1. PI3K/Akt/mTOR
  2. PI3K
  3. IC-87114

IC-87114 

Cat. No.: HY-10110 Purity: 98.66%
Handling Instructions

IC-87114 is a potent and selective PI3Kδ inhibitor with IC50 of 0.5 μM.

For research use only. We do not sell to patients.

IC-87114 Chemical Structure

IC-87114 Chemical Structure

CAS No. : 371242-69-2

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10 mM * 1 mL in DMSO USD 73 In-stock
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100 mg USD 480 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

IC-87114 is a potent and selective PI3Kδ inhibitor with IC50 of 0.5 μM.

IC50 & Target[1]

PI3Kδ

0.5 μM (IC50)

PI3Kγ

29 μM (IC50)

PI3Kβ

75 μM (IC50)

In Vitro

IC-87114 (IC87114), an analog of the original inhibitor, is synthesized and tested for PI3Kδ selectivity relative to the other class I PI3Ks. The IC50 of IC87114 for PI3Kδ inhibition is 0.5 μM whereas the IC50 values for PI3Kα, PI3Kβ, and PI3Kγ are >100, 75, and 29 μM, respectively. Thus IC87114 is 58-fold more selective for PI3Kδ relative to PI3Kγ, and over 100-fold selective relative to PI3Kα and PI3Kβ. IC87114 selectively antagonizes PI3Kδ over at least a concentration range of 0.3-10 μM[1]. IC-87114 (10 μM) is also used to selectively inhibit PI3Kδ catalytic activity to address this question. IC87114 (10 μM) effectively inactivates Akt in macrophages after treatment for 1 hour (n=6; P<0.001 versus control). The effect of IC-87114 (IC87114) is next detected ton AP-1 DNA-binding activity. The electrophoretic mobility shift assay assay demonstrates that DNA-binding activity of AP-1 is significantly increased after the treatment with TNF-α (10 ng/mL; P<0.001) and TNF-α (20 ng/mL; P<0.001). IC87114 alone induces AP-1 DNA-binding activity after treatment for 1 hour. Furthermore, there is stronger AP-1 DNA-binding activity after costimulation of IC87114 (10 μM) and TNF-α (0-20 ng/mL) than only treatment with TNF-α (0-20 ng/mL; n=5; P<0.01). IC87114 (10 μM) also effectively inhibits p110δ catalytic activities (Akt phosphorylation) in macrophages with or without TNF-α treatment for 24 hours (n=6; P<0.001)[2].

In Vivo

Treatment with PD 89059 (10 mg/kg), IC-87114 (0.3 mg/kg) and BAY 11-7085 (10 mg/kg), significantly (P<0.05) reduces the OVA- induced inflammatory cell influx into the airways and the histopathological airway remodeling. However, these treatments does not significantly improve OVA induced-AHR (P>0.05). Of note, the observed reduction in the histopathological airway remodeling induced by PD 89059, IC-87114 and BAY 11-7085 are less effective as compared to the reduction seen with AG 1478 and SU6656[3].

Molecular Weight

397.43

Formula

C₂₂H₁₉N₇O

CAS No.

371242-69-2

SMILES

O=C1N(C(CN2C3=C(C(N)=NC=N3)N=C2)=NC4=CC=CC(C)=C14)C5=C(C)C=CC=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 10 mg/mL (25.16 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5162 mL 12.5808 mL 25.1617 mL
5 mM 0.5032 mL 2.5162 mL 5.0323 mL
10 mM 0.2516 mL 1.2581 mL 2.5162 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1 mg/mL (2.52 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1 mg/mL (2.52 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1 mg/mL (2.52 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[2]

The murine macrophage cell line RAW264.7 and peritoneal macrophages from both types of mice are maintained in Dulbecco's modified Eagle's medium (DMEM) with 10% fetal calf serum (FCS). Cultures are maintained at 37°C in a humidified incubator in a 95% O2 plus 5% CO2 atmosphere. Cells are treated with varied concentrations of TNF-α and used IC-87114 (IC87114) to inhibit PtdIns(3,4,5)P3-dependent phosphorylation of Akt before TNF-α stimulation at early time points (30 min)[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

Mice[3]
BALB/c mice are immunized once by i.p. injection of 10 µg ovalbumin (OVA) in 0.2 ml of alu-Gel-S on day 0. Ten days later, mice are intranasally (i.n.) challenged with OVA (30 µg in 50 µL PBS) or PBS, once daily, over four consecutive days. To investigate if ERK1/2, PI3Kδ and NF-κB are signaling effectors downstream of EGFR transactivation, six treatment groups (A-F, 10-30 animals per group) are established. Mice in groups A and B are pretreated intranasally with 0.2 mL of the vehicle for the drugs. Groups C, D and E are pretreated with the same volume of three different drugs (PD 98059, IC-87114 and BAY 11-7085, respectively) at 10 mg/kg, 10 mg/kg and 0.3 mg/kg respectively, and group F with Dexamethasone (1 mg/kg), 1 h before each i.n. challenge with OVA. These doses are chosen from previous studies where they are shown to be effective.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

IC-87114IC87114IC 87114PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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IC-87114
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