2. PI3K/Akt/mTOR Immunology/Inflammation Metabolic Enzyme/Protease
  3. PI3K Interleukin Related MMP Akt
  4. 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.

PI3Kδ-IN-28

PI3Kδ-IN-28 Chemical Structure

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

PI3Kδ-IN-28 Related Antibodies

Top Publications Citing Use of Products

View All PI3K Isoform Specific Products:

View All Isoforms
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

View All Interleukin Related Isoform Specific Products:

View All Isoforms
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

View All MMP Isoform Specific Products:

View All Isoforms
MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8 MMP-19

View All Akt Isoform Specific Products:

View All Isoforms
Akt Akt1 Akt2 Akt3

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

IC50 & Target[1]

PI3Kδ

 

MMP-9

 

MMP-12

 

Akt

 

IL-4

 

In Vitro

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.

PI3Kδ-IN-28 Related Antibodies
Parmacokinetics
Species Dose Route T1/2 Cmax Tmax AUC0-t AUC0-∞ Bioavailability
Mice[1] 3 mg/kg i.v. 3.24 h 4564 ng/mL 0.08 h 16288 ng·h/mL 17092 ng·h/mL /
Mice[1] 30 mg/kg p.o. 2.64 h 8170 ng/mL 2.67 h 87135 ng·h/mL 87532 ng·h/mL 53.5 %
In Vivo

PI3Kδ-IN-28 (compound 48) (5-20 mg/kg; p.o.; daily) dose-dependently attenuates LPS-induced acute lung injury and septic lung injury in male C57BL/6J mice, with the efficacy at the dose of 20 mg/kg being superior to that of idelalisib[1].

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

Animal Model: C57BL/6J (male, 6-8 weeks old, intratracheal LPS-induced)[1]
Dosage: 5 mg/kg; 10 mg/kg; 20 mg/kg
Administration: p.o.; daily
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.
Animal Model: C57BL/6J (male, 6-8 weeks old, intraperitoneal LPS-induced)[1]
Dosage: 5 mg/kg; 10 mg/kg; 20 mg/kg
Administration: p.o.; daily
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.
Molecular Weight

546.54

Formula

C29H25F3N6O2
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
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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

PI3Kδ-IN-28 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

PI3Kδ-IN-28PI3KInterleukin RelatedMMPAktPhosphoinositide 3-kinaseILMatrix metalloproteinasesPKBProtein kinase Bpulmonary edemaRAW 264.7 cellsC57BL/6J micePI3K/AKT signalingPI3Kδacute lung injuryM1 macrophage polarizationM2 phenotypeseptic lung injuryinflammatory infiltrationInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PI3Kδ-IN-28
Cat. No.:
HY-184125
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.