IC-87114 free base · Synonyms: IC 87114 · IC87114

IC-87114 is a potent and selective PI3Kδ inhibitor.

For research use only. Not for human or veterinary use.

Target PI3K

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

IC-87114 structure

CAS No.: 371242-69-2

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 465.00	BP-02470-250mg	In stock	Get quote
500 mg	USD 740.00	BP-02470-500mg	In stock	Get quote
1 g	USD 1,180.00	BP-02470-1g	In stock	Get quote
2 g	USD 1,890.00	BP-02470-2g	In stock	Get quote
3 g	USD 2,270.00	BP-02470-3g	In stock	Get quote
5 g	USD 3,020.00	BP-02470-5g	In stock	Get quote
10 g	Inquire	BP-02470-10g	In stock	Inquire

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Description

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

Biological activity

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). 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.

Identifiers

SMILES: CC1=CC=CC=C1N1C(=O)C2=C(C=CC=C2C)N=C1CN1C=NC2=C(N)N=CN=C12
InChIKey: GNWHRHGTIBRNSM-UHFFFAOYSA-N

Specifications

MW (average): 397.4326
Formula: C₂₂H₁₉N₇O
CAS No.: 371242-69-2
Physical state: Solid
Color: White to gray
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 year;

Solubility

Soluble in DMSO

Documents

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.

[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.

[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.

Same target

Search PI3K

Same research area

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