上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。
TOPK-p38/JNK-IN-1
TOPK-p38/JNK-IN-1 (Compound B12) 是具有口服活性的 TOPK-p38/JNK 抑制剂，具有抗炎活性，对NO产生的 IC50 为2.14 µM。TOPK-p38/JNK-IN-1 抑制下游相关蛋白磷酸化，避免 TOPK 的降解。
TOPK-p38/JNK-IN-1 Chemical Structure
CAS No. : 2745108-35-2
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
| 生物活性 |
TOPK-p38/JNK-IN-1 (Compound B12) is an orally active TOPK-p38/JNK signaling pathway inhibitor with the IC50 value of 2.14 µM for NO production. TOPK-p38/JNK-IN-1 shows anti-inflammatory activities. TOPK-p38/JNK-IN-1 also inhibits phosphorylate downstream related proteins and avoids degradation of TOPK[1].
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| IC50 & Target[1] |
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JNK
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NO Production
2.14 μM (IC50)
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体外研究
(In Vitro) |
TOPK-p38/JNK-IN-1 (Compound B12) (10 µM, 1 h) inhibits the NO production in RAW264.7 cells[1]
. TOPK-p38/JNK-IN-1 (Compound B12) (0-100 µM, 24 h for RAW264.7 cells; 0-50µM, 6h for HaCaT cells) inhibits cell proliferation in a dose-dependent manner[1]
. TOPK-p38/JNK-IN-1 (Compound B12) (0-10 µM, 1h for RAW264.7 cells; 6 h for HaCaT cells) suppresses LPS-induced TOPK/NF-jB/p38/JNK activation[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[1]
| Cell Line: |
RAW264.7 cell lines |
| Concentration: |
4 µM, 20 µM and 100µM |
| Incubation Time: |
24 h |
| Result: |
Inhibited cell proliferation in a dose-dependent manner. |
Cell Proliferation Assay[1]
| Cell Line: |
HaCaT cell line. |
| Concentration: |
0.78 µM, 1.56 µM, 3.125µM, 6.25 µM, 12.5 µM, 25 µM and 50 µM. |
| Incubation Time: |
Pre-treated with compound B12 for 6 h, incubated with LPS (100 g/mL) for 24 h |
| Result: |
Inhibited excessive proliferation of LPS-induced HaCaT cells in a dose-dependent manner. |
Western Blot Analysis[1]
| Cell Line: |
RAW264.7 and HaCaT cell line. |
| Concentration: |
2.5 µM, 5 µM and 10µM. |
| Incubation Time: |
Pre-treated for 1 h, co-treated with LPS (0.5 µg/mL) for 0.5 h or 24 h and pre-treated for 6 h before SUV irradiation respectively. |
| Result: |
Inhibited the expression of iNOS and COX-2 in a dose-dependent manner, affected the phosphorylation of TOPK and inhibited P38/JNK protein phosphorylation and NF-κB p65 translocated into the nucleus. |
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体内研究
(In Vivo) |
TOPK-p38/JNK-IN-1 (Compound B12) (Inbred 6–8-week-old female BALB/c mice; 20-40 mg/kg; IG, once a day, each group for 7 days) could improve psoriasis-like skin inflammation[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: |
Inbred 6–8-week-old female BALB/c mice[1]. |
| Dosage: |
20 mg/kg, 40 mg/kg |
| Administration: |
IG, once a day, each group for 7 days. Induce skin inflammation by topically applying 62.5 mg of IMQ cream on the shaved 2 cm × 3 cm back skins. |
| Result: |
Successfully reduced the scales, thickness and erythema in psoriasis-like mice, histopathologically alleviated hyperkeratosis, acanthocyte proliferation and inflammatory cell infiltration. Inhibited the expression of related proteins (p-STAT3, p-TOPK, TOPK, p-p38, p-JNKs, PCNA, p-H2AX) in mouse skin tissues in a dose-dependent manner. |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[1]. Jing Wu, et al. Discovery of novel paeonol-based derivatives against skin inflammation in vitro and in vivo. Journal of Enzyme Inhibition and Medicinal Chemistry, 37:1, 817-831.
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