| S2871 |
T0070907
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T0070907 is a potent inhibitor of PPARγ (peroxisome proliferator activator receptor γ ) that induces G2/M arrest and enhances the effect of radiation in human cervical cancer cells through mitotic catastrophe. It also acts as an antagonist of PPARγ that suppresses breast cancer cell proliferation and motility via both PPARgamma-dependent and -independent mechanisms.
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Nucleic Acids Res, 2025, 53(14)gkaf669
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Cell Rep Med, 2025, 6(10):102373
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Apoptosis, 2025, 30(5-6):1391-1409
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| S2915 |
GW9662
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GW9662 is a selective PPAR antagonist for PPARγ with IC50 of 3.3 nM in a cell-free assay, with at least 10- to 600-fold functional selectivity in cells with PPARγ versus PPARα and PPARδ.
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J Extracell Vesicles, 2025, 14(8):e70143
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Stem Cell Res Ther, 2025, 16(1):347
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Genes Dis, 2025, 12(3):101333
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| S2798 |
GW6471
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GW 6471 is a potent antagonist of PPARα with IC50 of 0.24 μM.
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Mol Cancer, 2025, 24(1):34
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Cell Mol Immunol, 2025, 10.1038/s41423-025-01338-y
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Apoptosis, 2025, 30(5-6):1391-1409
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| S8025 |
GSK3787
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GSK3787 is a selective and irreversible antagonist of PPARδ with pIC50 of 6.6, with no measurable affinity for hPPARα or hPPARγ.
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JACC Basic Transl Sci, 2025, 10(7):101222
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Drug Des Devel Ther, 2024, 18:4799-4824
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Cell Discov, 2023, 9(1):54
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| S5817 |
GSK0660
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GSK0660 is a potent PPARβ/δ antagonist with a pIC50 of 6.8 (binding assay IC50 = 155 nM; antagonist assay IC50 = 300 nM) and is nearly inactive on PPARα and PPARγ with IC50s above approximately 10 μM.
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Cells, 2024, 13(3):206.
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Cells, 2024, 13(3)206
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Elife, 2023, 12e82970
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| S0531 |
DG172 dihydrochloride
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DG-172 dihydrochloride is a novel PPARβ/δ-selective antagonist with the IC50 of 27 nM.
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Cell Signal, 2022, 93:110304
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| E8300New |
Amezalpat
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Amezalpat acts as a PPARα antagonist with an IC50 value of 58 nM. This compound demonstrates antineoplastic effects.
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| S0773 |
Mifobate
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Mifobate (SR-202), a potent and specific PPARγ antagonist, selectively inhibits Thiazolidinedione (TZD)-induced PPARγ transcriptional activity (IC50=140 μM).
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