| 名稱 | PIK-90 |
| 描述 | PIK-90, a DNA-PK and PI3K inhibitor, suppresses p110α( IC50=11 nM), p110γ(IC50=18 nM) and DNA-PK(IC50=13 nM) . |
| 細(xì)胞實(shí)驗(yàn) | For viabilty, cells are seeded in 12-well plates in the presence of PIK-90 for 3 days. Cell viability is determined using a WST-1 assay.(Only for Reference) |
| 激酶實(shí)驗(yàn) | Expression and Assay of p110α/p85α, p110β/p85α, p110δ/p85α, and p110γ : IC50 values are measured using either a standard TLC assay for lipid kinase activity or a high-throughput membrane capture assay. Kinase reactions are performed by preparing a reaction mixture containing kinase, inhibitor (2% DMSO final concentration), buffer (25 mM HEPES, pH 7.4, 10 mM MgCl2), and freshly sonicated phosphatidylinositol (100 μg/mL). Reactions are initiated by the addition of ATP containing 10 μCi of γ-32P-ATP to a final concentration 10 μM or 100 μM, and allowed to proceed for 20 minutes at room temperature. For TLC analysis, reactions are then terminated by the addition of 105 μL 1N HCl followed by 160 μL CHCl3:MeOH (1:1). The biphasic mixture is vortexed, briefly centrifuged, and the organic phase transferred to a new tube using a gel loading pipette tip precoated with CHCl3. This extract is spotted on TLC plates and developed for 3-4 hours in a 65:35 solution of n-propanol:1M acetic acid. The TLC plates are then dried, exposed to a phosphorimager screen, and quantitated. For each compound, kinase activity is typically measured at 10-12 inhibitor concentrations representing two-fold dilutions from the highest concentration tested (100 μM). For compounds showing significant activity, IC50 determinations are repeated two to four times, and the reported value is the average of these independent measurements. |
| 體外活性 | 胰島素刺激的動物,PIK-90（10 mg/kg）處理,能夠抑制由胰島素刺激產(chǎn)生的血糖降低. |
| 體內(nèi)活性 | 在慢性淋巴細(xì)胞白血病細(xì)胞中,PIK-90（1-10 μM ）處理,抑制趨化性,明顯抑制細(xì)胞遷移進(jìn)入基質(zhì)細(xì)胞層,降低CXCL12誘導(dǎo)的肌動蛋白聚合。在dHL60細(xì)胞中,PIK-90抑制fMLP刺激的Akt磷酸化,損害極性和趨化性。在膠質(zhì)瘤細(xì)胞系中（U87 MG, SF188, SF763, LN229, A1207和LN-Z30細(xì)胞）,PIK-90阻斷Akt磷酸化,抑制細(xì)胞增殖。 |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | Ethanol : < 0.2 mg/mL (insoluble or slightly soluble)
DMSO : < 0.2 mg/mL (insoluble or slightly soluble), Sonication is recommended.
H2O : < 0.2 mg/mL (insoluble or slightly soluble)
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| 關(guān)鍵字 | Inhibitor | DNA-PK | PIK90 | PIK-90 | PI3K | Phosphoinositide 3-kinase | DNA-dependent protein kinase | PIK 90 | inhibit |
| 相關(guān)產(chǎn)品 | (2S,3R,4S)-4-Hydroxyisoleucine | AS-605240 | Quercetin | Quercetin Dihydrate | Apilimod | Bimiralisib | GDC0084 | Myricetin | Duvelisib (R enantiomer) hydrochloride | Isoprenaline hydrochloride | Erucic acid | Sapanisertib |
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