PPAR
Inhibitory Selectivity
Isoform-specific Inhibitors
PPAR Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S2871 |
T0070907T0070907 is a potent and selective PPARγ inhibitor with IC50 of 1 nM in a cell-free assay, with a >800-fold selectivity over PPARα and PPARδ. T0070907 significantly decreases the levels of DNA-PKcs and RAD51 proteins in ME-180 and SiHa cells. |
Knocking down LKB1 reversed the PPARc antagonist T0070907-induced changes in the protein expression of the M1 markers (iNOS, green) and the M2 markers (CD206, red) by immunofluorescence staining. Scale bar = 20 μm.
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| S7767 |
AZ6102AZ6102 is a potent TNKS1/2 inhibitor that has 100-fold selectivity against other PARP family enzymes and shows IC50 of 5 nM for Wnt pathway inhibition in DLD-1 cells. |
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| S2798 |
GW6471GW 6471 is a potent antagonist of PPARα with IC50 of 0.24 μM. |
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| S7484 |
FH535FH535 is a Wnt/β-catenin signaling inhibitor and also a dual PPARγ and PPARδ antagonist. |
Ki-67 staining in xenograft tissues from FH535-treated and control group. Magnifications: ×200 in left column, ×400 in right column.
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| S5824 |
Cinnamyl alcoholCinnamyl alcohol is a naturally occurring compound that is found within cinnamon. Cinnamyl alcohol can be significantly attenuated the enhanced expression of obesity-related proteins PPARγ in MDI medium-cultivated 3T3-L1 cells. |
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| S9129 |
20(S)-Ginsenoside Rh120(S)-Ginsenoside Rh1 (Prosapogenin A2, Sanchinoside B2, Sanchinoside Rh1) is one of major bioactive compounds extracted from red ginseng, which has been increasingly used for enhancing cognition and physical health worldwide. It exhibits potent characteristics of anti-inflammatory, antioxidant, immunomodulatory effects, and positive effects on the nervous system. Ginsenoside Rh1 inhibits the expression of PPAR-γ, TNF-α, IL-6, and IL-1β. |
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| S8029 |
WY-14643 (Pirinixic Acid)WY-14643 (Pirinixic Acid, NSC 310038) is a potent and selective PPARα activator with an EC50 of 1.5 μM. |
(A) Acot1 mRNA following adenovirus treatments and 0.1% Wy-14643 supplementation (n=7-9). (B) H&E staining shows that Wy-14643 reduced and normalized lipid droplet accumulation in the Acot1 knockdown treatment group.
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| S3290 |
Procyanidin B2Procyanidin B2 (PCB2), a natural flavonoid found in commonly consumed foods, possess anti-inflammatory, anti-oxidant and anti-cancer activities. Procyanidin B2 activates PPARγ to induce M2 polarization in mouse macrophages. Procyanidin B2 significantly suppresses the activation of NLRP3 inflammasome in the lung tissue induced by paraquat in the rat model. |
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| S9723 |
CDDO-ImCDDO-Im (CDDO-Imidazolide, RTA-403, TP-235) is an activator of nuclear factor erythroid 2–related factor 2 (Nrf2) and peroxisome proliferator-activated receptor (PPAR). CDDO-Im binds to PPARα and PPARγ with Ki of 232 nM and 344 nM, respectively. CDDO-Im inhibits inflammatory response and tumor growth in vivo. |
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| S3875 |
AlpinetinAlpinetin, a composition of Alpinia katsumadai Hayata, has been reported to have a number of biological properties, such as antibacterial, antitumor and other important therapeutic activities. Alpinetin is a flavonoid isolated from Alpinia katsumadai Hayata, activates activates PPAR-γ, with potent anti-inflammatory activity. |
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| S4708 |
PalmitoylethanolamidePalmitoylethanolamide (PEA, Palmidrol, N-palmitoylethanolamine) is an endogenous fatty acid amide and selectively activates PPAR-α in vitro with an EC50 value of 3.1±0.4 μM. |
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| S9177 |
Gypenoside XLIXGypenoside XLIX, a naturally occurring gynosaponin, is a selective peroxisome proliferator-activated receptor (PPAR)-alpha activator. |
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| S2915 |
GW9662GW9662 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. |
Primary microglia (G) were pretreated with JuA at indicated concentrations with or without GW9662 (2 μM) for 18 h, and then incubated with 2 mg/mL Aβ42 in the presence of vehicle (DMSO) or drug for an additional 24 h. The intracellular Aβ42 levels were measured using ELISA.
