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 | |
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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 | |
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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 |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Wendy Zhang, et al. Mitigating Motor Neuronal Loss in C. elegans Model of ALS8
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