Cat. No. Name Size Price Add Cart
KI2166IC-871145 mg$144
IC-8711410 mg$272
IC-8711450 mg$1072

Chemical Characteristic

Product NameIC-87114
CAS No.371242-69-2
Molecular Weight 397.43
FormulaC22H19N7O
Chemical Name2-[(6-Amino-9H-purin-9-yl)methyl]-5-methyl-3-(2-methylphenyl)-4(3H)-quinazolinone
Smilesn1c(n(c(=O)c2c(cccc12)C)c1c(cccc1)C)Cn1cnc2c1ncnc2N
Chemical Structure

Biological activities

IC-87114 is a highly selective antagonist of PI3Kδ. IC-87114 inhibits PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ with IC50s of >100, 75, 29 and 0.5 µM, respectively. IC-87114 blocks N-formyl-methionyl-leucyl-phenylalanine (FMLP)-induced neutrophil chemotaxis on intercellular adhesion molecule-1 (ICAM-1) with an EC50 of 0.375 µM.[1] IC-87114 (40 µM) completely blocks the anaphylaxis reaction in the back dermis. IC-87114 reduces DNA synthesis of wild-type bone marrow??erived mast cells (BMMCs) without significantly affecting p110δD910A/D910A BMMCs.[2] IC-87114 inhibits PI3K-dependent activation of Akt in splenic and peritoneal B cell subsets. IC-87114 inhibits chemoattractant-induced migration of splenic B-2, MZ, and B-1a B cells. IC-87114 inhibits MZ B cell adhesion in vitro and disrupts MZ B cell localization in mice. IC-87114 treatment inhibits T-dependent Ab responses in vivo in a rat model.[3]

Protocols

In vitro, IC-87114 is dissolved in PEG400.[3]

References

[1] Sadhu C, et al. Essential role of phosphoinositide 3-kinase delta in neutrophil directional movement. J Immunol. 2003, 170(5): 2647-2654.
[2] Ali K, et al. Essential role for the p110delta phosphoinositide 3-kinase in the allergic response. Nature. 2004, 431(7011): 1007-1011.
[3] Durand CA, et al. Phosphoinositide 3-kinase p110 delta regulates natural antibody production, marginal zone and B-1 B cell function, and autoantibody responses. J Immunol. 2009, 183(9): 5673-5684.

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