JAK2/STAT3-IN-2
JAK2/STAT3-IN-2 is an orally active JAK2/STAT3 inhibitor. JAK2/STAT3-IN-2 inhibits the phosphorylation of tyrosine residues in JAK2 and STAT3, blocks downstream signal transduction, disrupts the dimerization and nuclear translocation of STAT3, and suppresses pro-inflammatory transcriptional activity. JAK2/STAT3-IN-2 inhibits the expression of IL-17A and IL-17F, reduces immune cell infiltration, and inhibits the production of NO simultaneously. JAK2/STAT3-IN-2 exerts a protective effect in a mouse model of ulcerative colitis induced by DSS (HY-116282C). JAK2/STAT3-IN-2 can be used for the research of ulcerative colitis.
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- Fòrmula: C33H41BrN4O5S
- Peso molecular:685.67
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Almacenamiento:
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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Actividad biológica
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Chemical Information
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
[1]|
JAK2 |
STAT3 |
IL-17A |
IL-17F |
In Vitro
JAK2/STAT3-IN-2 (Compound 4c) (20 μM; 24 h) potently inhibits LPS (HY-D1056)-induced NO production in RAW264.7 macrophages with an IC50 of 3.56 μM, while exhibiting only extremely weak cytotoxicity at a concentration of 20 μM[1].
JAK2/STAT3-IN-2 (2-8 μM; 24 h) significantly downregulates the expression of TNF-α and IL-6 in LPS-induced RAW264.7 macrophages[1].
JAK2/STAT3-IN-2 (4-8 μM) inhibits the mRNA expression of IL-17A, IL-17F, JAK2 and STAT3 in LPS-induced RAW264.7 macrophages, indicating that it exerts anti-inflammatory effects mainly by inhibiting the JAK2-STAT3 pathway[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 macrophages
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Concentration:2, 4, 8 μM
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Incubation Time:24 h (incubation with LPS)
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Result:Significantly downregulated LPS-induced TNF-α and IL-6 expression.
Exhibited superior activity compared to dexamethasone at 4 μM and 8 μM.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (6-week-old male, 20 g)[1]
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Dosage:12.5-50 mg/kg
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Administration:i.g.; once daily; 9 days
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Result:Significantly alleviated DSS-induced body weight loss.
Reduced Disease Activity Index (DAI) scores.
Preserved colon length compared to the DSS model group.
Attenuated bowel wall thickening, reduced inflammatory cell infiltration, and mitigated goblet cell loss compared to the DSS model group.
Upregulated colonic Occludin expression, with the 25 mg/kg dose producing the most significant increase.
Significantly upregulated colonic MUC2 expression at the 50 mg/kg dose.
Significantly downregulated colonic mRNA expression of IL-17A, IL-17F, MMP3, JAK2, and STAT3 compared to the DSS model group.
Exerted the strongest inhibitory effect on JAK2 and STAT3 mRNA expression at the 50 mg/kg dose, surpassing the positive control.
Reduced the relative expression of phosphorylated JAK2/JAK2 and phosphorylated STAT3/STAT3 compared to the DSS model group, with the 50 mg/kg dose showing the most potent inhibition of phosphorylated STAT3/STAT3.
- Western Blot
- RNA extraction experimental
- Multiplex immunofluorescence IHC
- Multiplex immunohistochemistry
- Research Protocol for Inflammation-related Diseases
- Research Protocol for Cancer Immunology
- How to Choose the Right Model Animal
- Kinase activity and phosphorylation assays
- Cytoplasmic-Nuclear Fractionated Protein Extraction
- Dual Luciferin reporter gene assay
- DSS-Induced Colitis
- TNBS-Induced Colitis
- Protocol for Kinase activity and phosphorylation assays
Chemical Information
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Peso molecular 685.67
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Fòrmula C33H41BrN4O5S
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SMILES
C/C1=C\C2OC([C@@H](C2CC/C(C)=C/CC1)CN(S(=O)(C3=CN=CC=C3)=O)CCNC(CCN4CCC5=C4C=C(C=C5)Br)=O)=O
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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)
JAK2/STAT3-IN-2 Related Classifications
HY-183370 Related Classifications
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