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GW9662

Catalog No. T2260 CAS 22978-25-2

Synonyms: TIMTEC-BB SBB006523, GW 9662

GW9662 (TIMTEC-BB SBB006523) is a specific PPARγ antagonist (IC50: 3.3 nM, in a cell-free assay), with 100 to 1000-fold functional selectivity for PPARγ than PPARα/δ in cells.

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GW9662, CAS 22978-25-2

Pack Size	Availability	Price/USD
5 mg	In stock	$ 47.00
10 mg	In stock	$ 57.00
25 mg	In stock	$ 92.00
50 mg	In stock	$ 117.00
100 mg	In stock	$ 217.00
500 mg	In stock	$ 543.00
1 mL * 10 mM (in DMSO)	In stock	$ 52.00

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Purity: 99.94%

Purity: 99.74%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	GW9662 (TIMTEC-BB SBB006523) is a specific PPARγ antagonist (IC50: 3.3 nM, in a cell-free assay), with 100 to 1000-fold functional selectivity for PPARγ than PPARα/δ in cells.
Targets&IC50	PPARγ:3.3 nM
In vitro	Pretreatment with lipopolysaccharide (1 mg/kg, i.p.) significantly mitigates all characteristics of ischemia/reperfusion injury manifesting as renal damage and dysfunction in rats. However, this protective effect of lipopolysaccharide can be inhibited by GW9662 (1 mg/kg, i.p.).
In vivo	GW9662 inhibits the activation of PPARγ and suppresses the growth of human breast cancer cell lines (MCF7, MDA-MB-468, MDA-MB-231) with IC50 values of 20-30 μM. It binds to Cys(285) on PPARγ, a site conserved across the three types of PPAR. When used alongside Rosiglitazone (50 μM) for seven days in MDA-MB-231 cells, a statistically significant reduction in cell viability is observed. In primary mouse bone marrow and RAW264.7 cells, GW9662 (2 μM) can concentration-dependently reverse the inhibitory effects of PPARγ1 ligands on RANKL-induced osteoclastogenesis. Additionally, GW9662 (1 μM) inhibits RANKL-activated NF-κB in RAW264.7 cells, and at a concentration of 2 μM, it blocks the suppressive effect of IL-4 on osteoclastogenesis in BM cells. In primary preadipocytes from patients with thyroid eye disease, GW9662 (10 μM) inhibits hormone and agonist-induced adipocyte differentiation.
Kinase Assay	Binding assay: The human PPARα, PPARγ, and PPARδ ligand binding domains (LBDs) are expressed in E. coli as polyhistidine-tagged fusion proteins. Receptors are immobilized on SPA beads by addition of the desired receptor (15 nM) to a slurry of streptavidin-modifed SPA beads (0.5 mg/mL) in assay buffer. The mixture is allowed to equilibrate for at least 1 hour at room temperature, and the beads are pelleted by centrifugation at 1×103 g. The supernate is discarded, and the beads are resuspended in the original volume of fresh assay buffer with gentle mixing. The centrifugation/resuspension procedure is repeated, and the resulting slurry of receptor-coated beads is used immediately or stored at 4 ℃ for up to 1 week before use. [3H]GW2443 are used as radioligands for determination of competition binding to PPARα, PPARγ, and PPARδ, respectively. Unless otherwise indicated, the buffer used for all assays is 50 mM HEPES (pH 7), 50 mM NaCl, 5 mM CHAPS, 0.1 mg/mL BSA, and 10 mM DTT. For some experiments, the HEPES (pH 7) is replaced with 50 mM Tris (pH 8).
Cell Research	MDA-MB-231 cells are seeded at a density of 1 × 105 cells per 25 cm3 tissue culture flask. After 24 h (day 0), the growth medium is replaced with fresh medium containing rosiglitazone (50 μM), GW9662 (10 μM) or both together. Control flasks receives 0.1% DMSO. Cells are harvested on days 0, 3, 5, 7, 10 for each treatment condition by trypsinisation, stained using trypan blue, and the total and viable number of cells per flask calculates using a haemocytometer.(Only for Reference)

Synonyms	TIMTEC-BB SBB006523, GW 9662
Molecular Weight	276.68
Formula	C13H9ClN2O3
CAS No.	22978-25-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 27.7 mg/mL (100 mM)

Ethanol: 6.9 mg/mL (25 mM)), Heating is recommended.

