Deltazinone 1 是一种吡唑并哒嗪酮，是一种高度选择性的PDEδ抑制剂，KD为 8 nM。Deltazinone 1 抑制 PDEδ-Ras 相互作用。Deltazinone 1 显示出剂量依赖性抑制致癌 KRas 依赖性细胞系增殖。
| 生物活性 | Deltazinone 1, a pyrazolopyridazinone, is a highly selectivePDEδinhibitor with aKDof 8 nM. Deltazinone 1 inhibits the PDEδ-Ras interaction. Deltazinone 1 shows a dose-dependent inhibitory response on proliferation in oncogenic KRas-dependent cell lines[1][2]. |
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体外研究
(In Vitro) | Deltazinone 1 (0.375-24 μM; 0-120 小时) 以剂量依赖性方式抑制细胞生长[1]。
Deltazinone 1 (20 μM; 1小时) 降低 KRas 依赖性 Panc-Tu-I 细胞中的 S6P 磷酸化[1]。
Deltazinone 1 (10μM) 显示致癌 KRas 依赖性 Panc-Tu-I 细胞死亡，但不显示致癌 KRas 非依赖性 PANC-1 细胞[1]。
Cell Viability Assay[1] | Cell Line: | Panc-Tu-I, MIA PaCa-2, Capan-1 cells | | Concentration: | 0.375, 0.75, 1.5, 3, 6, 12, 24 μM | | Incubation Time: | 0-120 h | | Result: | Inhibited cell growth in a dose-dependent manner already observable at sub-μM concentrations.
At doses higher than 3 μM decreasing cell indices indicated cell death ~30 h in Panc-Tu-I cells and after ~40 h in MIA PaCa-2.
Doses up to 24 μM led to strong growth inhibition but not cell death in the Capan-1 cell line. |
Western Blot Analysis[1] | Cell Line: | Panc-Tu-I cells | | Concentration: | 20 μM | | Incubation Time: | 1 h | | Result: | Reduced S6P phosphorylation in the KRas-dependent Panc-Tu-I cells.
Did not significantly affect Erk response to EGF. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
