IPI-3063

SKU: orb1308187

Description

IPI-3063 is a potent and selective small molecule inhibitor of the PI3K p110δ isoform, demonstrating an IC50 of 2.5 ± 1.2 nM. It is a valuable research tool for studying B-cell malignancies and immune disorders in both in vitro and in vivo experimental models.

Research Area

Signal Transduction

Key Properties

• CAS Number: 1425043-73-7
• MW: 455.51
• Purity: 99.77% (May vary between batches)
• Formula: C₂₅H₂₅N₇O₂
• SMILES: CC(C)n1c(cc2cccc(-c3ccc(=O)n(C)c3)c2c1=O)[C@H](C)Nc1ncnc(N)c1C#N
• Target: PI3K
• Solubility: DMSO:83.33 mg/mL (182.94 mM)

Bioactivity

• Target IC50:
  p110β:1508 nM|p110δ:2.5 nM|p110α:1170 nM|p110γ:2187 nM
• In Vitro:
  IPI-3063 is a p110δ selective compound with an IC50=0.1 nM in p110δ-specific cell-based assays and cellular IC50 values for the other class I PI3K isoforms are at least 1,000-fold higher (IC50=1901±1318 nM for p110α, IC50=102.8±35.7 nM for p110β, IC50=418.8±117.2 nM for p110γ). IPI-3063 is very effective in reducing p-AKT (significant effect at 1 nM) and it also decreases p-ERK1/2 with a significant effect at 10 nM. IPI-3063 is very effective, achieving a significant decrease in B cell survival when present at 10 nM and it also inhibits p110α, p110β, and p110γ (IC50s: 1171±533 nM, 1508±624 nM, and 2187±1529 nM, respectively). IPI-3063 effectively decreases mouse B cell proliferation, survival, and plasmablast differentiation while increasing antibody class switching to IgG1.
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Storage & Handling

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

Alternative Names

p110β, p110γ, p110α, p110δ, inhibit, IPI 3063, IPI3063, IPI-3063, Inhibitor, Phosphoinositide 3-kinase, PI3K

Compound Identifiers

PubChem CID

71276090