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IPI-145(INK1197)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
IPI-145(INK1197)图片
CAS NO:1201438-56-3
规格:98%
分子量:416.86
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议
500mg电议
1g电议

产品介绍
PI3K-δ/PI3K-γ inhibitor
CAS:1201438-56-3
分子式:C22H17ClN6O
分子量:416.86
纯度:98%
存储:Store at -20°C

Background:

IPI-145 (also known as INK1197), an isoquinolinone derivative, is a small-molecule phosphoinositide-3 kinases (PI3K) inhibitor that selectively and potently inhibits two PI3K isoforms, PI3K-δ and PI3K-γ, with half maximal inhibition concentration IC50 of 2.5 nM and 27 nM respectively. Despite of preference for PI3K-δ and PI3K-γ, IPI-145 also inhibits other PI3K isoforms, PI3K-α and PI3K-β, to a lesser extent with IC50 of 1602 nM and 85 nM respectively.


Due to the essential role of PI3K-δ in the proliferation of B cell and T cell, IPI-145 exhibits potent anti-proliferative activity against both cells with IC50 of 0.5 nM and 9.5 nM respectively leading to inhibition of neutrophil migration and basophil activation.


Inhibition of immune function through IPI-145-induced PI3K-δ and PI3K-γ blockade potentiates its application in the treatment of multiple inflammatory, autoimmune and hematologic diseases.


参考文献:
[1] Winkler DG1, Faia KL, DiNitto JP, Ali JA, White KF, Brophy EE, Pink MM, Proctor JL, Lussier J, Martin CM, Hoyt JG, Tillotson B, Murphy EL, Lim AR, Thomas BD, Macdougall JR, Ren P, Liu Y, Li LS, Jessen KA, Fritz CC, Dunbar JL, Porter JR, Rommel C, Palombella VJ, Changelian PS, Kutok JL. PI3K-δ and PI3K-γ inhibition by IPI-145 abrogates immune responses and suppresses activity in autoimmune and inflammatory disease models. Chem Biol. 2013 Nov 21;20(11):1364-74. doi: 10.1016/j.chembiol.2013.09.017. Epub 2013 Nov 7.