2. PI3K/Akt/mTOR Immunology/Inflammation
  3. PI3K Akt PD-1/PD-L1 Interleukin Related CD3
  4. PI3Kδ-IN-25

PI3Kδ-IN-25 是一种具有口服活性的选择性的 PI3Kδ 抑制剂 (IC50 = 2.1 nM)。PI3Kδ-IN-25 对 PI3Kα，PI3Kγ，PI3Kβ 的 IC50 分别为 272，285，1171 nM。PI3Kδ-IN-25 在 B16F10 细胞中抑制 AKT Ser473 磷酸化，抑制 Treg 细胞增殖并下调 PD-L1 的表达。PI3Kδ-IN-25 在 B16F10 黑色素瘤和 Lewis 肺癌小鼠模型中通过减少肿瘤浸润 Treg 细胞并增强免疫反应发挥抗癌功效。PI3Kδ-IN-25 可用于黑色素瘤，肺癌等癌症的研究。

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PI3Kδ-IN-25

PI3Kδ-IN-25 Chemical Structure

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PI3Kδ-IN-25 相关抗体

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查看 PI3K 亚型特异性产品:

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PI3Kδ-IN-25 is an orally active selective PI3Kδ inhibitor (IC50 = 2.1 nM). PI3Kδ-IN-25 has IC50s of 272, 285, and 1171 nM for PI3Kα, PI3Kγ, and PI3Kβ, respectively. PI3Kδ-IN-25 inhibits AKT Ser473 phosphorylation, suppresses Treg cell proliferation, and downregulates PD-L1 expression in B16F10 cells. PI3Kδ-IN-25 exhibits anticancer effects in B16F10 melanoma and Lewis lung cancer mouse models by reducing tumor-infiltrating Treg cells and enhancing immune responses. PI3Kδ-IN-25 is potentially useful in the study of melanoma, lung cancer, and other cancers[1].

IC50 & Target[1]

PI3Kδ

2.1 nM ()

体外研究
(In Vitro)

PI3Kδ-IN-25 (Compound 18) (1 μM) 可抑制 PIK3CD (93.37%)、PIK3CG (87.63%) 和 PIK3CA (107.38%)，而对 RIPK2 (58.65%) 和 PIK3CB (42.68%) 仅表现出中等活性[1]。
PI3Kδ-IN-25 (96 小时) 对 Ramos、DOHH2、Hela、BxPC3、SGC7901、BGC823、MX-1、A375、B16F10 细胞表现出抗增殖活性，IC500 分别为 18.11、14.39、29.51、22.13、15.81、13.06、25.43、21.95， 11.42 μM，对 K562、HepG2、MCF-7 细胞表现出较弱的抗增殖活性，IC50 > 50 μM[1]。
PI3Kδ-IN-25 (1-10 μM，5-30 分钟) 可抑制 AKT Ser473 位点的磷酸化，表明其可有效阻断 B16F10 细胞中的 PI3K 信号通路[1]。
PI3Kδ-IN-25 (1-10 μM，72 小时) 可降低 CD4/CD25/FOXP3+++ 的比例以及 mIL-2 和 hTGFβ 诱导的 Treg 细胞中的 IL-10 浓度[1]。
PI3Kδ-IN-25 (1-10 μM， 72 小时) 在 10 μM 时下调 B16F10 细胞中的 PD-L1 表达[1]。

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

PI3Kδ-IN-25 相关抗体:

Western Blot Analysis[1]

Cell Line: B16F10 cells
Concentration: 1 μM, 3 μM, 10 μM
Incubation Time: 5 min, 15min, 30 min
Result: Inhibited AKT phosphorylation at Ser473.
体内研究
(In Vivo)

PI3Kδ-IN-25 (Compound 18) (1-30 mg/kg, 口服, 每天两次) 通过调节 B16F10 异种移植黑色素瘤和 Lewis 异种移植小鼠模型中的肿瘤微环境来抑制肿瘤生长[1]。

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

Animal Model: B16F10 xenograft (1.8 × 106) mouse (male C57BL/6J) melanoma model [1]
Dosage: 1 mg/kg, 3 mg/kg, 30 mg/kg
Administration: o.p., twice daily
Result: Resulted significant inhibition of pAKT(S473) levels at a single oral dose of 30 mg/kg. Inhibited tumor growth, increased level of leukocytes, T cells, and especially CD8 T cells, elevated the expression of CD3, suppressed the expression of PD-1 and PD-L1.
Animal Model: Lewis xenograft (1 × 106) mouse (male C57BL/6J) model[1]
Dosage: 1 mg/kg, 3 mg/kg, 30 mg/kg
Administration: o.p., twice daily
Result: Inhibited tumor growth, increased level of leukocytes, T cells, and especially CD8 T cells, decreased tumor-infiltrating Treg cells.
分子量

552.67

Formula

C26H28N6O4S2
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

PI3Kδ-IN-25 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:

PI3Kδ-IN-25PI3KAktPD-1/PD-L1Interleukin RelatedCD3Phosphoinositide 3-kinasePKBProtein kinase BPD-1/Programmed death-ligand 1ILCluster of differentiation 3InhibitorB16F10 cellsLewis lung cancer mousemelanomainhibitorinhibit

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