2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. Deltazinone 1

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。

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Deltazinone 1 Chemical Structure

Deltazinone 1 Chemical Structure

CAS No. : 894554-89-3

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Deltazinone 1 相关抗体

Top Publications Citing Use of Products

查看 Phosphodiesterase (PDE) 亚型特异性产品:

查看所有亚型
PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Deltazinone 1, a pyrazolopyridazinone, is a highly selective PDEδ inhibitor with a KD of 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].

IC50 & Target[2]

PDEδ

8 nM (Kd)

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]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Deltazinone 1 相关抗体:

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.
分子量

457.57

Formula

C27H31N5O2
CAS 号
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.
纯度 & 产品资料
参考文献

Deltazinone 1 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Deltazinone 1894554-89-3Deltazinone1Deltazinone-1Phosphodiesterase (PDE)pyrazolopyridazinonePDEδPDEδ-RasKRasPanc-Tu-IMIA PaCa-2Capan-1S6PInhibitorinhibitorinhibit

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HY-108436
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