WYJ-2
WYJ-2 is a selective agonist for toll-like receptor 2/1 (TLR2/1) with EC50 of 18.57 nM in human TLR2 and TLR1 transient-cotransfected HEK 293T cells. WYJ-2 induces pyroptosis and exhibits anticancer activity against non-small cell lung cancer (NSCLC).
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- CAS 番号: 3029403-05-9
- 分子式: C17H9F2N3O4
- 分子量:357.27
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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TLR2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | CC50 |
>100 μM
Compound: 2 WYJ-2
|
Cytotoxicity against human HEK293T cells incubated for 24 hrs by CCK-8 reagent based colorimetric assay
Cytotoxicity against human HEK293T cells incubated for 24 hrs by CCK-8 reagent based colorimetric assay
|
[PMID: 38498304] |
| RAW264.7 | CC50 |
>100 μM
Compound: 2 WYJ-2
|
Cytotoxicity against mouse RAW264.7 cells incubated for 24 hrs by CCK-8 reagent based colorimetric assay
Cytotoxicity against mouse RAW264.7 cells incubated for 24 hrs by CCK-8 reagent based colorimetric assay
|
[PMID: 38498304] |
| THP-1 | CC50 |
>100 μM
Compound: 2 WYJ-2
|
Cytotoxicity against human THP-1 cells incubated for 24 hrs by CCK-8 reagent based colorimetric assay
Cytotoxicity against human THP-1 cells incubated for 24 hrs by CCK-8 reagent based colorimetric assay
|
[PMID: 38498304] |
| THP-1 | CC50 |
>100 μM
Compound: 2 WYJ-2
|
Cytotoxicity against PMA differentiated human THP-1 cells incubated for 24 hrs by CCK-8 reagent based colorimetric assay
Cytotoxicity against PMA differentiated human THP-1 cells incubated for 24 hrs by CCK-8 reagent based colorimetric assay
|
[PMID: 38498304] |
WYJ-2 (0-10 μM) inhibits heterodimerization of TLR2 and TLR1 in THP-1 cells, stimulates the adaptor protein myeloid differentiation primary response protein 88 (MyD88) and then activates the NF-κB signaling pathway without significant cytotoxicity[1].
WYJ-2 (0-100 μM) inhibits proliferation in cancer cells A549, HeLa, HepG2 and MCF-7 with IC50 about 10 μM, induces cancer cell pyroptosis by activation of the NLRP3 inflammasome[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PAM-differentiated THP-1
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Concentration:0-10 μM
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Incubation Time:12 h
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Result:Upregulated levels of MyD88, p-p65, TLR1 and TLR2.
Increased NLRP3.
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Cell Line:PAM-differentiated THP-1
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Concentration:0-10 μM
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Incubation Time:12 h
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Result:Induced translocation of p-p65 in nucleus.
WYJ-2 (10 mg/kg, i.p.) exhibits a pharmacokinetic profil with half-time of T1/2 of 3.67 h and a clearance Cmax of 497 ± 49 ng/mL[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:A549 xenograft BALB/c mice[1]
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Dosage:5 mg/kg
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Administration:i.p. every two days for 30 days
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Result:Inhibited tumor growth with a TGI of 72.22% without significant loss of body weight.
化学情報
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CAS 番号 3029403-05-9
-
分子量 357.27
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分子式 C17H9F2N3O4
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SMILES
FC1=CC=C(C=C1C2=NC(C3=CC4=CC(F)=CC=C4OC3)=NO2)[N+]([O-])=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)