2. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling Immunology/Inflammation
  3. JAK STAT Interleukin Related
  4. 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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JAK2/STAT3-IN-2

JAK2/STAT3-IN-2 Chemical Structure

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JAK2/STAT3-IN-2 Related Antibodies

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Description

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[1].

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.

JAK2/STAT3-IN-2 Related Antibodies

ELISA Assay[1]

Cell Line: RAW264.7 macrophages
Concentration: 2, 4, 8 μM
Incubation Time: 24 h (incubation with LPS)
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

JAK2/STAT3-IN-2 (Compound 4c) (12.5-50 mg/kg; i.g.; once daily; 9 days) exerts dose-dependent protective effects against DSS-induced ulcerative colitis in male C57BL/6J mice, with the 50 mg/kg dose showing the strongest suppression of the IL-17A/IL-17F-JAK2-STAT3 signaling pathway[1].

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

Animal Model: C57BL/6J (6-week-old male, 20 g)[1]
Dosage: 12.5-50 mg/kg
Administration: i.g.; once daily; 9 days
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.
Molecular Weight

685.67

Formula

C33H41BrN4O5S
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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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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JAK2/STAT3-IN-2 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:

JAK2/STAT3-IN-2JAKSTATInterleukin RelatedJanus kinaseILRAW264.7 macrophagesIL-17FJAK2H9C2 rat cardiomyocytesCaco-2 intestinal epithelial cellsDSS-induced ulcerative colitis mice modelsHepG2 cellsIL-17AJAK2/STAT3 pathwaySTAT3Inhibitorinhibitorinhibit

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