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.
For research use only. We do not sell to patients.
- CAS No.: 2019223-60-8
- Formula: C26H34N8O
- Molecular Weight:474.60
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
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. Further protocols information, click here.
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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.
In Vivo
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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Molecular Weight 474.60
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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ROS/oxidative-stress fluorescent staining
ROS/oxidative-stress fluorescent staining uses cell-permeant fluorogenic probes that become fluorescent after oxidation inside cells or tissues; commonly used examples include DCFH-DA/DCFDA for broad cellular oxidant detection, DHE for superoxide-related signal detection, MitoSOX for mitochondrial superoxide-related signal detection, and CellROX probes for oxidative-stress-associated fluorescence readouts. The assay detects probe oxidation rather than a single ROS species unless the probe and analysis method have been chemically validated for that species. DCFH-DA enters cells, is deacetylated by intracellular esterases to DCFH, and produces fluorescent DCF after oxidation, so the readout is used as an operational measure of total cellular oxidative stress rather than a species-specific ROS measurement. DHE and MitoSOX can report superoxide-related oxidation, but red fluorescence alone can include non-specific ethidium-like oxidation products; HPLC or optimized spectral approaches are
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How to Choose the Right Model Animal
Choosing the right model animal is a validity-driven decision in which the species, strain, sex, age, genetic background, disease-induction method, outcome measures, and welfare burden must match the scientific question rather than laboratory tradition or convenience. A model should be selected by judging face validity, construct validity, and predictive validity: whether it resembles the human phenotype, whether it reproduces relevant mechanisms, and whether results are likely to predict human biology or treatment response. Animal studies often fail to translate because of species differences, weak disease resemblance, poor experimental design, inadequate reporting, publication bias, and underuse of randomization, blinding, and sample-size justification. Unresolved questions include how to rank competing models objectively, how much human-disease complexity must be reproduced for a given objective, and when non-animal systems such as organoids, ex vivo tissue, or computational models
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CPL302-253 Related Classifications
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