PIK-294

SKU: orb1223714

Description

A highly potent, selective p110δ inhibitor with IC50 of 10 nM; shows 1000-, 49- and 16-fold less potent to PI3Kα/β/γ.

Key Properties

• CAS Number: 900185-02-6
• MW: 489.5279
• Purity: >98% (HPLC)
• Formula: C₂₈H₂₃N₇O₂
• SMILES: O=C1N(C2=CC=CC=C2C)C(CN3N=C(C4=CC=CC(O)=C4)C5=C(N)N=CN=C53)=NC6=C1C(C)=CC=C6
• Target: PI3K
• Solubility: DMSO: ≥ 40 mg/mL

Bioactivity

• In Vitro:
  Analysis of the specific Class I PI3 Kinase catalytic isoforms p110α (IC50 = 10 μM), p110β (IC50 = 0.49 μM), p110δ (IC50 = 0.01 μM) and p110γ (IC50 = 0.16 μM) using the inhibitor PIK-294 indicates differential roles in CXCL8-induced neutrophil migration. PIK-294 inhibits both chemokinetic and chemotactic CXCL8-induced migration. When cells are pre-treated with the PI3Kδ selective inhibitor PIK-294, CXCL8-induced migration in the non-gradient and the gradient assay is significantly inhibited. PIK-294 is used at two concentrations 1 μM and 10 μM. Pre-treatment with 1 μM inhibits migration to a greater extent in the non-gradient assay than in the gradient assay. Pre-treatment with 10 μM inhibits migration to a significantly greater extent than the lower dose in both assays. Prior to stimulation with CXCL8, pre-treatment of the cells with the PI3K inhibitors, Wortmannin (50 nM), PIK-294 (10 μM) and AS-605240 (10 μM) for 2 minutes, cause a reduction in the phosphorylation of Akt. Pre-treatment of cells prior to stimulation with GM-CSF and the DMSO control with the PI3K inhibitors Wortmannin (50 nM), PIK-294 (10 μM) and AS-605240 (10 μM) for 2 minutes, reduce the phosphorylation of Akt (p<0.05 for inhibition of PI3Kδ).
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PIK294 | PIK 294 | PIK-294

Quick Database Links

Gene Symbol

PI3K