PIK-294

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种高效、选择性 p110δ 抑制剂，IC50 为 10 nM。

A highly potent, selective p110δ inhibitor with IC50 of 10 nM; shows 1000-, 49- and 16-fold less potent to PI3Kα/β/γ.

Analysis of the specific Class I PI3 Kinase catalytic isoforms p110α (IC50=10 μM), p110β (IC50=0.49 μM), p110δ (IC50=0.01 μM) and p110γ (IC50=0.16 μM) using the inhibitor PIK-294 indicates differential roles in CXCL8-induced neutrophil migration. PIK-294 inhibits both chemokinetic and chemotactic CXCL8-induced migration. When cells are pre-treated with the PI3Kδ selective inhibitor PIK-294,CXCL8-induced migration in the non-gradient and the gradient assay is significantly inhibited. PIK-294 is used at two concentrations 1 μM and 10 μM. Pre-treatment with 1 μM inhibits migration to a greater extent in the non-gradient assay than in the gradient assay. Pre-treatment with 10 μM inhibits migration to a significantly greater extent than the lower dose in both assays. Prior to stimulation with CXCL8, pre-treatment of the cells with the PI3K inhibitors, Wortmannin (50 nM), PIK-294 (10 μM) and AS-605240 (10 μM) for 2 minutes, cause a reduction in the phosphorylation of Akt.Pre-treatment of cells prior to stimulation with GM-CSF and the DMSO control with the PI3K inhibitors Wortmannin (50 nM), PIK-294 (10 μM) and AS-605240 (10 μM) for 2 minutes, reduce the phosphorylation of Akt (p<0.05 for inhibition of PI3Kδ).

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PIK294 | PIK 294 | PIK-294

PI3K/Akt/mTOR signaling

PI3K

p110α|p110β|p110γ|p110δ

Cancer

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900185-02-6

489.5279

C28H23N7O2

>98% (HPLC)

DMSO: ≥ 40 mg/mL

O=C1N(C2=CC=CC=C2C)C(CN3N=C(C4=CC=CC(O)=C4)C5=C(N)N=CN=C53)=NC6=C1C(C)=CC=C6

4(3H)-Quinazolinone, 2-[[4-amino-3-(3-hydroxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]methyl]-5-methyl-3-(2-methylphenyl)-

(-20℃)

With Ice Pack

≥ 2 years