Cat. No.: HY-10110

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IC-87114

3 Cited Publications

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Based on 3 publication(s) in Google Scholar

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.

Purity: 99.85%
CAS No.: 371242-69-2
Formula: C₂₂H₁₉N₇O
Molecular Weight:397.43

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

IC-87114 Chemical Structure

CAS No.: 371242-69-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

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)

All PI3K Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	>10 μM Compound: IC87114	Antiproliferative activity against human A549 cells after 24 to 48 hrs by MTT assay Antiproliferative activity against human A549 cells after 24 to 48 hrs by MTT assay	[PMID: 29486969]
COLO 205	IC₅₀	>10 μM Compound: IC87114	Antiproliferative activity against human COLO205 cells after 24 to 48 hrs by MTT assay Antiproliferative activity against human COLO205 cells after 24 to 48 hrs by MTT assay	[PMID: 29486969]
HCT-116	IC₅₀	>10 μM Compound: IC87114	Antiproliferative activity against human HCT116 cells after 24 to 48 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 24 to 48 hrs by MTT assay	[PMID: 29486969]
HL-60	IC₅₀	1 μM Compound: IC87114	Antiproliferative activity against human HL60 cells after 24 to 48 hrs by MTT assay Antiproliferative activity against human HL60 cells after 24 to 48 hrs by MTT assay	[PMID: 29486969]
MCF7	IC₅₀	>10 μM Compound: IC87114	Antiproliferative activity against human MCF7 cells after 24 to 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 24 to 48 hrs by MTT assay	[PMID: 29486969]
Sf21	IC₅₀	130 nM Compound: 1; IC87114	Inhibition of full length recombinant human N-terminal His6-tagged PI3K p110delta/human p85alpha expressed in baculovirus infected sf21 cells using PIP2 as substrate preincubated for 30 mins followed by substrate addition by HTRF assay Inhibition of full length recombinant human N-terminal His6-tagged PI3K p110delta/human p85alpha expressed in baculovirus infected sf21 cells using PIP2 as substrate preincubated for 30 mins followed by substrate addition by HTRF assay	[PMID: 28105286]

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].

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

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].

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

Chemical Information

CAS No. 371242-69-2
Appearance Solid
Molecular Weight 397.43
Formula C₂₂H₁₉N₇O
Color White to gray
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	2 years
	-20°C	1 year

Publications (3)

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Sci Signal

Suppression of caspase 8 activity by a coronin 1-PI3Kδ pathway promotes T cell survival independently of TCR and IL-7 signaling. [Abstract]

2021 Dec 21;14(714):eabj0057. PMID: 34932374
Int J Chron Obstruct Pulmon Dis

Cryptotanshinone Reverses Corticosteroid Insensitivity by Inhibition of Phosphoinositide-3-Kinase-δ in Chronic Obstructive Pulmonary Disease. [Abstract]

2023 May 6:18:797-809. PMID: 37180749
University of Cologne

2024.

Solvent & Solubility

In Vitro:

DMSO : 10 mg/mL (25.16 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 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

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

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].

MedChemExpress (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.

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (287 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Sadhu C, et al. Essential role of phosphoinositide 3-kinase delta in neutrophil directional movement. J Immunol. 2003 Mar 1;170(5):2647-54. [Content Brief]

[2]. Zheng L, et al. Inactivation of PI3Kδ induces vascular injury and promotes aneurysm development by upregulating the AP-1/MMP-12 pathway in macrophages. Arterioscler Thromb Vasc Biol. 2015 Feb;35(2):368-77. [Content Brief]

[3]. El-Hashim AZ, et al. Src-dependent EGFR transactivation regulates lung inflammation via downstream signaling involving ERK1/2, PI3Kδ/Akt and NFκB induction in a murine asthma model. Sci Rep. 2017 Aug 30;7(1):9919. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5162 mL	12.5808 mL	25.1617 mL	62.9042 mL
	5 mM	0.5032 mL	2.5162 mL	5.0323 mL	12.5808 mL
	10 mM	0.2516 mL	1.2581 mL	2.5162 mL	6.2904 mL
	15 mM	0.1677 mL	0.8387 mL	1.6774 mL	4.1936 mL
	20 mM	0.1258 mL	0.6290 mL	1.2581 mL	3.1452 mL
	25 mM	0.1006 mL	0.5032 mL	1.0065 mL	2.5162 mL

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IC-87114

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Publications Citing Use of MedChemExpress (MCE) IC-87114

All PI3K Isoforms

Biological Activity

Chemical Information

Publications (3)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

IC-87114 Related Classifications

Cat. No.: HY-10110