IC-87114

SKU: orb1305207

Description

IC-87114 is a potent and selective inhibitor of the PI3Kδ isoform, exhibiting an IC50 of 0.5 μM. This small molecule is a valuable research tool for studying B-cell and immune cell signaling in both cellular assays and animal models of inflammation and autoimmune diseases.

Research Area

Signal Transduction

Key Properties

• CAS Number: 371242-69-2
• MW: 397.43
• Purity: >99.99% (May vary between batches)
• Formula: C₂₂H₁₉N₇O
• SMILES: Cc1ccccc1-n1c(Cn2cnc3c(N)ncnc23)nc2cccc(C)c2c1=O
• Target: PI3K
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.52 mM);DMSO:8 mg/mL (20.13 mM)

Bioactivity

• Target IC50:
  PI3Kγ:29 μM|PI3Kβ:75 μM|PI3Kδ:0.5 μM
• In Vivo:
  In human neutrophils, IC87114 at a concentration of 5 μM effectively inhibits the biosynthesis of phosphatidylinositol 3-phosphate (PIP3) and chemotaxis stimulated by N-formylmethionyl-leucyl-phenylalanine (fMLP). Furthermore, in primary cells from acute myeloid leukemia (AML) patients, such as bone marrow mononuclear cells (BMMCs), IC87114 at 10 μM concentration suppresses constitutive and Flt-3-induced Akt phosphorylation as well as cell proliferation. In addition, IC87114 inhibits proliferation and interferon-gamma (IFN-γ) production in mouse CD62L positive (naive) and CD62L negative (effector/memory) CD4+ T cells stimulated by anti-CD3.
• In Vitro:
  In a mouse model of inflammation, IC87114 inhibits the extracellular secretion of proteases prompted by TNF1α stimulation.
• Cell Research:
  For AML cell proliferation assay, BMMCs are isolated and cultured in α-medium with 5% fetal calf serum (FCS) with or without FLT-3 ligand (10 ng/mL) for 48 hours and with or without IC87114. [3H]-thymidine (1 μCi [37 kBq]) is added for a final 6 hours and the amount of radioactivity incorporated is determined by trichloracetic acid precipitation. CD34+ cells from cord blood are cultured in stem cell factor (SCF; 20 ng/mL), FLT-3 ligand (10 ng/mL), and Tpo (20 nM) for 48 hours with or without 10 μM IC87114 and pulsed for 12 hours with [3H]-thymidine. (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

PI3Kγ, PI3Kδ, PI3K, PI3Kβ, Phosphoinositide 3-kinase, inhibit, Inhibitor, IC 87114, IC87114, IC-87114

Compound Identifiers

PubChem CID

9908783