PI3Kδ-IN-28
PI3Kδ-IN-28 is an orally active and selective PI3Kδ inhibitor with an IC50 of 6.1 nM. PI3Kδ-IN-28 inhibits pro-inflammatory M1 macrophage polarization, promotes anti-inflammatory M2 phenotype, and alleviates pulmonary edema and inflammatory infiltration. PI3Kδ-IN-28 is applicable to research related to acute lung injury.
For research use only. We do not sell to patients.
- Formula: C29H25F3N6O2
- Molecular Weight:546.54
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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PI3Kδ |
MMP-9 |
MMP-12 |
Akt |
IL-4 |
PI3Kδ-IN-28 (compound 48) potently and selectively inhibits recombinant PI3Kδ with an IC50 of 6.1 nM, exhibiting >344-fold selectivity over other Class I PI3K isoforms[1].
PI3Kδ-IN-28 (10 μM) exhibits potent anti-inflammatory activity in LPS-stimulated RAW 264.7 cells by suppressing M1 proinflammatory responses and promoting M2 anti-inflammatory polarization[1].
PI3Kδ-IN-28 (0.1-10 μM) can dose-dependently inhibit the expression of MMP2, MMP9, and MMP12 at both the mRNA and protein levels in LPS-stimulated RAW 264.7 cells; it also inhibits the PI3K/AKT signaling pathway, and its efficacy is higher than that of idelalisib (HY-13026)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, 6-8 weeks old, intratracheal LPS-induced)[1]
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Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg
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Administration:p.o.; daily
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Result:Suppressed lung index notably, and 20 mg/kg exhibited better therapeutic potency than idelalisib.
Dropped lung wet/dry ratio significantly, matching the efficacy of idelalisib.
Exerted no aggravating impacts on LPS-elicited weight loss.
Alleviated pulmonary edema and hemorrhage in a dose-responsive fashion.
Lessened peripheral monocyte quantities at 20 mg/kg, with negligible shifts in total leukocytes, lymphocytes and neutrophils.
Maintained intact alveolar structure, inhibited inflammatory cell infiltration and lowered lung injury scores dose-dependently; the 20 mg/kg dosage outperformed idelalisib.
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Animal Model:C57BL/6J (male, 6-8 weeks old, intraperitoneal LPS-induced)[1]
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Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg
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Administration:p.o.; daily
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Result:Reduced lung index markedly, with 20 mg/kg exerting stronger effects than idelalisib.
Lowered lung wet-to-dry ratio at 20 mg/kg and displayed better edema relief than idelalisib.
Rescued LPS-triggered acute body weight loss at 20 mg/kg.
Suppressed pulmonary edema and hemorrhage dose-dependently, with peak protection at 20 mg/kg.
Cut total white blood cell and monocyte counts at 20 mg/kg, whereas 5 mg/kg elevated neutrophil levels.
Alleviated inflammatory infiltration, parenchymal injury and lung inflammation scores, and maintained alveolar structure in a dose-dependent fashion; 20 mg/kg outperformed idelalisib.
Chemical Information
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Molecular Weight 546.54
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Formula C29H25F3N6O2
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SMILES
CC1=NC=NC2=C1C=C(C=C2C3=CC=C(C(N4CCN(CC4)C(C)=O)=C3)C#N)C5=CC(C(F)(F)F)=C(N=C5)OC
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PI3Kδ-IN-28 Related Classifications
HY-184125 Related Classifications
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