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PIK-93 is a PI4KIIIβ inhibitor (IC50 at 19 nM). PIK-93 is the first reported PI4-kinase inhibitor, which is able to inhibit PI4KIIIβ at low-nanomolar range. In addition, this compound also inhibits potently PI3Kγ in vitro (IC50 at 16 nM). This compound inhibits p110α, p110β, p110δwith IC50 of 0.039, 0.59, 0.12 µM. PIK-93 also displays the typical hydrogen bonding to the backbone amide of Val882, and additional ones to the backbone carbonyl of Val882 and between its sulphonamide and Asp964.
| Cell Experiment | |
|---|---|
| Cell lines | Differentiated HL60 (dHL60) cells |
| Preparation method | For actin staining, preincubate dHL60 cells in suspension with PIK-93 or vehicle for 40 min, centrifuge for 5 min at 2000 rpm at room temperature in a J6-B centrifuge, resuspend in mHBSS containing the respective agent at the same concentration, allowed to stick to fibronectin-covered coverslips, and subject to stimulation with a uniform concentration of 100 nM f-Met-Leu-Phe (fMLP) for 3 min. Fixing cellsare in 3.7% PFA and staining with 10 units/mL rhodamine-phalloidin for 15 min |
| Concentrations | 0.5 μM–1 μM |
| Incubation time | 40 min |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 389.88 |
| Formula | C14H16ClN3O4S2 |
| CAS Number | 593960-11-3 |
| Solubility (25°C) | DMSO 70 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Wendy Zhang, et al. Mitigating Motor Neuronal Loss in C. elegans Model of ALS8
| Related PI3K Products |
|---|
| PI3Kγ inhibitor AZ2
PI3Kγ inhibitor AZ2 is a highly selective PI3Kγ inhibitor (The pIC50 value for PI3Kγ is 9.3). |
| NIBR-17
NIBR-17 is a pan-class I PI3K inhibitor with suitable pharmacokinetic properties and inhibits tumor growth. |
| RV-1729
RV-1729 is an inhibitor of the phosphatidylinositol 3-kinase-δ (PI3Kδ). |
| Vulolisib
Vulolisib is a potent and orally active phosphatidylinositol 3-kinase (PI3K) inhibitor, with IC50 values of 0.2 nM, 168 nM, 90 nM and 49 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. |
| Vps34-IN-4
Vps34-IN-4 is a potent, selective, and orally active inhibitor of VPS34. |
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