PI3K/AKT/JAK2-IN-1
PI3K/AKT/JAK2-IN-1 is a potent multi-target inhibitor of the PI3K/AKT/JAK2 signaling pathway. PI3K/AKT/JAK2-IN-1 suppresses NO production (IC50 = 1.0 μM), reduces pro-inflammatory cytokines (TNF-α, IL-6, IL-1β, IL-17A, IL-22), and inhibits keratinocyte hyperproliferation by downregulating Ki67 and PCNA. PI3K/AKT/JAK2-IN-1 can be used for psoriasis research.
For research use only. We do not sell to patients.
- Formula: C25H14Cl2O7
- Molecular Weight:497.28
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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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IL-1β |
IL-17A |
IL-22 |
IL-6 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| RAW264.7 | CC50 |
40 μM
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Exhibits low cytotoxicity toward RAW264.7 cells for 24h.
Exhibits low cytotoxicity toward RAW264.7 cells for 24h.
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42235429 |
PI3K/AKT/JAK2-IN-1 (compound 15) (5-20 μM; 24 h) exhibits low cytotoxicity toward RAW264.7 cells, with a CC50 > 40 μM [1].
PI3K/AKT/JAK2-IN-1 (5-20 μM; 26 h) shows dose-dependent inhibition of NO production in LPS (HY-D1056)-stimulated RAW264.7 cells, with an IC50 of 1.0 μM [1].
PI3K/AKT/JAK2-IN-1(5-20 μM; 26 h) significantly inhibits the production of TNF-α, IL-6, and IL-1β in LPS-stimulated RAW264.7 cells [1].
PI3K/AKT/JAK2-IN-1 (5-20 μM; 24 h) does not significantly impair HaCaT cell viability [1].
PI3K/AKT/JAK2-IN-1 (5-20 μM; 26 h) significantly reduces the levels of IL-17A and IL-22 in IL-1β-stimulated HaCaT cells [1].
PI3K/AKT/JAK2-IN-1 shows strong binding to PI3K, AKT, JAK2, mTOR, and P62 in molecular docking analysis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAW264.7 cells
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Concentration:5, 10, or 20 μM
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Incubation Time:24 h
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Result:Exhibited low cytotoxicity toward RAW264.7 cells at all tested concentrations, with a CC50 > 40 μM.
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Cell Line:HaCaT cells
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Concentration:5, 10, or 20 μM
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Incubation Time:24 h
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Result:Did not impair HaCaT cell viability at all tested concentrations.
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Cell Line:RAW264.7 cells
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Concentration:5, 10, or 20 μM
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Incubation Time:24 h
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Result:Significantly inhibited the production of TNF-α, IL-6, and IL-1β compared to the LPS-induced group at all tested concentrations.
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Cell Line:IL-1β-stimulated HaCaT cells
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Concentration:5, 10, or 20 μM
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Incubation Time:24 h
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Result:Significantly inhibited the production of IL-17A and IL-22 compared to the IL-1β-induced group at all tested concentrations.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c mice (male, 6-8 weeks, 20 g), topically administered with 62.5 mg Imiquimod (HY-B0180) on the dorsal skin once daily for 5 days)[1]
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Dosage:25 mg/kg, 50 mg/kg, 100 mg/kg
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Administration:Topical application (topical); once daily; 5 days (starting simultaneously with IMQ application)
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Result:Significantly ameliorated psoriasis-like skin lesions, including reduced erythema, scales, and skin thickness.
Decreased PASI scores compared with the model group.
Reduced the spleen index in a dose-dependent manner, with medium-dose (50 mg/kg) and high-dose (100 mg/kg) groups approaching normal levels.
H&E staining revealed that epidermal hyperplasia and parakeratosis were effectively ameliorated, with the high-dose group showing the most significant improvement.
Immunofluorescence staining showed that Ki67 and PCNA expression levels in dorsal skin were markedly reduced.
Significantly decreased the levels of IL-17A, IL-23, IL-1β, and IFN-γ in both skin lesions and serum.
Western blot analysis demonstrated that PI3K, AKT, and JAK2 protein expressions in dorsal skin were downregulated.
Chemical Information
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Molecular Weight 497.28
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Formula C25H14Cl2O7
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SMILES
O=C1OC2=CC=CC=C2C(O)=C1C(C3=C(C4=C(OC3=O)C=CC=C4)O)C5=CC(Cl)=CC(Cl)=C5O
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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)
PI3K/AKT/JAK2-IN-1 Related Classifications
HY-184385 Related Classifications
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- PI3K/AKT/JAK2-IN-1
- PI3K
- Akt
- JAK
- TNF Receptor
- Interleukin Related
- PI3K/AKT/JAK2 signaling pathway
- PI3K inhibitor
- AKT inhibitor
- JAK2 inhibitor
- anti-inflammation
- anti-psoriasis
- psoriasis
- biscoumarin derivative
- RAW264.7
- HaCaT
- LPS
- IMQ-induced psoriasis mouse model
- IL-6
- TNF-α
- IL-1β
- IL-17A
- IL-22
- IL-23
- IFN-γ
- NO
- Ki67
- PCNA
- Inhibitor
- inhibitor
- inhibit