880546-17-8
Chemical Structure
K-14585
- CAS No.: 880546-17-8
- Formula:C51H56Cl2N8O4
- Molecular Weight:915.95
IUPAC Name: (S)-6-amino-N-((S)-1-(benzhydrylamino)-1-oxo-3-phenylpropan-2-yl)-2-(2-(3-(1-(2,6-dichlorobenzyl)-3-(pyrrolidin-1-ylmethyl)-1H-indol-5-yl)ureido)acetamido)hexanamide
InChIKey: ADEQJSQZZXWZPW-GSVOJQHPSA-N
SMILES: ClC(C=CC=C1Cl)=C1CN2C(C(C(CN3CCCC3)=C2)=C4)=CC=C4NC(NCC(N[C@@H](CCCCN)C(N[C@@H](CC5=CC=CC=C5)C(NC(C6=CC=CC=C6)C7=CC=CC=C7)=O)=O)=O)=O
Biological Activity: K-14585 is a peptide competitive PAR2 antagonist. K-14585 inhibits PAR2-dependent IL-8 production, NF-κB phosphorylation, and p38 signaling. K-14585 reduces SLIGKV (PAR2 agonist peptide)-induced Ca2+ mobilisation in primary human keratinocytes[1][2][3].
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K-14585 | K-14585 is a peptide competitive PAR2 antagonist. K-14585 inhibits PAR2-dependent IL-8 production, NF-κB phosphorylation, and p38 signaling. K-14585 reduces SLIGKV (PAR2 agonist peptide)-induced Ca2+ mobilisation in primary human keratinocytes. | |||||||||||||||||||||
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- [1]. Goh FG, et al. Dual effect of the novel peptide antagonist K-14585 on proteinase-activated receptor-2-mediated signalling. Br J Pharmacol. 2009 Dec;158(7):1695-704. [Content Brief]
- [2]. Kanke T, et al. Novel antagonists for proteinase-activated receptor 2: inhibition of cellular and vascular responses in vitro and in vivo. Br J Pharmacol. 2009 Sep;158(1):361-71. [Content Brief]
- [3]. Sevigny LM, et al. Interdicting protease-activated receptor-2-driven inflammation with cell-penetrating pepducins. Proc Natl Acad Sci U S A. 2011 May 17;108(20):8491-6. [Content Brief]
Keywords
