IC-87114 |
カタログ番号GC15540 |
IC-87114 は、IC50 が 0.5 μM の強力かつ選択的な PI3Kδ 阻害剤です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 371242-69-2
Sample solution is provided at 25 µL, 10mM.
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, Bjørgo 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.
Cell experiment: | The murine macrophage cell line RAW264.7 and peritoneal macrophages from both types of mice are maintained in Dulbecco's modified Eagle's medium (DMEM) with 10% fetal calf serum (FCS). Cultures are maintained at 37°C in a humidified incubator in a 95% O2 plus 5% CO2 atmosphere. Cells are treated with varied concentrations of TNF-α and used IC-87114 (IC87114) to inhibit PtdIns(3,4,5)P3-dependent phosphorylation of Akt before TNF-α stimulation at early time points (30 min)[2]. |
Animal experiment: | Mice[3]BALB/c mice are immunized once by i.p. injection of 10 µg ovalbumin (OVA) in 0.2 ml of alu-Gel-S on day 0. Ten days later, mice are intranasally (i.n.) challenged with OVA (30 µg in 50 µL PBS) or PBS, once daily, over four consecutive days. To investigate if ERK1/2, PI3Kδ and NF-κB are signaling effectors downstream of EGFR transactivation, six treatment groups (A-F, 10-30 animals per group) are established. Mice in groups A and B are pretreated intranasally with 0.2 mL of the vehicle for the drugs. Groups C, D and E are pretreated with the same volume of three different drugs (PD 98059, IC-87114 and BAY 11-7085, respectively) at 10 mg/kg, 10 mg/kg and 0.3 mg/kg respectively, and group F with Dexamethasone (1 mg/kg), 1 h before each i.n. challenge with OVA. These doses are chosen from previous studies where they are shown to be effective. |
References: [1]. Sadhu C, et al. Essential role of phosphoinositide 3-kinase delta in neutrophil directional movement. J Immunol. 2003 Mar 1;170(5):2647-54. |
Cas No. | 371242-69-2 | SDF | |
Chemical Name | 2-[(6-aminopurin-9-yl)methyl]-5-methyl-3-(2-methylphenyl)quinazolin-4-one | ||
Canonical SMILES | CC1=C2C(=CC=C1)N=C(N(C2=O)C3=CC=CC=C3C)CN4C=NC5=C4N=CN=C5N | ||
Formula | C22H19N7O | M.Wt | 397.43 |
溶解度 | ≥ 6.6mg/mL in DMF | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
1 mM | 2.5162 mL | 12.5808 mL | 25.1617 mL |
5 mM | 0.5032 mL | 2.5162 mL | 5.0323 mL |
10 mM | 0.2516 mL | 1.2581 mL | 2.5162 mL |
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- Purity: >98.50%
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Average Rating: 5
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