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编 号：F755201
分子式：C17H15F3N2O4
分子量：368.31
分子式：C17H15F3N2O4
分子量：368.31
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CAS No: 2745108-35-2
产品详情
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.
体内研究：
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.Animal Model:Inbred 6–8-week-old female BALB/c mice.
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.
体外研究：
TOPK-p38/JNK-IN-1 (Compound B12) (10 μM, 1 h) inhibits the NO production in RAW264.7 cells.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.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.
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.
体内研究：
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.Animal Model:Inbred 6–8-week-old female BALB/c mice.
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.
体外研究：
TOPK-p38/JNK-IN-1 (Compound B12) (10 μM, 1 h) inhibits the NO production in RAW264.7 cells.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.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.
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