1. Cell Cycle/DNA Damage
  2. PPAR

GSK0660 

Cat. No.: HY-12377 Purity: 99.27%
Handling Instructions

GSK0660 is a potent antagonist of PPARβ and PPARδ, with IC50s of both 155 nM, and is nearly inactive on PPARα and PPARγ with IC50s of both >10 μM.

For research use only. We do not sell to patients.

GSK0660 Chemical Structure

GSK0660 Chemical Structure

CAS No. : 1014691-61-2

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 79 In-stock
Estimated Time of Arrival: December 31
5 mg USD 72 In-stock
Estimated Time of Arrival: December 31
10 mg USD 119 In-stock
Estimated Time of Arrival: December 31
50 mg USD 468 In-stock
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100 mg USD 840 In-stock
Estimated Time of Arrival: December 31
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

GSK0660 is a potent antagonist of PPARβ and PPARδ, with IC50s of both 155 nM, and is nearly inactive on PPARα and PPARγ with IC50s of both >10 μM.

IC50 & Target[1]

PPARβ/δ

155 nM (IC50)

In Vitro

GSK0660 is a potent antagonist of PPARβ and PPARδ, with IC50s of both 155 nM, and is nearly inactive on PPARα and PPARγ with IC50s of both >10 μM. GSK0660 antagonizes 100% of the activity of PPARβ/δ with a pIC50 of 6.8. GSK0660 (100 nM) reduces CPT1a (a PPARβ/δ target gene) expression below the basal vehicle-treated level by approximately 50%, but shows no effect on PDK4 expression, which is also a PPARβ/δ target gene in skeletal muscle cells[1]. GSK0660 (0.5 μM) reduces the levels of AMPK and eNOS phosphorylation, and BMP-2, Runx-2 mRNA expression in MC3T3-E1 cells. GSK0660 (0.1 and 0.5 μM) reverses the bezafibrate-induced enchancement of ALP activity on d 7 in MC3T3-E1 cells[2]. GSK0660 (1 μM) markedly blocks GW501516-mediated attenuation of glutamate release, and the effect of GW501516 on ROS generation in BV-2 cells stimulated with LPS. Furthermore, GSK0660 significantly reduces inhibitory effect of GW501516 on the LPS-induced expression of gp91phox mRNA in BV-2 cells[3].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 49 mg/mL (117.09 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3895 mL 11.9477 mL 23.8954 mL
5 mM 0.4779 mL 2.3895 mL 4.7791 mL
10 mM 0.2390 mL 1.1948 mL 2.3895 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[2]

Cell viability is determined by the MTT dye. MC3T3-E1 cells are incubated with bezafibrate (1−1000 μM) for 24, 48, or 72 h, and are pretreated with the AMPK inhibitor compound C (5 μM), PPARβ inhibitor GSK0660 (0.5 μM), PPARα inhibitor MK886 (10 μM), or NOS inhibitor L-NAME (1000 μM) followed by bezafibrate (100 μM) incubation for 48 h. After the incubations, 10 μL of MTT is added to each well of a 96-well microplate, and the microplates are placed in an incubator at 37°C for 4 h. One hundred fifty microliters of DMSO is added to all wells and mixed thoroughly to lyse the cells and dissolve the dark blue crystals. After 10 min, the absorbance is measured at 570 nm using a microplate reader[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

418.49

Formula

C₁₉H₁₈N₂O₅S₂

CAS No.

1014691-61-2

SMILES

O=C(C1=C(S(=O)(NC2=CC=C(NC3=CC=CC=C3)C=C2OC)=O)C=CS1)OC

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
GSK0660
Cat. No.:
HY-12377
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GSK0660

Cat. No.: HY-12377