1. PI3K/Akt/mTOR Immunology/Inflammation
  2. PI3K Akt PD-1/PD-L1 Interleukin Related CD3
  3. PI3Kδ-IN-25

PI3Kδ-IN-25 is an orally active selective PI3Kδ inhibitor (IC50 = 2.1 nM). PI3Kδ-IN-25 has IC50s of 272, 285, and 1171 nM for PI3Kα, PI3Kγ, and PI3Kβ, respectively. PI3Kδ-IN-25 inhibits AKT Ser473 phosphorylation, suppresses Treg cell proliferation, and downregulates PD-L1 expression in B16F10 cells. PI3Kδ-IN-25 exhibits anticancer effects in B16F10 melanoma and Lewis lung cancer mouse models by reducing tumor-infiltrating Treg cells and enhancing immune responses. PI3Kδ-IN-25 is potentially useful in the study of melanoma, lung cancer, and other cancers.

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PI3Kδ-IN-25

PI3Kδ-IN-25 Chemical Structure

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Description

PI3Kδ-IN-25 is an orally active selective PI3Kδ inhibitor (IC50 = 2.1 nM). PI3Kδ-IN-25 has IC50s of 272, 285, and 1171 nM for PI3Kα, PI3Kγ, and PI3Kβ, respectively. PI3Kδ-IN-25 inhibits AKT Ser473 phosphorylation, suppresses Treg cell proliferation, and downregulates PD-L1 expression in B16F10 cells. PI3Kδ-IN-25 exhibits anticancer effects in B16F10 melanoma and Lewis lung cancer mouse models by reducing tumor-infiltrating Treg cells and enhancing immune responses. PI3Kδ-IN-25 is potentially useful in the study of melanoma, lung cancer, and other cancers[1].

IC50 & Target[1]

PI3Kδ

2.1 nM ()

In Vitro

PI3Kδ-IN-25 (Compound 18) (1 μM) inhibits PIK3CD (93.37%), PIK3CG (87.63%) and PIK3CA (107.38%) while showing only moderate activity against RIPK2 (58.65%) and PIK3CB (42.68%)[1].
PI3Kδ-IN-25 (96 h) shows antiproliferative activities against Ramos, DOHH2, Hela, BxPC3, SGC7901, BGC823, MX-1, A375, B16F10 cells, with IC50s of 18.11, 14.39, 29.51, 22.13, 15.81, 13.06, 25.43, 21.95, 11.42 μM, respectively, shows weak antiproliferative activities against K562, HepG2, MCF-7 cells, with IC50s > 50 μM[1].
PI3Kδ-IN-25 (1-10 μM, 5-30 min) inhibits the phosphorylation of AKT at Ser473, suggesting an effective blockade of the PI3K signaling pathway in B16F10 cells[1].
PI3Kδ-IN-25 (1-10 μM, 72 h) reduces the ratio of CD4/CD25/FOXP3+++, the concentration of IL-10 in mIL-2 and hTGFβ induced Treg cells[1].
PI3Kδ-IN-25 (1-10 μM, 72 h) down-regulates of PD-L1 expression in B16F10 cells at 10 μΜ[1].

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

Western Blot Analysis[1]

Cell Line: B16F10 cells
Concentration: 1 μM, 3 μM, 10 μM
Incubation Time: 5 min, 15min, 30 min
Result: Inhibited AKT phosphorylation at Ser473.
In Vivo

PI3Kδ-IN-25 (Compound 18) (1-30 mg/kg, o.p., twice daily) inhibits tumor growth by regulating the tumor microenvironment in B16F10 xenograft melanoma and Lewis xenograft mouse model[1].

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

Animal Model: B16F10 xenograft (1.8 × 106) mouse (male C57BL/6J) melanoma model [1]
Dosage: 1 mg/kg, 3 mg/kg, 30 mg/kg
Administration: o.p., twice daily
Result: Resulted significant inhibition of pAKT(S473) levels at a single oral dose of 30 mg/kg. Inhibited tumor growth, increased level of leukocytes, T cells, and especially CD8 T cells, elevated the expression of CD3, suppressed the expression of PD-1 and PD-L1.
Animal Model: Lewis xenograft (1 × 106) mouse (male C57BL/6J) model[1]
Dosage: 1 mg/kg, 3 mg/kg, 30 mg/kg
Administration: o.p., twice daily
Result: Inhibited tumor growth, increased level of leukocytes, T cells, and especially CD8 T cells, decreased tumor-infiltrating Treg cells.
Molecular Weight

552.67

Formula

C26H28N6O4S2

SMILES

O=C(N1CC[C@H](NC2=NC=NC3=C2C=C(C4=CC(NS(C5=CC=C(C=C5)C)(=O)=O)=C(N=C4)OC)S3)C1)CC

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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  • 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.

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PI3Kδ-IN-25
Cat. No.:
HY-175369
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