PIK-294 is a highly selective inihibitor of the phosphoinositide 3-kinase (PI3K) p110δ with an IC50 value of 10 nM compared to IC50 values of 10 μM, 490 nM and 160 nM for PI3Kα/β/γ, respectively. PIK-294 has been used to help distinguish the unique roles of the various PI3-K isoforms. PIK-294 inhibited both chemokinetic and chemotactic CXCL8-induced migration.
Chemical Formula: C28H23N7O2
Exact Mass: 489.19
Molecular Weight: 489.52792
Elemental Analysis: C, 68.70; H, 4.74; N, 20.03; O, 6.54
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: 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 Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
Analysis of the specific Class I PI3 Kinase catalytic isoforms p110α (IC50=10 μM), p110β (IC50=0.49 μM), p110δ (IC50=0.01 μM) and p110γ (IC50=0.16 μM) using the inhibitor PIK-294 indicates differential roles in CXCL8-induced neutrophil migration. PIK-294 inhibits both chemokinetic and chemotactic CXCL8-induced migration. When cells are pre-treated with the PI3Kδ selective inhibitor PIK-294, CXCL8-induced migration in the non-gradient and the gradient assay is significantly inhibited.
PIK-294 is used at two concentrations 1 μM and 10 μM. Pre-treatment with 1 μM inhibits migration to a greater extent in the non-gradient assay than in the gradient assay. Pre-treatment with 10 μM inhibits migration to a significantly greater extent than the lower dose in both assays. Prior to stimulation with CXCL8, pre-treatment of the cells with the PI3K inhibitors, Wortmannin (50 nM), PIK-294 (10 μM) and AS-605240 (10 μM) for 2 minutes, cause a reduction in the phosphorylation of Akt. Pre-treatment of cells prior to stimulation with GM-CSF and the DMSO control with the PI3K inhibitors Wortmannin (50 nM), PIK-294 (10 μM) and AS-605240 (10 μM) for 2 minutes, reduce the phosphorylation of Akt (p<0.05 for inhibition of PI3Kδ).
Inhibitors of the PI3k/Akt/Ikk/NF-kb signalling pathway, pharmaceutically acceptable salts thereof and compositions containing said inhibitors for prophylaxis and treatment of viral diseases. Fedichev, Petr Olegovich; Vinnik, Andrey Alexandrovich. PCT Int. Appl. (2013), WO 2013147649 A2 20131003 .
Methods for predicting cancer treatment responsiveness to phosphatidylinositol 3-kinase (PI3K) inhibitors. Jane, Stephen M.; Darido, Charbel. PCT Int. Appl. (2013), WO 2013029116 A1 20130307.
Methods for treating oncovirus positive cancers. Jimeno, Antonio; Hausman, Diana F.; Peterson, Scott. PCT Int. Appl. (2012), WO 2012118978 A1 20120907.
Use of phosphatidylinositol-3'-kinase (PI3K) p110 delta isoform inhibitors for treating retroviral infection and replication. Katsikis, Peter D.; Boesteanu, Alina C.; Turner, Martin. PCT Int. Appl. (2012), WO 2012009452 A1 20120119.
Methods and compositions for treatment of ophthalmic conditions. Wilson, Troy Edward; Rommel, Christian; Liu, Yi; Ren, Pingda. PCT Int. Appl. (2010), WO 2010059593 A1 20100527.
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