Thi-DPPY
Thi-DPPY (compound 8e) is a potent and orally active JAK3 inhibitor with IC50 values of 62.4, 1.38 nM for BTK, JAK, respectively. Thi-DPPY shows anti-proliferative activity against HBE cells. Thi-DPPY shows anti-inflammatory activity in vivo. Thi-DPPY has the potential for the research of idiopathic pulmonary fibrosis (IPF).
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- CAS 番号: 2307699-34-7
- 分子式: C28H28ClN5O4S
- 分子量:566.07
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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JAK3 1.38 nM (IC50) |
BTK 62.4 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| Sf9 | IC50 |
1.38 nM
Compound: 8e
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Inhibition of recombinant human N-terminal GST-tagged JAK3 (781 to end residues) expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate incubated for 60 mins in presence of ATP by ADP-Glo kinase assay
Inhibition of recombinant human N-terminal GST-tagged JAK3 (781 to end residues) expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate incubated for 60 mins in presence of ATP by ADP-Glo kinase assay
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[PMID: 31866272] |
DPPY (compound 8e) shows anti-proliferative activity against HBE (human bronchial epithelia) cells with an IC50 of 39.0 µM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
DPPY (30, 60 mg/kg) significantly decreases the expression of IL-6, IL-17A, TNF-α and MDA in lung tissue in a dose dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:5-6 week old, 20-25 g, C57BL mice (BLM-induced pulmonary inflammation and pulmonary fibrosis model)[1]
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Dosage:30, 60 mg/kg
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Administration:I.g.; once daily for 14 days
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Result:Attenuated the pulmonary morphology changes and reduced the collagen disposition induced by BLM in mouse lung.
化学情報
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CAS 番号 2307699-34-7
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分子量 566.07
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分子式 C28H28ClN5O4S
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SMILES
C=CC(NC1=CC(OC2=NC(NC3=CC(Cl)=C(C=C3)OCCCN4CCOCC4)=NC5=C2SC=C5)=CC=C1)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Thi-DPPY 関連分類
HY-147742 関連分類
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