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PIK-90

Catalog No. T2461 CAS 677338-12-4

PIK-90, a DNA-PK and PI3K inhibitor, suppresses p110α( IC50=11 nM), p110γ(IC50=18 nM) and DNA-PK(IC50=13 nM) .

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PIK-90, CAS 677338-12-4

Pack Size	Availability	Price/USD
5 mg	In stock	$ 39.00
10 mg	In stock	$ 47.00
25 mg	In stock	$ 85.00
50 mg	In stock	$ 147.00

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Purity: 99.62%

Purity: 98.25%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	PIK-90, a DNA-PK and PI3K inhibitor, suppresses p110α( IC50=11 nM), p110γ(IC50=18 nM) and DNA-PK(IC50=13 nM) .
Targets&IC50	PI3Kγ:18 nM, PI3Kα:11 nM, DNA-PK:13 nM
In vitro	In insulin-stimulated animals, treatment with PIK-90 (10 mg/kg) is capable of inhibiting the reduction of blood glucose levels induced by insulin stimulation.
In vivo	In chronic lymphocytic leukemia cells, treatment with PIK-90 (1-10 μM) suppresses chemotaxis, significantly inhibiting cell migration into the stromal cell layer and reducing CXCL12-induced actin polymerization. In dHL60 cells, PIK-90 inhibits Akt phosphorylation stimulated by fMLP, impairing cell polarity and chemotaxis. Moreover, in glioma cell lines (U87 MG, SF188, SF763, LN229, A1207, and LN-Z30 cells), PIK-90 blocks Akt phosphorylation, inhibiting cell proliferation.
Kinase Assay	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	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)

Molecular Weight	351.36
Formula	C18H17N5O3
CAS No.	677338-12-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 0.2 mg/mL (insoluble or slightly soluble)

DMSO: 3.51 mg/ml (10 mM), Sonication is recommended.

H2O: < 0.2 mg/mL (insoluble or slightly soluble)

References and Literature

1. Van Keymeulen A, et al. J Cell Biol. 2006, 174(3), 437-445. 2. Fan QW, et al. Cancer Res. 2007, 67(17), 7960-7965. 3. Niedermeier M, et al. Blood. 2009, 113(22), 5549-5557. 4. Knight ZA, et al. Cell. 2006, 125(4), 733-747.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Kinase Inhibitor Library Bioactive Compound Library DNA Damage & Repair Compound Library Bioactive Compounds Library Max Anti-Prostate Cancer Compound Library Metabolism Compound Library Glycolysis Compound Library Anti-Ovarian Cancer Compound Library Anti-Colorectal Cancer Compound Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

PIK-90 677338-12-4 DNA Damage/DNA Repair PI3K/Akt/mTOR signaling DNA-PK PI3K Inhibitor PIK90 Phosphoinositide 3-kinase DNA-dependent protein kinase PIK 90 inhibit inhibitor

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