A selective, irreversible PPARβ/δ antagonist
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GSK3787

Item No. 15219

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-chloro-N-[2-[[5-(trifluoromethyl)-2-pyridinyl]sulfonyl]ethyl]-benzamide
CAS Number
188591-46-0
Molecular Formula
C15H12ClF3N2O3S
Formula Weight
392.8
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 3 mg/mlDMSO: 5 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.3 mg/ml
λmax
238 nm
SMILES
O=S(C1=NC=C(C(F)(F)F)C=C1)(CCNC(C2=CC=C(Cl)C=C2)=O)=O
InChi Code
InChI=1S/C15H12ClF3N2O3S/c16-12-4-1-10(2-5-12)14(22)20-7-8-25(23,24)13-6-3-11(9-21-13)15(17,18)19/h1-6,9H,7-8H2,(H,20,22)
InChi Key
JFUIMTGOQCQTPF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $52

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    10 mg

    $81

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    25 mg

    $176

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    50 mg

    $275

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    Product Description

    PPARβ/δ is thought to play a role in lipid homeostasis and glucose disposal by regulating genes involved in fatty acid oxidation, reverse cholesterol transport, and carbon substrate utilization in skeletal muscle. It has also been implicated in the progression of certain cancers.1,2,3,4 GSK3787 is an irreversible antagonist of PPARβ/δ (pIC50 = 6.6) with no measurable affinity for PPARα or PPARγ (pIC50 >5).5 At 1μM, it inhibits the expression of PPARβ/δ-regulated target genes, pyruvate dehydrogenase kinase 4 and carnitine palmitoyl transferase 1a, which are important for energy homeostasis in human skeletal muscle cells.5 GSK3787 (at 1 μM) also antagonizes agonist-induced expression of angiopoietin-like protein 4 in mouse fibroblasts, mouse keratinocytes, and human MCF-7, Huh7, and HepG2 cancer cell lines.6

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Michalik, L., Desvergne, B., and Wahli, W. Peroxisome-proliferator-activated receptors and cancers: Complex stories. Nat. Rev. Cancer 4(1), 61-70 (2004).

    2. Girroir, E.E., Hollingshead, H.E., Billin, A.N., et al. Peroxisome proliferator-activated receptor-ß/δ (PPAR ß/δ) ligands inhibit growth of UACC903 and MCF7 human cancer cell lines. Toxicology 243(1-2), 236-243 (2008).

    3. Peters, J.M., Foreman, J.E., and Gonzalez, F.J. Dissecting the role of peroxisome proliferator-activated receptor-ß/δ (PPARß/δ) in colon, breast, and lung carcinogenesis. Cancer Metastasis Rev. 30(3-4), 619-640 (2011).

    4. Elikkottil, J., Kohli, D.R., and Gupta, K. Antitumor activity of a PPARδ antagonist. Cancer Biol. Ther. 8(13), 1262-1264 (2009).

    5. Shearer, B.G., Wiethe, R.W., Ashe, A., et al. Identification and characterization of 4-chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide (GSK3787), a selective and irreversible peroxisome proliferator-activated receptor δ (PPARδ) antagonist. J. Med. Chem. 53(4), 1857-1861 (2010).

    6. Palkar, P.S., Borland, M.G., Naruhn, S., et al. Cellular and pharmacological selectivity of the peroxisome proliferator-activated receptor-β/δ antagonist GSK3787. Mol. Pharmacol. 78(3), 419-430 (2010).