Retinoid Receptor
Inhibitory Selectivity
Isoform-specific Inhibitors
Retinoid Receptor Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S6691New |
AGN 193109AGN 193109 is a novel class of RAR antagonists which effectively block hormoneinduced activation and is the most potent and effective antagonist of RARα, RARβ, and RARγ, with Kd values of 2 nM, 2 nM, and 3 nM, respectively. |
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| S1653 |
TretinoinTretinoin, which is a ligand for both the retinoic acid receptor (RAR) and the retinoid X receptor (RXR), can induce granulocytic differentiation and apoptosis in acute promyelocytic leukemia (APL) cells. |
HL60 differentiation measured by expression of CD11b (flow cytometry) after a single dose exposure to HH1 or MC180295 for 4 days. 1 mM ATRA and high concentrations of DMSO (1.25%) were used as positive controls.
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| S2098 |
BexaroteneBexarotene is a retinoid specifically selective for retinoid X receptors, used as an oral antineoplastic agent in the treatment of cutaneous T-cell lymphoma. |
Bexarotene inhibited microglia activation after SAH. Left, Representative immunofluorescent images of Iba1 (red) and DAPI (blue) in basal cortex at 24 h after SAH (N = 4/group, mean ± SD). Scale bar, 30 μm. Right, quantification of Iba1 positive cells per mm2. ***p < 0.001 compared with the Sham group, ###p < 0.001 compared with the SAH + vehicle group.
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| S1276 |
AdapaleneAdapalene is a dual RAR and RXR agonist, used in the treatment of acne. |
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| S1368 |
AcitretinAcitretin is a second generation retinoid used for psoriasis. |
Acitretin does not induce HIV reactivation in J-lat and ACH-2 cells. (a, b) HIV reactivation induced by acid retinoic (AR) derivative acitretin (25 – 1 μM) in J-Lat cells clone 8.4 (a) and 9.2(b). HDAC inhibitors (HDCAi) panobinostat (PNB, 0.16μM) and vorinostat (VOR, 4 – 0.16 μM) were used as controls. Reactivation was determined by the quantification of GFP+ cells (%) after culturing J-Lat with HDACi and acitretin for 24h. (c, d) HIV reactivation induced by acitretin and HDACi in ACH-2 cells. Reactivation was determined after 48h of incubation by quantification of CAp24 (c) and HIV RNA copy number (d) in the supernatant. Values represent mean±SD of at least three independent experiments performed in triplicate. UN, untreated. *P < 0.05; **P < 0.01; ***P < 0.001.
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| S1569 |
TazaroteneTazarotene is a retinoid prodrug of tazarotenic acid, which is a RAR agonist, used to treat psoriasis, acne, and sun damaged skin. |
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| S2933New |
AM580AM580 is a retinoic acid receptor agonist with Kd values of 8 nM, 131 nM and 450 nM for RARα, RARβ and RARγ. |
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| S6132New |
All trans-RetinalAll trans-Retinal, a component of the retinoid cycle, is converted to retinoic acid in vivo by the action of retinal dehydrogenase. Retinoic acid is a ligand for both RAR and RXR. All trans-retinal ias a potent photosensitizer. |
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| S4627 |
TTNPB (Arotinoid Acid)TTNPB (Arotinoid Acid) is a potent RAR agonist, and inhibits binding of [3H]tRA with IC50 of 5.1 nM, 4.5 nM, and 9.3 nM for human RARα, β, and γ, respectively. |
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| S4260 |
TamibaroteneTamibarotene is a synthetic retinoic acid receptor (RAR) agonist with high specificity for RARα and RARβ over RARγ. |
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| S4699 |
EtretinateEtretinate is an oral aromatic retinoid acid which is effective in psoriasis and other dermatological syndromes. It activates retinoid receptors, causing an induction of cell differentiation, inhibition of cell proliferation, and inhibition of tissue infiltration by inflammatory cells. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S6691New |
AGN 193109AGN 193109 is a novel class of RAR antagonists which effectively block hormoneinduced activation and is the most potent and effective antagonist of RARα, RARβ, and RARγ, with Kd values of 2 nM, 2 nM, and 3 nM, respectively. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S1653 |
TretinoinTretinoin, which is a ligand for both the retinoic acid receptor (RAR) and the retinoid X receptor (RXR), can induce granulocytic differentiation and apoptosis in acute promyelocytic leukemia (APL) cells. |
HL60 differentiation measured by expression of CD11b (flow cytometry) after a single dose exposure to HH1 or MC180295 for 4 days. 1 mM ATRA and high concentrations of DMSO (1.25%) were used as positive controls.
|
|
| S2098 |
BexaroteneBexarotene is a retinoid specifically selective for retinoid X receptors, used as an oral antineoplastic agent in the treatment of cutaneous T-cell lymphoma. |
Bexarotene inhibited microglia activation after SAH. Left, Representative immunofluorescent images of Iba1 (red) and DAPI (blue) in basal cortex at 24 h after SAH (N = 4/group, mean ± SD). Scale bar, 30 μm. Right, quantification of Iba1 positive cells per mm2. ***p < 0.001 compared with the Sham group, ###p < 0.001 compared with the SAH + vehicle group.
|
|
| S1276 |
AdapaleneAdapalene is a dual RAR and RXR agonist, used in the treatment of acne. |
||
| S1368 |
AcitretinAcitretin is a second generation retinoid used for psoriasis. |
Acitretin does not induce HIV reactivation in J-lat and ACH-2 cells. (a, b) HIV reactivation induced by acid retinoic (AR) derivative acitretin (25 – 1 μM) in J-Lat cells clone 8.4 (a) and 9.2(b). HDAC inhibitors (HDCAi) panobinostat (PNB, 0.16μM) and vorinostat (VOR, 4 – 0.16 μM) were used as controls. Reactivation was determined by the quantification of GFP+ cells (%) after culturing J-Lat with HDACi and acitretin for 24h. (c, d) HIV reactivation induced by acitretin and HDACi in ACH-2 cells. Reactivation was determined after 48h of incubation by quantification of CAp24 (c) and HIV RNA copy number (d) in the supernatant. Values represent mean±SD of at least three independent experiments performed in triplicate. UN, untreated. *P < 0.05; **P < 0.01; ***P < 0.001.
|
|
| S1569 |
TazaroteneTazarotene is a retinoid prodrug of tazarotenic acid, which is a RAR agonist, used to treat psoriasis, acne, and sun damaged skin. |
||
| S2933New |
AM580AM580 is a retinoic acid receptor agonist with Kd values of 8 nM, 131 nM and 450 nM for RARα, RARβ and RARγ. |
||
| S6132New |
All trans-RetinalAll trans-Retinal, a component of the retinoid cycle, is converted to retinoic acid in vivo by the action of retinal dehydrogenase. Retinoic acid is a ligand for both RAR and RXR. All trans-retinal ias a potent photosensitizer. |
||
| S4627 |
TTNPB (Arotinoid Acid)TTNPB (Arotinoid Acid) is a potent RAR agonist, and inhibits binding of [3H]tRA with IC50 of 5.1 nM, 4.5 nM, and 9.3 nM for human RARα, β, and γ, respectively. |
||
| S4260 |
TamibaroteneTamibarotene is a synthetic retinoic acid receptor (RAR) agonist with high specificity for RARα and RARβ over RARγ. |
||
| S4699 |
EtretinateEtretinate is an oral aromatic retinoid acid which is effective in psoriasis and other dermatological syndromes. It activates retinoid receptors, causing an induction of cell differentiation, inhibition of cell proliferation, and inhibition of tissue infiltration by inflammatory cells. |