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| S0531 |
DG172 dihydrochlorideDG-172 dihydrochloride is a novel PPARβ/δ-selective antagonist with the IC50 of 27 nM. |
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| S5817 |
GSK0660GSK0660 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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| S9199 |
Pseudoginsenoside F11Pseudoginsenoside F11, a natural product found in American ginseng but not in Asian ginseng, is a novel partial PPARγ agonist. |
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| S3786 |
GlabridinGlabridin (Q-100692, KB-289522, LS-176045), one of the active phytochemicals in licorice extract, binds to and activates the ligand binding domain of PPARγ, as well as the full length receptor. It is also a GABAA receptor positive modulator promoting fatty acid oxidation and improving learning and memory. |
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| S0170 |
BMS-687453BMS-687453 (compound 2) is a potent and selective agonist of PPARα with EC50 of 10 nM and IC50 of 260 nM for human PPARα. |
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| S9674 |
SaroglitazarSaroglitazar (Lipaglyn, ZYH1) is an agonist of peroxisome proliferator-activated receptor (PPAR) with EC50 of 0.65 pM and 3 nM for hPPARα and hPPARγ in HepG2 cells, respectively. |
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| S9480 |
Raspberry KetoneRaspberry ketone (p-Hydroxybenzyl acetone, Frambinone, Oxyphenylon, Rheosmin, Rasketone) is a natural phenolic compound that is the primary aroma compound of red raspberries. Raspberry ketone shows cardioprotective action against isoproterenol-induced myocardial infarction in rats, and the effects may be due to its PPAR-α agonistic activity. |
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| S6906 |
Capric acidCapric acid (DA, Decanoic acid, Decylic acid), a component of medium-chain triclycerides occurring naturally in coconut oil and palm kernel oil, contributes to seizure control through direct AMPA receptor inhibition. Capric acid is also a modulating ligand for PPARs. Due to its specific melting range the product may be solid, liquid, a solidified melt or a supercooled melt. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S2871 |
T0070907T0070907 is a potent and selective PPARγ inhibitor with IC50 of 1 nM in a cell-free assay, with a >800-fold selectivity over PPARα and PPARδ. T0070907 significantly decreases the levels of DNA-PKcs and RAD51 proteins in ME-180 and SiHa cells. |
Knocking down LKB1 reversed the PPARc antagonist T0070907-induced changes in the protein expression of the M1 markers (iNOS, green) and the M2 markers (CD206, red) by immunofluorescence staining. Scale bar = 20 μm.
|
|
| S7767 |
AZ6102AZ6102 is a potent TNKS1/2 inhibitor that has 100-fold selectivity against other PARP family enzymes and shows IC50 of 5 nM for Wnt pathway inhibition in DLD-1 cells. |
||
| S2798 |
GW6471GW 6471 is a potent antagonist of PPARα with IC50 of 0.24 μM. |
||
| S7484 |
FH535FH535 is a Wnt/β-catenin signaling inhibitor and also a dual PPARγ and PPARδ antagonist. |
Ki-67 staining in xenograft tissues from FH535-treated and control group. Magnifications: ×200 in left column, ×400 in right column.
|
|
| S5824 |
Cinnamyl alcoholCinnamyl alcohol is a naturally occurring compound that is found within cinnamon. Cinnamyl alcohol can be significantly attenuated the enhanced expression of obesity-related proteins PPARγ in MDI medium-cultivated 3T3-L1 cells. |
||
| S9129 |
20(S)-Ginsenoside Rh120(S)-Ginsenoside Rh1 (Prosapogenin A2, Sanchinoside B2, Sanchinoside Rh1) is one of major bioactive compounds extracted from red ginseng, which has been increasingly used for enhancing cognition and physical health worldwide. It exhibits potent characteristics of anti-inflammatory, antioxidant, immunomodulatory effects, and positive effects on the nervous system. Ginsenoside Rh1 inhibits the expression of PPAR-γ, TNF-α, IL-6, and IL-1β. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S8029 |
WY-14643 (Pirinixic Acid)WY-14643 (Pirinixic Acid, NSC 310038) is a potent and selective PPARα activator with an EC50 of 1.5 μM. |
(A) Acot1 mRNA following adenovirus treatments and 0.1% Wy-14643 supplementation (n=7-9). (B) H&E staining shows that Wy-14643 reduced and normalized lipid droplet accumulation in the Acot1 knockdown treatment group.
|
|
| S3290 |
Procyanidin B2Procyanidin B2 (PCB2), a natural flavonoid found in commonly consumed foods, possess anti-inflammatory, anti-oxidant and anti-cancer activities. Procyanidin B2 activates PPARγ to induce M2 polarization in mouse macrophages. Procyanidin B2 significantly suppresses the activation of NLRP3 inflammasome in the lung tissue induced by paraquat in the rat model. |
||
| S9723 |
CDDO-ImCDDO-Im (CDDO-Imidazolide, RTA-403, TP-235) is an activator of nuclear factor erythroid 2–related factor 2 (Nrf2) and peroxisome proliferator-activated receptor (PPAR). CDDO-Im binds to PPARα and PPARγ with Ki of 232 nM and 344 nM, respectively. CDDO-Im inhibits inflammatory response and tumor growth in vivo. |
||
| S3875 |
AlpinetinAlpinetin, a composition of Alpinia katsumadai Hayata, has been reported to have a number of biological properties, such as antibacterial, antitumor and other important therapeutic activities. Alpinetin is a flavonoid isolated from Alpinia katsumadai Hayata, activates activates PPAR-γ, with potent anti-inflammatory activity. |
||
| S4708 |
PalmitoylethanolamidePalmitoylethanolamide (PEA, Palmidrol, N-palmitoylethanolamine) is an endogenous fatty acid amide and selectively activates PPAR-α in vitro with an EC50 value of 3.1±0.4 μM. |
||
| S9177 |
Gypenoside XLIXGypenoside XLIX, a naturally occurring gynosaponin, is a selective peroxisome proliferator-activated receptor (PPAR)-alpha activator. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S2915 |
GW9662GW9662 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. |
Primary microglia (G) were pretreated with JuA at indicated concentrations with or without GW9662 (2 μM) for 18 h, and then incubated with 2 mg/mL Aβ42 in the presence of vehicle (DMSO) or drug for an additional 24 h. The intracellular Aβ42 levels were measured using ELISA.
|
|
| S0531 |
DG172 dihydrochlorideDG-172 dihydrochloride is a novel PPARβ/δ-selective antagonist with the IC50 of 27 nM. |
||
| S5817 |
GSK0660GSK0660 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. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S9199 |
Pseudoginsenoside F11Pseudoginsenoside F11, a natural product found in American ginseng but not in Asian ginseng, is a novel partial PPARγ agonist. |
||
| S3786 |
GlabridinGlabridin (Q-100692, KB-289522, LS-176045), one of the active phytochemicals in licorice extract, binds to and activates the ligand binding domain of PPARγ, as well as the full length receptor. It is also a GABAA receptor positive modulator promoting fatty acid oxidation and improving learning and memory. |
||
| S0170 |
BMS-687453BMS-687453 (compound 2) is a potent and selective agonist of PPARα with EC50 of 10 nM and IC50 of 260 nM for human PPARα. |
||
| S9674 |
SaroglitazarSaroglitazar (Lipaglyn, ZYH1) is an agonist of peroxisome proliferator-activated receptor (PPAR) with EC50 of 0.65 pM and 3 nM for hPPARα and hPPARγ in HepG2 cells, respectively. |
||
| S9480 |
Raspberry KetoneRaspberry ketone (p-Hydroxybenzyl acetone, Frambinone, Oxyphenylon, Rheosmin, Rasketone) is a natural phenolic compound that is the primary aroma compound of red raspberries. Raspberry ketone shows cardioprotective action against isoproterenol-induced myocardial infarction in rats, and the effects may be due to its PPAR-α agonistic activity. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S6906 |
Capric acidCapric acid (DA, Decanoic acid, Decylic acid), a component of medium-chain triclycerides occurring naturally in coconut oil and palm kernel oil, contributes to seizure control through direct AMPA receptor inhibition. Capric acid is also a modulating ligand for PPARs. Due to its specific melting range the product may be solid, liquid, a solidified melt or a supercooled melt. |
