YS121

YS121 is a dual inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1; IC50 = 3.4 μM) and 5-lipoxygenase (5-LOX; IC50 = 6.5 μM) . YS121 exhibits direct, reversible, and specific binding to mPGES-1 (KD = 10-14 μM) [1]. YS121 dose-dependently reduces PGE2 production with an EC50 of 12 μM in IL-1β-stimulated A549 cells[2]. YS121 (compound 9) activates PPAR-α and -γ (EC50 = 1 and 3.6 μM, respectively) [3]. YS121 exhibits anti-inflammatory efficiency in human whole blood as well as in vivo. YS121 can be used for pleurisy research[1].

Product Specifications

CAS Number

[916482-17-2]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Lipoxygenase; PGE synthase; PPAR

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Immunology/Inflammation; Metabolic Enzyme/Protease; Vitamin D Related/Nuclear Receptor

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/ys121.html

Purity

99.74

Solubility

DMSO : 125 mg/mL (ultrasonic)

Smiles

CCCCCCC(SC1=NC(NC2=CC=CC(C)=C2C)=CC(Cl)=N1)C(O)=O

Molecular Formula

C20H26ClN3O2S

Molecular Weight

407.96

Precautions

H302, H315, H319, H335

References & Citations

[1]Koeberle A, et al. The molecular pharmacology and in vivo activity of 2- (4-chloro-6- (2,3-dimethylphenylamino) pyrimidin-2-ylthio) octanoic acid (YS121), a dual inhibitor of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase. J Pharmacol Exp Ther. 2010 Mar;332 (3) :840-8.|[2]Chang HH, et al. Identification and development of mPGES-1 inhibitors: where we are at? Future Med Chem. 2011 Nov;3 (15) :1909-34.|[3]Rau O, et al. Alpha-alkyl substituted pirinixic acid derivatives as potent dual agonists of the peroxisome proliferator activated receptor alpha and gamma. Arch Pharm (Weinheim) . 2008 Mar;341 (3) :191-5.