IC-87114
IC87114 is a PI(3)Kδ selective inhibitor with IC50 of 50 nM.
It has been reported that IC87114 reduced FMLP-induced PIP3 synthesis and chemotaxis in neutrophils[1]. IC87114 also blocked TNF1α-stimulated elastase exocytosis from neutrophils in a mouse model of inflammation. A role for PI3Kδ in TNFα-induced signaling was demonstrated by a reduction in Akt-phosphorylation and PDK1 enzyme activity upon treatment of this cell type with IC87114 [2]. In human memory T cells, IC87114 largely inhibited T-cell receptor-induced PI(3)K signaling by both naive and effector. Cytokine production in memory T cells was blocked by IC87114 from healthy and allergic donors, or from inflammatory arthritis patients [3].
References:
[1]. Workman P, van Montfort RL. PI(3) kinases: revealing the delta lady. Nat Chem Biol. 2010 Feb;6(2):82-3.
[2]. Puri KD, Doggett TA, Douangpanya J, Hou Y, Tino WT, Wilson T, Graf T, Clayton E, Turner M, Hayflick JS, Diacovo TG. Mechanisms and implications of phosphoinositide 3-kinase delta in promoting neutrophil trafficking into inflamed tissue. Blood. 2004 May 1;103(9):3448-56.
[3]. Soond DR, Bj?rgo E, Moltu K, Dale VQ, Patton DT, Torgersen KM, Galleway F, Twomey B, Clark J, Gaston JS, Taskén K, Bunyard P, Okkenhaug K. PI3K p110delta regulates T-cell cytokine production during primary and secondary immune responses in mice and humans. Blood. 2010 Mar 18;115(11):2203-13.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 397.43 |
Cas No. | 371242-69-2 |
Formula | C22H19N7O |
Solubility | insoluble in H2O; insoluble in EtOH; ≥6.62 mg/mL in DMF |
Chemical Name | 2-[(6-aminopurin-9-yl)methyl]-5-methyl-3-(2-methylphenyl)quinazolin-4-one |
SDF | Download SDF |
Canonical SMILES | CC1=C2C(=CC=C1)N=C(N(C2=O)C3=CC=CC=C3C)CN4C=NC5=C4N=CN=C5N |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Description | IC-87114 is a selective inhibitor of PI3Kδ with an IC50 value of 0.5 μM. | |||||
Targets | PI3Kδ | PI3Kγ | PI3Kβ | |||
IC50 | 0.5 μM | 29 μM | 75 μM |
Quality Control & MSDS
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Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet