CPL302-253
CPL302-253 is a PI3Kδ inhibitor with an IC50 of 12.20 nM and a human Kd 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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- CAS No.: 2019223-60-8
- Formule: C26H34N8O
- Masse moléculaire:474.60
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
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.
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Cell Line:Normal Human Bronchial Epithelial (NHBE) cells
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Concentration:0, 0.0457, 0.137,
0.412, 1.24, 3.7, 11.1, 33.3, 100 μM -
Incubation Time:48 h
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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.
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Cell Line:co-culture of A549 lung epithelial cells and primary human CD8+ T cells isolated from PBMC
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Concentration:1 μM
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Incubation Time:72 h
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c (female, 18-25 g bodyweight, HDM-induced asthma model)[1]
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Dosage:0.5 mg/kg; 5 mg/kg
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Administration:i.n.; daily; 3 days
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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.
Chemical Information
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CAS No. 2019223-60-8
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Masse moléculaire 474.60
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Formule C26H34N8O
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SMILES
CC(C)(C)N(CC1)CCN1CC2=NN(C(N3CCOCC3)=C4)C(N=C4C5=C6C=CNC6=CN=C5)=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)