PO-322
PO-322 is a selective SGK1 inhibitor with an IC50 of 54 nM. PO-322 reduces NDRG1 phosphorylation through inhibition of SGK1. PO-322 inhibits T cell proliferation and the production of IL-17, IFN-γ, and IL-6, accompanied by upregulated phosphorylation of p70S6K and STAT5. PO-322 exhibits immunosuppressive activity both in vitro and in vivo, and attenuates DNFB-induced delayed-type hypersensitivity and Imiquimod (HY-B0180)-induced psoriasis-like dermatitis. PO-322 is useful for research related to autoimmune diseases and psoriasis.
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- No. CAS: 91837-56-8
- Fòrmula: C15H10N4O2
- Peso molecular:278.27
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
SGK1 54 nM (IC50) |
IL-17 |
IL-6 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| PBMC | IC50 |
0.6 μM
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Inhibition of human T-cell proliferation in PBMCs following alloantigen stimulation, measured by CFSE labelling and flow cytometry after 72 hrs incubation.
Inhibition of human T-cell proliferation in PBMCs following alloantigen stimulation, measured by CFSE labelling and flow cytometry after 72 hrs incubation.
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31724152 |
| T-cell line | IC50 |
0.7 μM
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Inhibition of human T-cell proliferation following anti-CD3/anti-CD28 stimulation, measured by CFSE labelling and flow cytometry using the proliferation index after 72 hrs incubation.
Inhibition of human T-cell proliferation following anti-CD3/anti-CD28 stimulation, measured by CFSE labelling and flow cytometry using the proliferation index after 72 hrs incubation.
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31724152 |
In Vitro
PO-322 (1-1000 nM) is a highly selective SGK1 inhibitor that exhibits extremely high inhibitory activity against SGK1, with an inhibition rate of 98% and an IC50 of 54 nM[1].
PO-322 (0.125-8 μM; 72 h) inhibits human T cell proliferation after alloantigen stimulation with an IC50 of 0.6 μM[1].
PO-322 (0.125-8 μM; 72 h) inhibits human T cell proliferation after anti-CD3/anti-CD28 stimulation with an IC50 of 0.7 μM[1].
PO-322 (10-80 μM; 72 h) shows no significant cytotoxicity in resting T cells, IL-7-treated activated T cells, or PBMCs at high concentrations[1].
PO-322 inhibits the SGK1/NDRG1 signaling pathway in T cells while increasing p70S6K and STAT5 phosphorylation, without affecting Akt or ERK1/2[1].
PO-322 (0.5-8 μM; 24-48 h) does not induce apoptosis in activated human T cells at high concentrations[1].
PO-322 (0.125-2 μM; 48 h) inhibits the expression of pro-inflammatory cytokines IL-17, IFN-γ, and IL-6 in activated T cells, but does not affect the anti-inflammatory cytokine IL-10[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human T cells
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Concentration:0.125, 0.5, 2 and 8 μM
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Incubation Time:72 h
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Result:Inhibited human T-cell proliferation after anti-CD3 or anti-CD28 stimulation with an IC50 value of 0.7 μM.
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Cell Line:Activated human T cells
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Concentration:0.5, 2 and 8 μM
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Incubation Time:24 and 48 h
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Result:Did not induce activated T-cell apoptosis at 24 or 48 hr.
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Cell Line:Resting T cells, IL-7-treated activated T cells, and PBMCs
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Concentration:10, 20, 40 and 80 μM
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Incubation Time:72 h
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Result:Had no significant effects on the relative viability of resting T cells, IL-7-treated activated T cells, or PBMCs at 72 h.
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Cell Line:Activated T cells
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Concentration:0.125, 0.5 and 2 μM
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Incubation Time:48 h
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Result:Significantly inhibited IL-17, IFN-γ, and IL-6 expression.
Did not affect IL-10 expression.
In Vivo
PO-322 (10-40 mg/kg; i.p.; daily; 6 days) significantly reduces the severity of Imiquimod (HY-B0180)-induced dermatitis in mice[1].
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, 8-11 weeks old, DNFB-induced delayed-type hypersensitivity)[1]
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Dosage:2.5, 10, and 40 mg/kg
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Administration:i.p.; daily; 3 days
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Result:Markedly reduced ear swelling, including increases in ear thickness and patch weight, in a dose-dependent manner.
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Animal Model:BALB/c (female, Imiquimod-induced psoriasis-like dermatitis)[1]
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Dosage:10 or 40 mg/kg
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Administration:i.p.; daily; 6 days
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Result:Markedly reduced scaling and redness compared with the vehicle-treated group.
Significantly reduced histological scores, splenic mass, and total T-cell number in the spleen.
- Western Blot
- BrdU Incorporation Assay
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Research Protocol for Cancer Immunology
- Cell Viability Determination by MTT Colorimetric Assay
- Kinase activity and phosphorylation assays
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- PCNA Immunodetection Proliferation Assay
- Imiquimod-Induced Psoriasiform Dermatitis
- Protocol for Cell Counting and Cell Density Analysis
- TPA/Croton Oil Ear Edema and Dermatitis
- Contact Hypersensitivity Dermatitis
- Protocol for Kinase activity and phosphorylation assays
- MTT Cell Proliferation Assay
Chemical Information
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No. CAS 91837-56-8
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Peso molecular 278.27
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Fòrmula C15H10N4O2
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SMILES
O=C1NC2=C(/C1=N\NC3=NC4=C(O3)C=CC=C4)C=CC=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PO-322 Related Classifications
HY-187958 Related Classifications
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