2745108-35-2
2745108-35-2 structure
- Name: TOPK-p38/JNK-IN-1
- Chemical Name: TOPK-p38/JNK-IN-1
- CAS Number: 2745108-35-2
- Molecular Formula: C17H15F3N2O4
- Molecular Weight: 368.31
- Catalog: Signaling Pathways MAPK/ERK Pathway JNK
- Create Date: 2022-05-21 12:57:22
- Modify Date: 2024-01-11 17:01:17
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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].
| Name | TOPK-p38/JNK-IN-1 |
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| Description | 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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| Related Catalog | |
| Target |
JNK NO Production:2.14 μM (IC50) |
| 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]. 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. |
| 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. |
| References |
| Molecular Formula | C17H15F3N2O4 |
|---|---|
| Molecular Weight | 368.31 |