PIK-90

Catalog No.S1187

PIK-90 Chemical Structure

Molecular Weight(MW): 351.36

PIK-90 is a PI3Kα/γ/δ inhibitor with IC50 of 11 nM/18 nM/58 nM, respectively, less potent to PI3Kβ.

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5 Customer Reviews

  • 3D cultures expressing control (pQCXIP GFP) or K-Ras V12 (pQCXIP GFP K-Ras V12) were continuously treated with 5, 10, or 20 uM of the MEK inhibitor U0126 or 2.0 uM of the PI3K inhibitor PIK-90. At day 10, these structures were fixed and stained for aPKC and DNA. Representative images are shown. Bar, 50 um.

    J Cell Biol 2012 198(2), 185-94. PIK-90 purchased from Selleck.

    Tyr(P)Irs1 determined in CHOIR/Irs1 cells treated with kinase inhibitors. Cells were treated for 30 min without or with PIK-90 at concentrations increasing sequentially 2-fold between the boundaries shown in Fig. 4 before incubation with insulin (30 nM, 30 min). Cleared lysates were subject to immunoblotting with antibodies against Irs1 or Tyr(P). The bands were quantified on a Kodak Image Station 4000MM Pro, and the data were analyzed using Carestream Molecular Imaging software version 5.0.

    J Biol Chem 2014 289(18), 12467-84. PIK-90 purchased from Selleck.

  • For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of PIK-90 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 μM HCl and 0.1% Nonidet-40) was added to dissolve the formazan. The absorbance of each well was measured by ELx808 (BioTek, Winooski, VT) or Wallac Victor2 (Perkin-Elmer Life Sciences, Boston, MA) Microplate Reader. Viable cells are presented as percent of control, vehicle-treated cells.

     

     

    Dr. Yong-Weon Yi from Georgetown University Medical Center. PIK-90 purchased from Selleck.

    We treated all of drugs in T47D which has a PI3KCA H1044R mutation with the concentration shown below for 1 hour and performed western blot analysis using antibodies to phospho-AKT(SERINE 472), and total AKT.

     

     

    Saraswati Sukumar of Johns Hopkins University School of Medicine. PIK-90 purchased from Selleck.

  • Biochim Biophys Acta, 2015, 1853(10 Pt A):2570-9.. PIK-90 purchased from Selleck.

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Biological Activity

Description PIK-90 is a PI3Kα/γ/δ inhibitor with IC50 of 11 nM/18 nM/58 nM, respectively, less potent to PI3Kβ.
Targets
PI3Kα [1] PI3Kγ [1] PI3Kδ [1] PI3Kβ [1]
11 nM 18 nM 58 nM 350 nM
In vitro

PIK-90 shows distinct patterns of isoform selectivity to inhibit different subsets of four class I PI3K isoforms. In addition, PIK-90 completely inhibits the fMLP-stimulated phosphorylation of Akt and impairs polarity and chemotaxis in dHL60 cells. [1] PIK-90 exhibits significantly antiproliferative activity by effectively blocking phosphorylation of Akt in six glioma cell lines varying in mutational status at PTEN or p53, including U87 MG, SF188, SF763, LN229, A1207 and LN-Z30 cells. Moreover, PIK-90 induces a modest G0G1 arrest at a concentration (0.5 μM) sufficient to inhibit phosphorylation of Akt substantially. [2] In chronic lymphocytic leukemia (CLL) cells, PIK-90 inhibits chemotaxis to levels that are 57.8% of controls at 1 μM and 56.8% of controls at 10 μM. Consistently, PIK-90 inhibits pseudoemperipolesis to levels that are 74.2% PIK-90 of controls at 1 μM and 57.9% of controls at 10 μM. In addition, PIK-90 also leads to a significant reduction of CLL cell migration into the stromal cell layer and decreases CXCL12-induced actin polymerization. [3]

In vivo Immediately following insulin treatment, PIK-90 (10 mg/kg) completely protects animals from this insulin-stimulated decline in blood glucose. [4]

Protocol

Kinase Assay:[1]
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Expression and Assay of p110α/p85α, p110β/p85α, p110δ/p85α, and p110γ :

IC50 values are measured using either a standard TLC assay for lipid kinase activity or a high-throughput membrane capture assay. Kinase reactions are performed by preparing a reaction mixture containing kinase, inhibitor (2% DMSO final concentration), buffer (25 mM HEPES, pH 7.4, 10 mM MgCl2), and freshly sonicated phosphatidylinositol (100 μg/mL). Reactions are initiated by the addition of ATP containing 10 μCi of γ-32P-ATP to a final concentration 10 μM or 100 μM, and allowed to proceed for 20 minutes at room temperature. For TLC analysis, reactions are then terminated by the addition of 105 μL 1N HCl followed by 160 μL CHCl3:MeOH (1:1). The biphasic mixture is vortexed, briefly centrifuged, and the organic phase transferred to a new tube using a gel loading pipette tip precoated with CHCl3. This extract is spotted on TLC plates and developed for 3-4 hours in a 65:35 solution of n-propanol:1M acetic acid. The TLC plates are then dried, exposed to a phosphorimager screen, and quantitated. For each compound, kinase activity is typically measured at 10-12 inhibitor concentrations representing two-fold dilutions from the highest concentration tested (100 μM). For compounds showing significant activity, IC50 determinations are repeated two to four times, and the reported value is the average of these independent measurements.
Cell Research:[2]
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  • Cell lines: U87 MG, SF188, SF763, LN229, A1207 and LN-Z3 cells
  • Concentrations: 0 to 1 μM
  • Incubation Time: 72 hours
  • Method: For viabilty, cells are seeded in 12-well plates in the presence of PIK-90 for 3 days. Cell viability is determined using a WST-1 assay.
    (Only for Reference)
Animal Research:[4]
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  • Animal Models: FVB/N female mice are fasted at 9:00 a.m. and then given human insulin or vehicle (PBS) intravenously at 12:00 p.m.
  • Formulation: PIK-90 is dissolved in DMSO and then diluted in water.
  • Dosages: ≤10 mg/kg
  • Administration: Administered via i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 0.28 mg/mL (0.79 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
1% DMSO+30% polyethylene glycol+1% Tween 80, pH 4
15 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 351.36
Formula

C18H17N5O3

CAS No. 677338-12-4
Storage powder
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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PI3K Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID