1. PI3K/Akt/mTOR
  2. PI4K

PI4KIIIbeta-IN-10 

Cat. No.: HY-100198 Purity: 98.21%
Data Sheet SDS Handling Instructions

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

PI4KIIIbeta-IN-10 Chemical Structure

CAS No. : 1881233-39-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 439 In-stock
1 mg USD 180 In-stock
5 mg USD 420 In-stock
10 mg USD 660 In-stock
25 mg USD 1320 In-stock
50 mg USD 2040 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

    PI4KIIIbeta-IN-10 purchased from MCE. Usage Cited in: Elife. 2017 Nov 1;6. pii: e29388.

    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

    • Technical Information

    • Purity & Documentation

    • References

    Description

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

    IC50 & Target

    IC50: 3.6 nM (ΡΙ4ΚΙΙΙβ), 720 nM (PI3Kδ), ~1 µM (PI3KC2γ), ~10 µM (PI3Kα), ~3 µM (PI4KIIIα)[1]

    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].

    References
    Preparing Stock Solutions
    Concentration Volume 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
    Please refer to the solubility information to select the appropriate solvent.
    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
    Molecular Weight

    475.58

    Formula

    C₂₂H₂₅N₃O₅S₂

    CAS No.

    1881233-39-1

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 30 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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    Product Name:
    PI4KIIIbeta-IN-10
    Cat. No.:
    HY-100198
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