PIK-90

SKU: orb1305454

Description

PIK-90 is a potent dual inhibitor of DNA-PK and PI3K, demonstrating nanomolar IC50 values against p110α (11 nM), p110γ (18 nM), and DNA-PK (13 nM). This small molecule is a valuable research tool for investigating DNA damage response and PI3K signaling pathways in both cellular and biochemical assays.

Research Area

Molecular Biology, Signal Transduction

Key Properties

• CAS Number: 677338-12-4
• MW: 351.36
• Purity: 99.89%
• Formula: C₁₈H₁₇N₅O₃
• SMILES: COc1ccc2C3=NCCN3C(NC(=O)c3cccnc3)=Nc2c1OC
• Target: PI3K,DNA-PK
• Solubility: H2O:< 0.2 mg/mL (insoluble or slightly soluble);Ethanol:< 0.2 mg/mL (insoluble or slightly soluble);DMSO:< 0.2 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  PI3KC2α:47 nM|p110β:350 nM|PI3KC2β:64 nM|mTORC1:1.05 μM|hsVPS34:830 nM|ATM:610 nM|PI3Kγ:18 nM|ATR:15 μM|PI4KIIIα:830 nM|PI4KIIIβ:3.1 μM|PI3Kα:11 nM|DNA-PK:13 nM|p110δ:58 nM
• 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.
• 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.
• 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)

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

inhibit, Inhibitor, DNA-dependent protein kinase, DNA-PK, DNAPK, Phosphoinositide 3-kinase, PI3K, PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, PIK 90, PIK90, PIK-90

Compound Identifiers

PubChem CID

135398491