PIK-90

Catalog No.S1187 Batch:S118701

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Technical Data

Formula

C18H17N5O3
Molecular Weight 351.36 CAS No. 677338-12-4
Solubility (25°C)* In vitro 5%TFA 2.53 mg/mL (7.2 mM)
DMSO 0.28 mg/mL (0.79 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 (from reference)

Kinase Assay:[1]
  • 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 Assay:[2]
  • 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.
Animal Study:[4]
  • 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.

  • Dosages

    ≤10 mg/kg

  • Administration

    Administered via i.p.

Customer Product Validation

Data from [Data independently produced by J Biol Chem, 2014, 289(18), 12467-84]

Data from [Data independently produced by J Cell Biol, 2012, 198(2), 185-94]

, , Dr. Yong-Weon Yi from Georgetown University Medical Center

, , Saraswati Sukumar of Johns Hopkins University School of Medicine

Selleck's PIK-90 has been cited by 28 publications

Efficient generation of human NOTCH ligand-expressing haemogenic endothelial cells as infrastructure for in vitro haematopoiesis and lymphopoiesis [ Nat Commun, 2024, 15(1):7698] PubMed: 39227582
A secreted proteomic footprint for stem cell pluripotency [ PLoS One, 2024, 19(6):e0299365] PubMed: 38875182
Directed differentiation of hPSCs through a simplified lateral plate mesoderm protocol for generation of articular cartilage progenitors [ PLoS One, 2023, 18(1):e0280024] PubMed: 36706111
Lateral plate mesoderm cell-based organoid system for NK cell regeneration from human pluripotent stem cells [ Cell Discov, 2022, 8(1):121] PubMed: 36344493
Plasma membrane-nucleo-cytoplasmic coordination of a receptor-like cytoplasmic kinase promotes EDS1-dependent plant immunity [ Nat Plants, 2022, 8(7):802-816] PubMed: 35851623
CK2-induced cooperation of HHEX with the YAP-TEAD4 complex promotes colorectal tumorigenesis [ Nat Commun, 2022, 13(1):4995] PubMed: 36008411
SARS-CoV-2 ORF10 antagonizes STING-dependent interferon activation and autophagy [ J Med Virol, 2022, 94(11):5174-5188] PubMed: 35765167
TMEM43 promotes pancreatic cancer progression by stabilizing PRPF3 and regulating RAP2B/ERK axis [ Cell Mol Biol Lett, 2022, 27(1):24] PubMed: 35260078
Loss of BTK ameliorates the pathological cardiac fibrosis and dysfunction [ Matrix Biol, 2022, S0945-053X(22)00104-4] PubMed: 36031013
African Swine Fever Virus pI215L Inhibits Type I Interferon Signaling by Targeting Interferon Regulatory Factor 9 for Autophagic Degradation [ J Virol, 2022, 96(17):e0094422] PubMed: 35972295

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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