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

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.

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CPL302-253

CPL302-253 Chemical Structure

CAS No. : 2019223-60-8

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CPL302-253 Related Antibodies

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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Description

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].

In Vitro

CPL302-253 (150 nM-4 μM; assay-specific durations) inhibits biomarker expression and B cell proliferation in the activated CD19 B cell + PBMC BT co-culture system, with only minimal, low-magnitude activity in one other non-immune primary cell co-culture system[1].
CPL302-253 (1-10000 nM; 1 h pre-incubation, then 72 h with stimulants) inhibits CD25 expression and proliferation in activated primary human CD19+ B cells, with significant effects observed at concentrations as low as 10 nM[1].
CPL302-253 (1-10000 nM; 48 h) inhibits IFNγ production in activated primary human CD8+ T cells, with significant effects observed at concentrations as low as 1 nM[1].
CPL302-253 (1 μM; 72 h) inhibits IL-33 expression in A549 lung epithelial cells co-cultured with activated primary human CD8+ T cells[1].
CPL302-253 (1 μM; 30 min pre-incubation, then 6 h with stimulants) inhibits IL-8 production in primary human neutrophils stimulated with either CSE or LPS[1].
CPL302-253 (15 min before priming/stimulation, with total assay duration including 2 h post-LPS incubation), co-administered with dexamethasone, reduces ROS accumulation in primary human neutrophils activated with GM-CSF and LPS[1].
CPL302-253 (1 nM-100000 nM; 25 min) inhibits basophil activation, as measured by CD63 expression, with an IC50 of 36 nM[1].

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

CPL302-253 Related Antibodies

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.
In Vivo

CPL302-253 (0.5-5 mg/kg; i.n.; daily; 3 days) effectively blocks asthma-associated eosinophil lung infiltration and IL-33 production in a HDM-induced asthma mouse model[1].

MedChemExpress (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.
Molecular Weight

474.60

Formula

C26H34N8O
CAS No.
SMILES

CC(C)(C)N(CC1)CCN1CC2=NN(C(N3CCOCC3)=C4)C(N=C4C5=C6C=CNC6=CN=C5)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CPL302-253 Related Classifications

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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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