1. Immunology/Inflammation Metabolic Enzyme/Protease
  2. PGE synthase Lipoxygenase
  3. 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 dose- dependently reduces PGE2 production with EC50=12 μM in IL-1β-stimulated A549 cells.

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YS121 Chemical Structure

YS121 Chemical Structure

CAS No. : 916482-17-2

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5 mg USD 240 In-stock
10 mg USD 420 In-stock
25 mg USD 900 In-stock
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Based on 1 publication(s) in Google Scholar

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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 dose- dependently reduces PGE2 production with EC50=12 μM in IL-1β-stimulated A549 cells[1].

Cellular Effect
Cell Line Type Value Description References
A549 IC50
12 μM
Compound: 2d
Inhibition of mPGES1 in human A549 cells assessed as inhibition of IL-1-beta-induced PGE2 formation by cell-intact assay
Inhibition of mPGES1 in human A549 cells assessed as inhibition of IL-1-beta-induced PGE2 formation by cell-intact assay
[PMID: 19053751]
A549 IC50
3.9 μM
Compound: 2d
Inhibition of PGES1 in human A549 cell microsome assessed as PGE2 formation by cell-free assay
Inhibition of PGES1 in human A549 cell microsome assessed as PGE2 formation by cell-free assay
[PMID: 19053751]
COS-7 EC50
1 μM
Compound: 3
Agonist activity at wild-type human PPARalpha LBD expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay
Agonist activity at wild-type human PPARalpha LBD expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay
[PMID: 25022880]
COS-7 IC50
1 μM
Compound: 2
Activation of human PPARalpha ligand binding domain expressed in COS7 cells by luciferase reporter gene assay
Activation of human PPARalpha ligand binding domain expressed in COS7 cells by luciferase reporter gene assay
[PMID: 25037914]
COS-7 EC50
3.6 μM
Compound: 3
Agonist activity at human PPARgamma LBD expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay
Agonist activity at human PPARgamma LBD expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay
[PMID: 25022880]
COS-7 EC50
3.6 μM
Compound: 2
Transactivation of human PPARgamma LBD expressed in african green monkey Cos7 cells co-transfected with fused GAL4-DBD after 14 hrs by Dual-Glo Luciferase reporter gene assay
Transactivation of human PPARgamma LBD expressed in african green monkey Cos7 cells co-transfected with fused GAL4-DBD after 14 hrs by Dual-Glo Luciferase reporter gene assay
[PMID: 20307981]
COS-7 IC50
3.6 μM
Compound: 2
Activation of human PPARgamma ligand binding domain expressed in COS7 cells by luciferase reporter gene assay
Activation of human PPARgamma ligand binding domain expressed in COS7 cells by luciferase reporter gene assay
[PMID: 25037914]
Molecular Weight

407.96

Formula

C20H26ClN3O2S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (306.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4512 mL 12.2561 mL 24.5122 mL
5 mM 0.4902 mL 2.4512 mL 4.9024 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4512 mL 12.2561 mL 24.5122 mL 61.2805 mL
5 mM 0.4902 mL 2.4512 mL 4.9024 mL 12.2561 mL
10 mM 0.2451 mL 1.2256 mL 2.4512 mL 6.1281 mL
15 mM 0.1634 mL 0.8171 mL 1.6341 mL 4.0854 mL
20 mM 0.1226 mL 0.6128 mL 1.2256 mL 3.0640 mL
25 mM 0.0980 mL 0.4902 mL 0.9805 mL 2.4512 mL
30 mM 0.0817 mL 0.4085 mL 0.8171 mL 2.0427 mL
40 mM 0.0613 mL 0.3064 mL 0.6128 mL 1.5320 mL
50 mM 0.0490 mL 0.2451 mL 0.4902 mL 1.2256 mL
60 mM 0.0409 mL 0.2043 mL 0.4085 mL 1.0213 mL
80 mM 0.0306 mL 0.1532 mL 0.3064 mL 0.7660 mL
100 mM 0.0245 mL 0.1226 mL 0.2451 mL 0.6128 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
YS121
Cat. No.:
HY-111140
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