PIK-75 hydrochloride

SKU: orb1305791

Description

PIK-75 hydrochloride is a potent and selective inhibitor of the p110α isoform of PI3K (IC50 = 5.8 nM) and DNA-PK (IC50 = 2 nM). This small molecule is a valuable research tool for studying PI3K signaling in cancer biology and DNA damage response pathways in both cellular and biochemical assays.

Research Area

Cell Biology, Molecular Biology, Signal Transduction

Key Properties

• CAS Number: 372196-77-5
• MW: 488.74
• Purity: 98.00%
• Formula: C₁₆H₁₄BrN₅O₄S·HCl
• SMILES: Cl.CN(N=Cc1cnc2ccc(Br)cn12)S(=O)(=O)c1cc(ccc1C)[N+]([O-])=O
• Target: Apoptosis,PI3K,DNA-PK
• Solubility: DMSO:Slightly soluble

Bioactivity

• Target IC50:
  PI3KC2β:1 μM|p110β:1.3 μM|mTORC1:1 μM|mTORC2:10 μM|PI3KC2α:10 μM|hsVPS34:2.6 μM|ATM:2.3 μM|p110δ:510 nM|DNA-PK:2 nM|p110α:5.8 nM|PI4KIIIβ:50 μM|ATR:21 μM|p110γ:76 nM
• In Vivo:
  In non-asthmatic airway smooth muscle cells, asthmatic ASM cells and lung fibroblasts, PIK-75 (1 μM) inhibited mitochondrial activity and induced cell death. In airway smooth muscle cells, PIK-75 (10 nM) inhibited TNF-α-induced CD38 mRNA expression and significantly reduced TNF-α-induced ADP-ribose cyclase activity. In TGFβ-stimulated ASM cells, PIK75 inhibited only asthmatic cells by decreasing mitochondrial activity.
• In Vitro:
  In non-asthmatic airway smooth muscle cells, asthmatic ASM cells and lung fibroblasts, PIK-75 (1 μM) inhibited mitochondrial activity and induced cell death. In airway smooth muscle cells, PIK-75 (10 nM) inhibited TNF-α-induced CD38 mRNA expression and significantly reduced TNF-α-induced ADP-ribose cyclase activity. In TGFβ-stimulated ASM cells, PIK75 inhibited only asthmatic cells by decreasing mitochondrial activity.
• Cell Research:
  Mitochondrial activity is assessed after stimulation with TGFβ with or without inhibitors for 48 hours using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium (MTT) assay. Harvested washed cells are resuspended in DMEM-lO% FCS and aliquoted (500 μL) into 24-well cluster plates prior to serial dilution (1:2) in duplicates. To each well, 100 μL of an appropriate MTT concentration (dissolved in PBS and filtered through a 0.2 μm filter before use to remove any blue formazan product) is added immediately after diluting the cells, which are then incubated for 3.5 hours at 37 °C. The resulting blue formazan product is solubilized overnight (16 hours) at 37 °C by the addition of 500 μL of 10% sodium dodecyl sulfate (SDS) in 0.01 M HCl to each well. A sample (150 μL) from each duplicate well is transferred to a 96-well microplate, and the optical density determinedby automated spectrophotometry against a reagent blank (no cells). Absorbance is measured at a test wavelength of 570 nm and a reference wavelength of 690 nm. For each primary cell culture, results from three to six wells from each treatment are averaged, and data are expressed as absorbance 570 to 690 nm.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PI3K, PIK 75 Hydrochloride, PIK 75 hydrochloride, PIK 75, PIK75, PIK-75 HCl, PIK75 hydrochloride, PIK75 Hydrochloride, PIK-75 Hydrochloride, p110δ, p110γ, p110β, p110α, pancreatic, CHO-IR, DNAPK, DNA-PK, Apoptosis, apoptotic

Compound Identifiers

PubChem CID

75106606