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 (Compound B12) is an orally active TOPK-p38/JNK signaling pathway inhibitor with the IC 50 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].

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.

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.

2745108-35-2

C17H15F3N2O4

368.31

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years