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BioChemicals
IC-87114
tcsc0184
IC-87114
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5mg
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100mg
$
147.00
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ORDERING INFORMATION
International
TAICLONE BIOTECH CORP.
order@taiclone.com
+886-2-2735-9682
+886-2-2735-9807
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Product Description
IC-87114 is a potent and selective
PI3Kδ
inhibitor with
IC
50
of 0.5 μM.
IC50 & Target: IC50: 0.5 μM (PI3Kδ)
[1]
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 IC
50
of IC87114 for PI3Kδ inhibition is 0.5 μM whereas the IC
50
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]
.
Information
CAS No
371242-69-2
Formula
C
22
H
19
N
7
O
Clinical Information
clinicalinformation
Pathway
PI3K/Akt/mTOR
Target
PI3K
Specifications
Purity / Grade
>98%
Solubility
DMSO : 10 mg/mL (25.16 mM; Need ultrasonic)
Smiles
smiles
Misc Information
Observed Molecular Weight
397.43
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