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IC-87114

Catalog No. T2660 CAS 371242-69-2

Synonyms: IC 87114

IC-87114 is a specific PI3Kδ inhibitor(IC50=0.5 μM).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

IC-87114, CAS 371242-69-2

Pack Size	Availability	Price/USD
2 mg	In stock	$ 33.00
5 mg	In stock	$ 52.00
10 mg	In stock	$ 83.00
25 mg	In stock	$ 148.00
50 mg	In stock	$ 252.00
100 mg	In stock	$ 397.00
200 mg	In stock	$ 582.00
1 mL * 10 mM (in DMSO)	In stock	$ 58.00

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Purity: 100%

Purity: 95.58%

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Description	IC-87114 is a specific PI3Kδ inhibitor(IC50=0.5 μM).
Targets&IC50	PI3Kδ:0.5 μM, PI3Kγ:29 μM
In vitro	In a mouse model of inflammation, IC87114 inhibits the extracellular secretion of proteases prompted by TNF1α stimulation.
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.
Kinase Assay	PI3K kinase assay: Phosphatidylinositol-(4,5)-bisphosphate (PIP2) containing phospholipid liposomes are prepared. Briefly, bovine PIP2 and phosphatidylserine (1:2 molar ratio) are vacuum-dried and resuspended at 1 mM PIP2 in 20 mM HEPES-KOH, pH 7.4, 50 mM NaCl, and 5 mM EDTA. The lipid suspension is subjected to a brief sonication, followed by 5 freeze-thaw cycles and then 20 extrusion cycles to produce the liposomes. The assay is conducted in 60 μL reaction volumes in 20 mM HEPES, pH 7.4, buffer containing 1 nM PI3K, 1 μM PIP2, 200 μM ATP, 1 μCi [γ-32P]ATP, 5 mM MgCl2, plus 50 μg/mL horse IgG as carrier protein. The reaction is incubated for 10 min at room temperature, quenched in 140 of 1 M K2PO4, 30 mM EDTA, pH 8.0, captured onto a 96-well polyvinylidene difluoride filter plate, and washed five times with 1 M K2PO4. The filter is allowed to dry completely, and the bound radioactivity is quantitated. IC87114 dilutions are assayed in a final concentration of 1% (w/w) DMSO.
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)

Synonyms	IC 87114
Molecular Weight	397.43
Formula	C22H19N7O
CAS No.	371242-69-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 10 mg/mL (25.16 mM), Sonification is recommended.

References and Literature

1. Sadhu C, et al. J Immunol, 2003, 170(5), 2647-2654. 2. Sujobert P, et al. Blood, 2005, 106(3), 1063-1066. 3. Ali K, et al. Nature, 2004, 431(7011), 1007-1011. 4. Soond DR, et al. Blood, 2010, 115(11), 2203-2213. 5. Wen PJ, et al. Nat Commun, 2011, doi:10.1038/ncomms1500. 6. 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. 7. 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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Aging Compound Library Anti-Ovarian Cancer Compound Library Anti-Obesity Compound Library NO PAINS Compound Library Reprogramming Compound Library Kinase Inhibitor Library Anti-Lung Cancer Compound Library Oxidation-Reduction Compound Library Glycometabolism Compound Library

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Keywords

IC-87114 371242-69-2 PI3K/Akt/mTOR signaling PI3K IC 87114 Inhibitor inhibit IC87114 Phosphoinositide 3-kinase inhibitor

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