2. Metabolic Enzyme/Protease MAPK/ERK Pathway PI3K/Akt/mTOR Stem Cell/Wnt
  3. Phosphodiesterase (PDE) p38 MAPK Akt mTOR ERK
  4. Deltafluorine

Deltafluorine 是一种磷酸二酯酶 δ (PDEδ) 抑制剂，其 IC50 为 27 nM，KD 为 148 nM。Deltafluorine 可共价修饰 PDEδ 配体结合位点中的特异性谷氨酸残基 p.E88，干扰其分子伴侣功能。Deltafluorine 可抑制 MAPK 和 Akt-mTOR 通路的信号传导，降低 ERK1/2 的表达水平。Deltafluorine 可在 Kras 驱动的肺腺癌自发性小鼠模型中减小肿瘤体积。Deltafluorine 可用于肺腺癌的相关研究。

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Deltafluorine

Deltafluorine Chemical Structure

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Deltafluorine 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

查看 p38 MAPK 亚型特异性产品:

查看所有亚型
p38 MAPK p38α p38β MAPK13 p38δ p38γ

查看 Akt 亚型特异性产品:

查看所有亚型
Akt Akt1 Akt2 Akt3

查看 mTOR 亚型特异性产品:

查看所有亚型
mTOR mTORC1 mTORC2

查看 ERK 亚型特异性产品:

查看所有亚型
ERK ERK1 ERK2 ERK5 ERK8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Deltafluorine is a phosphodiesterase delta (PDEδ) inhibitor with an IC50 of 27 nM, a KD of 148 nM. Deltafluorine covalently modifies the specific glutamate residue p.E88 in the ligand binding site of PDEδ, interfering with its chaperone function. Deltafluorine inhibits signaling through the MAPK and Akt-mTOR pathway, reduces ERK1/2 expression. Deltafluorine reduces tumor volume in an autochthonous mouse model of Kras-driven lung adenocarcinoma. Deltafluorine can be used for the research of lung adenocarcinoma[1].

IC50 & Target[1]

PDEδ

27 nM (IC50)

PDEδ

148 nM (Kd)

ERK1

 

ERK2

 

体外研究
(In Vitro)

Deltafluorine (Compound 22a) (60 μM；0-7 天) 在体外可于 7 天内以高于 85% 的效率共价修饰纯化的 PDEδ 的 p.E88 残基，其二级速率常数为 5.4 M−1 s−1[1]。
Deltafluorine (10 μM；2 h) 可在 Jurkat 细胞中诱导 PDEδ 发生显著的热稳定性变化，其 ΔTm为 16.6 ± 3.2 °C[1]。
Deltafluorine (5 μM；0.25-4 h) 可降低 PA-TU-8902 细胞中 ERK1/2 和 S6 的磷酸化水平[1]。
Deltafluorine (5 μM；0-120 h) 可抑制 PA-TU-8902 细胞增殖，细胞生长抑制率为 84 ± 2%[1]。
Deltafluorine (5 μM; 2 h) 可在 PA-TU-8902 细胞中抑制 MAPK 和 Akt-mTOR 通路[1]。

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

Deltafluorine 相关抗体:

Western Blot Analysis[1]

Cell Line: PA-TU-8902 cells
Concentration: 5 μM
Incubation Time: 0.25, 0.5, 1, 2, 4 h
Result: Reduced phosphorylation of ERK1/2 (Thr202/Tyr204) and S6 (S235/236) in PA-TU-8902 cells over the time course.

Cell Proliferation Assay[1]

Cell Line: PA-TU-8902 cells
Concentration: 5 μM
Incubation Time: 4 h treatment + 20 h wash-out regimen over 4 days
Result: Inhibited growth of PA-TU-8902 cells with 84 ± 2% growth inhibition under wash-out conditions.
体内研究
(In Vivo)

Deltafluorine (Compound 22a) (15 mg/kg; 腹腔注射; 每日；连续 21 天) 处理可在由 Kras 驱动的高侵袭性肺腺癌小鼠模型中显著抑制肿瘤生长[1]。

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

Animal Model: KrasLSL.G12D/wt; Trp53fl/fl (KP mice; autochthonous lung adenocarcinoma model induced by intratracheal Adeno-CMV-Cre instillation)[1]
Dosage: 15 mg/kg
Administration: I.p.; daily; 21 days
Result: Reduced tumor load by 42% compared to untreated controls.
Lowered lung tumor volume occupancy to 21.6% versus 47.5% in untreated controls.
分子量

677.29

Formula

C33H42ClFN4O4S2
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

Deltafluorine 相关分类

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  • 稀释计算器

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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:

DeltafluorinePhosphodiesterase (PDE)p38 MAPKAktmTORERKPKBProtein kinase BMammalian target of RapamycinExtracellular signal regulated kinasesMAP-kinase pathwayKrasG12DJurkatglutathioneAkt-mTORPhosphodiesterase delta (PDEδ)PA-TU-8902 cellsInhibitorinhibitorinhibit

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