes under a heat lamp followed by 1×30 second wash and 6×5 min washes in 1M NaCl /1% Phosphoric Acid. The membrane is dried for 20 minutes under a heat lamp followed by overnight exposure to a phosphor screen and phosphorimaging followed on a Typhoon 9500. Intensities are quantified using SPOT. Specifications for each enzyme follow. L-α-Phosphatidylinositol and DOPS:DOPC lipids are sonicated in water to generate 1mg/mL PI:DOPS:DOPC. Reaction is set-up as follows 1) kinase assay buffer, PI:DOPS:DOPC, BSA and PI4KIIIβ, are combined in a total volume of 10 µL (2.5x solution); 2) 5 µL of inhibitor solution is added (5x solution) and incubated with enzyme mixture for 15 minutes; 3) 10 µL cold ATP and γ³²P-ATP are added (2.5x solution) to initiate the reaction which ran for 30 minutes. Final conditions are as follows: 20 mM Bis-Tris Propane pH 7.5, 10 mM MgCl₂, 0.075 mM Triton X-100, 0.5 mM EGTA, 1 mM DTT, 100 µM PI, 500 ng/µL BSA, 2.5 nM PI4KIIIβ, 2% DMSO, 10 µM ATP and 1 uCi γ³²P-ATP^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

[1]. Rutaganira FU, et al. Design and Structural Characterization of Potent and Selective Inhibitors of Phosphatidylinositol 4 Kinase IIIβ. J Med Chem. 2016 Mar 10;59(5):1830-9. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1027 mL	10.5135 mL	21.0270 mL	52.5674 mL
	5 mM	0.4205 mL	2.1027 mL	4.2054 mL	10.5135 mL
	10 mM	0.2103 mL	1.0513 mL	2.1027 mL	5.2567 mL
	15 mM	0.1402 mL	0.7009 mL	1.4018 mL	3.5045 mL
	20 mM	0.1051 mL	0.5257 mL	1.0513 mL	2.6284 mL
	25 mM	0.0841 mL	0.4205 mL	0.8411 mL	2.1027 mL
	30 mM	0.0701 mL	0.3504 mL	0.7009 mL	1.7522 mL
	40 mM	0.0526 mL	0.2628 mL	0.5257 mL	1.3142 mL
	50 mM	0.0421 mL	0.2103 mL	0.4205 mL	1.0513 mL
	60 mM	0.0350 mL	0.1752 mL	0.3504 mL	0.8761 mL
	80 mM	0.0263 mL	0.1314 mL	0.2628 mL	0.6571 mL
	100 mM	0.0210 mL	0.1051 mL	0.2103 mL	0.5257 mL