PI4KIIIbeta-IN-10
Modify Date: 2024-01-11 12:48:57
PI4KIIIbeta-IN-10 structure
|
Common Name | PI4KIIIbeta-IN-10 | ||
|---|---|---|---|---|
| CAS Number | 1881233-39-1 | Molecular Weight | 475.581 | |
| Density | 1.4±0.1 g/cm3 | Boiling Point | N/A | |
| Molecular Formula | C22H25N3O5S2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of PI4KIIIbeta-IN-10PI4KIIIbeta-IN-10 is a potent PI4KIIIβ inhibitor with an IC50 of 3.6 nM. |
| Name | PI4KIIIbeta-IN-10 |
|---|---|
| Synonym | More Synonyms |
| Description | PI4KIIIbeta-IN-10 is a potent PI4KIIIβ inhibitor with an IC50 of 3.6 nM. |
|---|---|
| Related Catalog | |
| Target |
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) |
| 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]. |
| Kinase Assay | 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]. |
| References |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Molecular Formula | C22H25N3O5S2 |
| Molecular Weight | 475.581 |
| Exact Mass | 475.123566 |
| LogP | 3.64 |
| Index of Refraction | 1.631 |
| Storage condition | 2-8℃ |
| N-(5-{3-[(4-Hydroxyphenyl)sulfamoyl]-4-methoxyphenyl}-4-methyl-1,3-thiazol-2-yl)-2,2-dimethylpropanamide |
| Propanamide, N-[5-[3-[[(4-hydroxyphenyl)amino]sulfonyl]-4-methoxyphenyl]-4-methyl-2-thiazolyl]-2,2-dimethyl- |