2. PI3K/Akt/mTOR Immunology/Inflammation Metabolic Enzyme/Protease NF-κB
  3. PI3K IFNAR Reactive Oxygen Species (ROS) Interleukin Related
  4. CPL302-253

CPL302-253 是一种 PI3Kδ 抑制剂，其 IC50 为 12.20 nM，人源 Ka 为 0.85 nM。CPL302-253 可在功能上调控 PI3Kδ 活性，阻断免疫细胞 IFNγ、IL-33、ROS 生成并影响免疫功能。CPL302-253 在哮喘小鼠模型中能够阻断诱发哮喘的炎症反应进程。CPL302-253 可用于哮喘的相关研究。

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CPL302-253

CPL302-253 Chemical Structure

CAS No. : 2019223-60-8

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CPL302-253 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CPL302-253 is a PI3Kδ inhibitor with an IC50 of 12.20 nM and a human Ka of 0.85 nM. CPL302-253 functionally regulates PI3Kδ activity, blocks the production of IFNγ, IL-33 and ROS in immune cells, and affects immune function. CPL302-253 blocks the progression of asthma-inducing inflammatory responses in a mouse model of asthma. CPL302-253 can be used for research related to asthma[1].

体外研究
(In Vitro)

CPL302-253 (150 nM-4 μM) 可抑制活化 CD19 B 细胞+PBMC BT 共培养体系中的 IL-2、IL-6、IL-17 和 TNFα 表达及 B 细胞增殖[1]。
CPL302-253 (1-10000 nM; 1 h pre-incubation, then 72 h with stimulants) 可抑制活化的人原代 CD19+ B 细胞中 CD25 的表达与增殖[1]。
CPL302-253 (1-10000 nM; 48 h) 可抑制活化的人原代 CD8+ T 细胞中 IFNγ 的产生[1]。
CPL302-253 (1 μM; 72 h) 可抑制与活化的人原代 CD8+ T 细胞共培养的 A549 肺上皮细胞中 IL-33 的表达[1]。
CPL302-253 (1 μM; 30 min pre-incubation, then 6 h with stimulants) 可抑制经 CSE 或 LPS (HY-D1056) 刺激的人原代中性粒细胞中 IL-8 的产生[1]。
CPL302-253 与 Dexamethasone (HY-14648) 联合，可降低经 GM-CSF 和 LPS 活化的人原代中性粒细胞中的 ROS 累积[1]。
CPL302-253 (1 nM-100000 nM; 25 min) 可抑制嗜碱性粒细胞活化 (以 CD63 表达水平为检测指标)，其 IC50 为 36 nM[1]。

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

CPL302-253 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: Normal Human Bronchial Epithelial (NHBE) cells
Concentration: 0, 0.0457, 0.137,
0.412, 1.24, 3.7, 11.1, 33.3, 100 μM
Incubation Time: 48 h
Result: Did not affect any measured cell health parameters at concentrations below 10 μM.
Had a minimum effective concentration (MEC) ranging from 10.6 μM to 75.3 μM for each cell health parameter.
Had an AC50 for all measured cell health parameters greater than 100 μM.

ELISA Assay[1]

Cell Line: co-culture of A549 lung epithelial cells and primary human CD8+ T cells isolated from PBMC
Concentration: 1 μM
Incubation Time: 72 h
Result: Strongly inhibited IL-33 expression in A549 cells co-cultured with activated CD8+ T cells, resulting in significantly lower normalized IL-33 levels compared to untreated co-cultures.
体内研究
(In Vivo)

CPL302-253 (0.5-5 mg/kg；经鼻给药；每日 1 次；连续 3 天) 可在屋尘螨 (HDM) 诱导的哮喘小鼠模型中有效阻断哮喘相关的嗜酸性粒细胞肺部浸润及 IL-33 的产生[1]。

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

Animal Model: Balb/c (female, 18-25 g bodyweight, HDM-induced asthma model)[1]
Dosage: 0.5 mg/kg; 5 mg/kg
Administration: i.n.; daily; 3 days
Result: Reduced eosinophil numbers to near naive levels and nearly eliminated IL-33 elevation at 0.5 mg/kg dose.
Significantly reduced eosinophil counts and IL-33 concentrations at 5 mg/kg dose.
Blocked eosinophil influx to the lungs and reduced IL-33 production in BAL fluid compared to HDM-challenged vehicle controls for both doses.
分子量

474.60

Formula

C26H34N8O
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

CPL302-253 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:

CPL302-2532019223-60-8PI3KIFNARReactive Oxygen Species (ROS)Interleukin RelatedPhosphoinositide 3-kinaseInterferon-α/β receptorInterferon-alpha/beta receptor ILPI3KδCD8+ T cellsA549 lung epithelial cellsprimary human neutrophilshuman kinasesCD19+ B cellsimmune functionsasthmaclass I PI3K isoformsinflammatory processesInhibitorinhibitorinhibit

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