Description
YS-121 is a dual inhibitor of Microsomal prostaglandin E2 synthase-1 (mPGES-1) . Cyclooxygenases (COX-1 and COX-2) have been involved in catalyzing the formation of prostaglandins and related eicosanoids and play an essential role in the pathogenesis of breast cancer. Actions of COX-2 are mediated by prostaglandin E2 (PGE2). Microsomal PGES-1 (mPGES-1), the inducible form of PGES, has a marked affinity for coupling with COX-2. Expression of mPGES-1 has been observed in inflammatory conditions and cancers of the stomach, colon, lung, endometrium, and skin . YS-121 inhibited the activity of mPGES-1 with an IC50 of 3.9 μM . YS-121 also inhibited the activity of 5-LO with the IC50 of 4.1 μM . YS-121 effectively inhibited PGE2 and LT synthesis in both cell free and intact cell assays. Intraperitoneal administration of YS-121 (1.5 mg/kg) reduced pleural levels of PGE2 and LTB4 while blocking exudate formation and leukocyte infiltration in carrageenan-induced rat pleurisy . YS-121 (10 μM) showed minor effects on COX-1 and COX-2, inhibiting these enzymes 24.8% and 38%, respectively .
Product information
CAS Number: 916482-17-2
Molecular Weight: 407.96
Formula: C20H26ClN3O2S
Chemical Name: 2-({4-chloro-6-[(2,3-dimethylphenyl)amino]pyrimidin-2-yl}sulfanyl)octanoic acid
Smiles: CCCCCCC(SC1N=C(Cl)C=C(NC2C=CC=C(C)C=2C)N=1)C(O)=O
InChiKey: HVJBWTVMRIOTEL-UHFFFAOYSA-N
InChi: InChI=1S/C20H26ClN3O2S/c1-4-5-6-7-11-16(19(25)26)27-20-23-17(21)12-18(24-20)22-15-10-8-9-13(2)14(15)3/h8-10,12,16H,4-7,11H2,1-3H3,(H,25,26)(H,22,23,24)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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