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TOPK-p38/JNK-IN-1

Catalog No. T61440 CAS 2745108-35-2

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].

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TOPK-p38/JNK-IN-1, CAS 2745108-35-2

Pack Size	Availability	Price/USD
25 mg	6-8 weeks	$ 1,520.00
50 mg	6-8 weeks	$ 1,980.00
100 mg	6-8 weeks	$ 2,500.00

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Description	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].
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), administered orally at doses of 20-40 mg/kg to inbred 6-8-week-old female BALB/c mice once daily for a week, was found effective in mitigating psoriasis-like skin inflammation. This study used a model wherein skin inflammation was induced by applying 62.5 mg of IMQ cream on a specific shaved area of the mice's back. Treatment with Compound B12 led to a noticeable reduction in scales, thickness, and erythema characteristic of psoriasis-like conditions in mice. Histopathological examinations revealed significant alleviation of hyperkeratosis, acanthocyte proliferation, and inflammatory cell infiltration. Furthermore, the compound dose-dependently inhibited the expression of psoriasis-related proteins (p-STAT3, p-TOPK, TOPK, p-p38, p-JNKs, PCNA, p-H2AX) in the skin tissues of the mice.

Molecular Weight	368.31
Formula	C17H15F3N2O4
CAS No.	2745108-35-2

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

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TOPK-p38/JNK-IN-1 2745108-35-2 inhibitor inhibit

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