2. PI3K/Akt/mTOR Protein Tyrosine Kinase/RTK JAK/STAT Signaling Epigenetics Stem Cell/Wnt Apoptosis Immunology/Inflammation
  3. PI3K Akt JAK TNF Receptor Interleukin Related
  4. 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.

PI3K/AKT/JAK2-IN-1

PI3K/AKT/JAK2-IN-1 Chemical Structure

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PI3K/AKT/JAK2-IN-1 Related Antibodies

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JAK1 JAK2 JAK3 Tyk2 JAK

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

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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

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Description

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[1].

IC50 & Target

IL-6

 

IL-1β

 

IL-17A

 

IL-22

 

Cellular Effect
Cell Line Type Value Description References
RAW264.7 CC50
40 μM
Exhibits low cytotoxicity toward RAW264.7 cells for 24h.
Exhibits low cytotoxicity toward RAW264.7 cells for 24h.
42235429
In Vitro

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.

PI3K/AKT/JAK2-IN-1 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: RAW264.7 cells
Concentration: 5, 10, or 20 μM
Incubation Time: 24 h
Result: Exhibited low cytotoxicity toward RAW264.7 cells at all tested concentrations, with a CC50 > 40 μM.

Cell Viability Assay[1]

Cell Line: HaCaT cells
Concentration: 5, 10, or 20 μM
Incubation Time: 24 h
Result: Did not impair HaCaT cell viability at all tested concentrations.

ELISA Assay[1]

Cell Line: RAW264.7 cells
Concentration: 5, 10, or 20 μM
Incubation Time: 24 h
Result: Significantly inhibited the production of TNF-α, IL-6, and IL-1β compared to the LPS-induced group at all tested concentrations.

Cell Cytotoxicity Assay[1]

Cell Line: IL-1β-stimulated HaCaT cells
Concentration: 5, 10, or 20 μM
Incubation Time: 24 h
Result: Significantly inhibited the production of IL-17A and IL-22 compared to the IL-1β-induced group at all tested concentrations.
In Vivo

PI3K/AKT/JAK2-IN-1 (compound 15) (25-100 mg/kg; topical application; once daily; 5 days) significantly ameliorates Imiquimod (IMQ, HY-B0180)-induced psoriasis-like skin lesions in BALB/c mice, downregulates Ki67 and PCNA expression, decreases IL-17A, IL-23, IL-1β, and IFN-γ levels in skin lesions and serum, and impairs the PI3K/AKT/JAK2 signaling pathway in the affected skin[1].

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

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]
Dosage: 25 mg/kg, 50 mg/kg, 100 mg/kg
Administration: Topical application (topical); once daily; 5 days (starting simultaneously with IMQ application)
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.
Molecular Weight

497.28

Formula

C25H14Cl2O7
SMILES

O=C1OC2=CC=CC=C2C(O)=C1C(C3=C(C4=C(OC3=O)C=CC=C4)O)C5=CC(Cl)=CC(Cl)=C5O
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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PI3K/AKT/JAK2-IN-1 Related Classifications

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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:

PI3K/AKT/JAK2-IN-1PI3KAktJAKTNF ReceptorInterleukin RelatedPhosphoinositide 3-kinasePKBProtein kinase BJanus kinaseTumor Necrosis Factor ReceptorTNFRILPI3K/AKT/JAK2 signaling pathwayPI3K inhibitorAKT inhibitorJAK2 inhibitoranti-inflammationanti-psoriasispsoriasisbiscoumarin derivativeRAW264.7HaCaTLPSIMQ-induced psoriasis mouse modelIL-6TNF-αIL-1βIL-17AIL-22IL-23IFN-γNOKi67PCNAInhibitorinhibitorinhibit

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