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)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CAPAN-1 IC50
48 μM
Compound: 2
Antiproliferative activity against KRAS-dependent human Capan1 cells after 48 hrs by CCK8 assay
Antiproliferative activity against KRAS-dependent human Capan1 cells after 48 hrs by CCK8 assay
[PMID: 29510040]
CAPAN-1 IC50
56.9 μM
Compound: S2
Antiproliferative activity against KRAS-dependent human Capan1 cells after 48 hrs by CCK8 assay
Antiproliferative activity against KRAS-dependent human Capan1 cells after 48 hrs by CCK8 assay
[PMID: 28929751]
HCT-116 IC50
74 μM
Compound: 2
Antiproliferative activity against human HCT116 cells incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human HCT116 cells incubated for 72 hrs by CCK8 assay
[PMID: 32603594]
HCT-116 IC50
82.4 μM
Compound: 1
Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition and measured after 72 hrs by CCK8 assay
Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition and measured after 72 hrs by CCK8 assay
[PMID: 35178186]
SW480 IC50
18.3 μM
Compound: 1
Antiproliferative activity against human SW480 cells assessed as cell growth inhibition and measured after 72 hrs by CCK8 assay
Antiproliferative activity against human SW480 cells assessed as cell growth inhibition and measured after 72 hrs by CCK8 assay
[PMID: 35178186]
SW480 IC50
56 μM
Compound: 2
Antiproliferative activity against human SW480 cells incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human SW480 cells incubated for 72 hrs by CCK8 assay
[PMID: 32603594]
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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  • 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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