1. MAPK/ERK Pathway
  2. JNK
  3. TOPK-p38/JNK-IN-1

TOPK-p38/JNK-IN-1 

Cat. No.: HY-144761
Handling Instructions

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.

For research use only. We do not sell to patients.

TOPK-p38/JNK-IN-1 Chemical Structure

TOPK-p38/JNK-IN-1 Chemical Structure

CAS No. : 2745108-35-2

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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].

IC50 & Target[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

368.31

Formula

C17H15F3N2O4

CAS No.
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Storage

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TOPK-p38/JNK-IN-1
Cat. No.:
HY-144761
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