化合物 TOPK-p38/JNK-IN-1 T61440

Product Introduction
Bioactivity


英文名: TOPK-p38/JNK-IN-1

描述: TOPK-p38/JNK-IN-1 (Compound B12) is an orally active inhibitor of the TOPK-p38/JNK signaling pathway, with an IC50 value of 2.14 μM for the inhibition of NO production. It demonstrates anti-inflammatory properties by inhibiting downstream phosphorylation of related proteins and preventing the degradation of TOPK [1].

体外活性: 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]. 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.

体内活性: 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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途