Zunsemetinib_product_DataBase

Bioactivity

Zunsemetinib (CDD-450) is an orally active and selective p38α mitogen-activated protein kinase-activated protein kinase 2 (MK2) pathway inhibitor. Zunsemetinib can be used for the research of immuno-inflammatory diseases[1].

Target

MK2

Invitro

Zunsemetinib (1 and 10 μM; 1 hour; WT and NOM ID BMMs) has no effect on NLRP3 expression, but decreases IL-1β expression by promoting IL-1β mRNA degradation[1].Zunsemetinib (0.4 nM~1 μM; 16 hours; PBMC) reduces IL-1β secretion and promotes IL-1β mRNA instability[1].Zunsemetinib selectively blocks p38α MAPK activation of the proinflammatory kinase MK2 while sparing p38α activation of other effectors such as PRAK and ATF2. Zunsemetinib inhibits in vitro osteoclast formation induced by RANKL[1]. RT-PCR[1] Cell Line:

In Vivo

Zunsemetinib (1,000 ppm; p.o.) blocks LPS-induced TNF-α expression persisted for up to 4 weeks after dosing[1].Zunsemetinib (10 and 20 mg/kg; p.o.) increases bone density[1].Zunsemetinib prevents osteopenia in NOM IDc mice through inhibition of osteoclastogenesis[1]. Animal Model:

Name

Zunsemetinib

CAS

1640282-42-3

Formula

C25H22ClF2N5O3

Molar Mass

513.92

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[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.

PeptideDB

Zunsemetinib

CAS: 1640282-42-3 F: C25H22ClF2N5O3 W: 513.92