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PIK-93

Cat. No. M3474
PIK-93 Structure
Size Price Availability Quantity
5mg USD 130 In stock
25mg USD 420 In stock
100mg USD 1050 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 389.88
Formula C14H16ClN3O4S2
CAS Number 593960-11-3
Purity >99%
Solubility DMSO 70 mg/mL
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PIK-93 supplier, PI3K, inhibitors

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