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YS121

CAT: 0804-HY-111140-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-111140-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
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].
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.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C (Powder, protect from light)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
5-LOX; PPARα; PPARγ

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CatalogName
sc-296707YS121

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