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。
| 生物活性 | TOPK-p38/JNK-IN-1 (Compound B12) is an orally activeTOPK-p38/JNKsignaling pathway inhibitor with theIC50value 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 ofTOPK[1]. |
| IC50& Target[1] | JNK | 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]
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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]
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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].
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].
| 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. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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