YS-121
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
YS-121 is a dual inhibitor of Microsomal prostaglandin E2 synthase-1 (mPGES-1) [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 [2].
YS-121 inhibited the activity of mPGES-1 with an IC50 of 3.9 μM [1]. YS-121 also inhibited the activity of 5-LO with the IC50 of 4.1 μM [3]. 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 [4]. YS-121 (10 μM) showed minor effects on COX-1 and COX-2, inhibiting these enzymes 24.8% and 38%, respectively [1].
References:
[1] Koeberle A, Zettl H, Greiner C, et al. Pirinixic acid derivatives as novel dual inhibitors of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase[J]. Journal of medicinal chemistry, 2008, 51(24): 8068-8076.
[2] Mehrotra S, Morimiya A, Agarwal B, et al. Microsomal prostaglandin E2 synthase‐1 in breast cancer: a potential target for therapy[J]. The Journal of pathology, 2006, 208(3): 356-363.
Werz O, Greiner C, Koeberle A, et al. Novel and potent inhibitors of 5-lipoxygenase product synthesis based on the structure of pirinixic acid[J]. Journal of medicinal chemistry, 2008, 51(17): 5449-5453.
Koeberle A, Rossi A, Zettl H, 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]. Journal of Pharmacology and Experimental Therapeutics, 2010, 332(3): 840-848.
| Physical Appearance | A solution in methyl acetate. To change the solvent, simply evaporate the acetate containing under a gentle stream of nitrogen and immediately add the solvent of choice. |
| Storage | Store at -20°C |
| M.Wt | 408 |
| Cas No. | 916482-17-2 |
| Formula | C20H26ClN3O2S |
| Solubility | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide |
| Chemical Name | 2-[[4-chloro-6-[(2,3-dimethylphenyl)amino]-2-pyrimidinyl]thio]-octanoic acid |
| SDF | Download SDF |
| Canonical SMILES | CC1=C(NC2=CC(Cl)=NC(SC(C(O)=O)CCCCCC)=N2)C=CC=C1C |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