References and Literature

1. Leesnitzer LM, et al. Biochemistry, 2002, 41(21), 6640-6650. 2. Seargent JM, et al. Br J Pharmacol, 2004, 143(8), 933-937. 3. Bendixen AC, et al. Proc Natl Acad Sci U S A, 2001, 98(5), 2443-2448. 4. Starkey K, et al. J Clin Endocrinol Metab, 2003, 88(1), 55-59. 5. Collino M, et al. Kidney Int, 2005, 68(2), 529-536. 6. Sato K, et al. PPARγ antagonist attenuates mouse immune-mediated bone marrow failure by inhibition of T cell function.Haematologica. 2016 Jan;101(1):57-67. 7. Qiao N, Lin Y, Wang Z, et al. Maresin1 Promotes M2 Macrophage Polarization Through peroxisome proliferator–activated receptor-γ Activation to Expedite Resolution of Acute Lung Injury[J]. Journal of Surgical Research. 2020, 256: 584-594. 8. Lin X, Ma Y, Qian T, et al. Basic Fibroblast Growth Factor Promotes Prehierarchical Follicle Growth and Yolk Deposition in the Chicken[J]. Theriogenology. 2019. 9. Zong X, Wang H, Xiao X, et al. Cathelicidin-WA facilitated intestinal fatty acid absorption through enhancing PPAR-γ dependent barrier function[J]. Frontiers in immunology. 2019, 10: 1674. 10. Miao Y, Zhang Y, Qiao S, et al. Oral administration of curcumin ameliorates pulmonary fibrosis in mice through 15d-PGJ2-mediated induction of hepatocyte growth factor in the colon[J]. Acta Pharmacologica Sinica. 2020: 1-14.

Citations

1. Miao Y, Wu X, Xue X, et al. Morin, the PPARγ agonist, inhibits Th17 differentiation by limiting fatty acid synthesis in collagen-induced arthritis. Cell Biology and Toxicology. 2022: 1-20. 2. Yang L, Zheng Y, Miao Y, et al. Bergenin, a PPARγ agonist, inhibits Th17 differentiation and subsequent neutrophilic asthma by preventing GLS1-dependent glutaminolysis. Acta Pharmacologica Sinica. 2021: 1-14. 3. Miao Y, Zhang C, Yang L, et al. The activation of PPARγ enhances Treg responses through up-regulating CD36/CPT1-mediated fatty acid oxidation and subsequent N-glycan branching of TβRII/IL-2Rα. Cell Communication and Signaling. 2022, 20(1): 1-22 4. Miao Y, Zhang Y, Qiao S, et al. Oral administration of curcumin ameliorates pulmonary fibrosis in mice through 15d-PGJ2-mediated induction of hepatocyte growth factor in the colon. Acta Pharmacologica Sinica. 2020: 1-14 5. Zong X, Wang H, Xiao X, et al. Cathelicidin-WA facilitated intestinal fatty acid absorption through enhancing PPAR-γ dependent barrier function. Frontiers in immunology. 2019, 10: 1674. 6. Qiao N, Lin Y, Wang Z, et al. Maresin1 Promotes M2 Macrophage Polarization Through peroxisome proliferator–activated receptor-γ Activation to Expedite Resolution of Acute Lung Injury. Journal of Surgical Research. 2020, 256: 584-594. 7. Lin X, Ma Y, Qian T, et al. Basic Fibroblast Growth Factor Promotes Prehierarchical Follicle Growth and Yolk Deposition in the Chicken. Theriogenology. 2019 8. Xie X, Zhang W, Zhou X, et al.Low doses of IFN-γ maintain self-renewal of leukemia stem cells in acute myeloid leukemia.Oncogene.2023: 1-13.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Neurodegenerative Disease Compound Library Anti-Diabetic Compound Library Bioactive Compounds Library Max Mitochondria-Targeted Compound Library Metabolism Compound Library Anti-Hypertension Compound Library Glycometabolism Compound Library Anti-Cancer Compound Library Transcription Factor-Targeted Compound Library

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Keywords

GW9662 22978-25-2 DNA Damage/DNA Repair Metabolism PPAR Peroxisome proliferator-activated receptors TIMTEC-BB SBB 006523 TIMTEC-BB SBB-006523 Inhibitor inhibit TIMTEC-BB SBB006523 GW-9662 GW 9662 inhibitor

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