IC-87114 is an ATP-competitive, purine-quinazoline-based inhibitor of PI3Kdelta with an IC50 of 0.5 uM. It is selective over other major isoforms of PI3K (PI3Ka = >100 uM; PI3Kb = 75 uM; PI3Kg = 29 uM) as well as a PIK-related kinases such as DNA-PK and mTOR. [1]
Studies with IC-87114 have assisted in showing that PI3Kdelta is responsible for fMLP-induced PIP3 generation in neutrophils and critical to chemotaxis, but not adhesion. Furthermore, inhibition of PI3Kdelta affects cell polarization and CD18 integrin-dependent chemotactic migration, but is less implicated in random movement. [1]
Technical information:
Chemical Formula: | C22H19N7O | |
CAS #: | 371242-69-2 | |
Molecular Weight: | 397.43 | |
Purity: | > 98% | |
Appearance: | White | |
Chemical Name: | 2-((6-amino-9H-purin-9-yl)methyl)-5-methyl-3-o-tolylquinazolin-4(3H)-one | |
Solubility: | Up to 10 mM in DMSO | |
Synonyms: | IC-87114, IC87114, IC 87114 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
1. | Sadhu et al, Essential role of phosphoinositide 3-kinase delta in neutrophil directional movement. J. Immunol. 2003, 170, 2647-2654. Pubmed ID: 12594293 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.