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Zunsemetinib

Catalog No. T39126 CAS 1640282-42-3

Synonyms: CDD-450, ATI-450

Zunsemetinib (CDD-450) is a potent and specific inhibitor of the p38α-MK2 pathway, exerting its effects through oral administration. It has proven activity against immuno-inflammatory diseases, making it a valuable tool for research in this area.

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Zunsemetinib, CAS 1640282-42-3

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5 mg	Inquiry	$ 697.00
10 mg	Inquiry	$ 1,190.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	Zunsemetinib (CDD-450) is a potent and specific inhibitor of the p38α-MK2 pathway, exerting its effects through oral administration. It has proven activity against immuno-inflammatory diseases, making it a valuable tool for research in this area.
In vitro	Zunsemetinib, at concentrations of 1 and 10 μM for 1 hour in WT and NOM ID BMMs, does not alter NLRP3 expression but effectively lowers IL-1β expression by facilitating the degradation of IL-1β mRNA. Similarly, when applied over 16 hours in PBMCs at doses ranging from 0.4 nM to 1 μM, it diminishes IL-1β secretion and induces IL-1β mRNA instability. The compound uniquely inhibits the p38α MAPK pathway's activation of MK2, a proinflammatory kinase, without affecting the activation of other pathways such as PRAK and ATF2. Additionally, Zunsemetinib prevents the formation of osteoclasts in vitro, a process triggered by RANKL. This demonstrates its role in not just modulating specific gene expressions but also its potential in affecting cellular inflammatory responses and osteoclastogenesis.
In vivo	Zunsemetinib, administered orally at 1,000 ppm, effectively inhibits LPS-induced TNF-α expression for up to four weeks post-dosing, as demonstrated in 8-week-old WT female mice[1]. At dosages of 10 and 20 mg/kg, this compound also significantly enhances bone density in rats, indicating a potential therapeutic application in bone health[1]. Furthermore, Zunsemetinib prevents osteopenia in NOM ID c mice by inhibiting osteoclastogenesis, showcasing its multifaceted role in bone metabolism regulation[1].

Synonyms	CDD-450, ATI-450
Molecular Weight	513.93
Formula	C25H22ClF2N5O3
CAS No.	1640282-42-3

Storage

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

References and Literature

1. Zunsemetinib (ATI-450) – Investigational oral MK2 pathway inhibitor 2. Aclaris Therapeutics Announces ATI-450 (MK2 pathway Inhibitor) publication in Journal of Experimental Medicine 3. Wang C, et al. Selective inhibition of the p38α MAPK-MK2 axis inhibits inflammatory cues including inflammasome priming signals. J Exp Med. 2018;215(5):1315-1325.

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Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Zunsemetinib 1640282-42-3 CDD 450 ATI450 CDD450 CDD-450 ATI-450 ATI 450 inhibitor inhibit

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