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Retinoid Receptor

Retinoid receptors are nuclear receptors (a class of proteins) that bind to retinoids. When bound to a retinoid, they act as transcription factors, altering the expression of genes with corresponding response elements. Significant age-related declines in the levels of retinoid receptors in the forebrains of rats have been reversed by supplementation with the omega-3 fatty acids eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA), which can restore neurogenesis. Subtypes include: Retinoic acid receptors (RARs), Retinoid X receptors (RXRs), RAR-related orphan receptors (RORs).

  • Isotretinoin
    T16114759-48-2
    Isotretinoin (13-cis-Retinoic acid) binds to and activates nuclear retinoic acid receptors (RARs); activated RARs serve as transcription factors that promote cell differentiation and apoptosis. Isotretinoin is a naturally-occurring retinoic acid with potential antineoplastic activity. This agent also exhibits immunomodulatory and anti-inflammatory responses and inhibits ornithine decarboxylase, thereby decreasing polyamine synthesis and keratinization.
    • $36
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  • BMS 195614
    T22192253310-42-8
    BMS 195614 (BMS614) is a selective RARα antagonist. BMS 195614 can bind to the RARα subunit.
    • $181
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  • ER 50891
    T22767187400-85-7In house
    ER-50891 is a potent retinoic acid receptor alpha (RARα) antagonist. er-50891 reduces the inhibitory effect of allosteric retinoic acid and restores osteoblast differentiation induced by bone morphogenetic protein 2.
    • $197
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  • KCL-286
    T785751952276-71-9In house
    KCL-286 is an orally available and potent retinoic acid receptor beta agonist for the amelioration of spinal cord injury (SCI).
    • $479
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  • K-8012
    T242401346513-17-4In house
    K-8012 is a modulator of the N-terminally truncated RXRα and improves anticancer activities in an RXRα-dependent manner.
    • $117
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  • Cecropin B acetate
    TP1313L
    Cecropin B acetate induces NF-κB activation and suppresses CYP3A29 by disrupting the association of the PXR/retinoid X receptor alpha (RXR-α) complex with DNA sequences. Cecropin B acetate exhibits strong antimicrobial activity.
    • $87
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  • Fluorobexarotene
    T113031190848-23-7In house
    Fluorobexarotene possesses an apparent RXR binding affinity that is 75% greater than Bexarotene. Fluorobexarotene  is a potent retinoid-X-receptor (RXR) agonist, with a Ki value of 12 nM and an EC50 value of 43 nM for RXRα receptor. Fluorobexarotene possesses an apparent RXR binding affinity that is 75% greater than Bexarotene.
    • $183
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  • MSU-42011
    T774992456434-36-7In house
    MSU-42011 is an orally active retinoid X receptor-like (RXR) agonist.MSU-42011 potently inhibits the expression of iNOS, low SREBP-induced and activated RXR, and p-ERK at the protein level.MSU-42011 has demonstrated antitumor activity in a kras-driven mouse model of lung cancer.MSU-42011 is an effective therapy for the treatment of preclinical krasdriven lung cancer and has immunomodulatory activity.
    • $41
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  • BMS493
    T14689215030-90-3In house
    BMS493 is an inverse agonist of the pan-retinoic acid receptor (RAR) that inhibits retinoic acid-induced differentiation, enhances the interaction of nuclear co-inhibitors with RARs, attenuates RA signaling, potentiates TPP-induced toxicity, and inhibits the increase in phospholipase A2 activity.
    • $49
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  • Tamibarotene
    T669494497-51-5
    Tamibarotene (Amnolake) is an orally active, synthetic retinoid, developed to overcome all-trans retinoic acid (ATRA) resistance, with potential antineoplastic activity.
    • $39
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    TargetMol | Citations Cited
  • Bexarotene
    T6410153559-49-0
    Bexarotene (LGD1069) is a retinoid analogue that is used to treat the skin manifestations of cutaneous T cell lymphoma (CTCL).
    • $30
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    TargetMol | Citations Cited
  • Adapalene
    T1093106685-40-9
    Adapalene (CD271) is a dual RAR and RXR agonist, utilized in the treatment of skin conditions.
    • $42
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  • Tazarotene
    T6696118292-40-3
    Tazarotene (Zorac) is a synthetic, topical retinoid. Tazarotene induces the expression of tazarotene-induced gene 3 (TIG3), a tumor suppressor gene. In psoriasis, tazarotene normalizes abnormal keratinocyte differentiation and reduces their hyperproliferation.
    • $32
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  • Acitretin
    T133055079-83-9
    Acitretin (Ro 10-1670) is a second-generation, systemic retinoid that has been used in the treatment of psoriasis.
    • $111
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  • AR7
    T395580306-38-3
    AR7 is a retinoic acid receptor α (RARα) antagonist.
    • $31
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  • Retinoic acid
    T1051302-79-4
    Retinoic acid (Tretinoin), a metabolite of vitamin A, is a natural agonist of the retinoic acid receptor RAR and inhibits RARα/β/γ (IC50=14 nM). Retinoic acid induces cellular differentiation, reduces cellular proliferation, and inhibits tumorigenesis.
    • $33
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  • Ch55
    T14946110368-33-7
    Ch55 (3,5-Di-tert-butylchalcone) is an effective inducer of the differentiation of HL60 cells (EC50 = 200 nM) and shows high affinity with RAR-α and RAR-β receptors. Ch55 can be used in studies about cancer.
    • $41
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  • Magnolol
    T3000528-43-8
    Magnolol (5,5'-Diallyl-2,2'-biphenyldiol) is a dual agonist of RXRα( EC50=10.4 μM) and PPARγ(EC50=17.7 μM). It blocks TNF-α-induced NF-KB activation.
    • $39
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  • WYC-209
    T53412131803-90-0
    WYC-209 inhibits proliferation of malignant murine melanoma tumor-repopulating cells (TRCs, IC50: 0.19 uM). It targets the retinoic acid receptor (RAR).
    • $55
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  • AGN 192870
    T61588166977-57-7
    AGN 192870 is a potent retinoic acid receptor (RAR) antagonist.AGN 192870 can be used to study cell growth arrest, differentiation and apoptosis.
    • $64
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  • palovarotene
    T4538410528-02-8
    Palovarotene (Ro 3300074) is an agonist of nuclear retinoic acid receptor γ (RAR-γ).
    • $33
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  • UVI 3003
    T17209847239-17-2
    UVI 3003 is a highly selective antagonist of the retinoid X receptor. UVI 3003 inhibits Xenopus and human RXRα in Cos7 cells (IC50s: 0.22 and 0.24 μM, respectively).
    • $30
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  • AM580
    T5854102121-60-8
    AM580 (CD336) is a retinoic acid receptor agonist that is selective for RARα( IC50 : 8 nM )
    • $33
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  • AC-55649
    T1409059662-49-6
    AC-55649 is a potent, highly isoform-selective agonist of human RARβ2 receptor, with a pEC50 of 6.9.
    • $58
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  • Etodolac
    T100241340-25-4
    Etodolac (AY-24236) inhibits the activity of cyclooxygenase I and II, thereby preventing the formation of prostaglandin which is involved in the induction of pain, fever, and inflammation. Etodolac is a pyranocarboxylic acid and non-steroidal anti-inflammatory drug (NSAID) with antipyretic and analgesic activities. It also inhibits platelet aggregation by blocking platelet cyclooxygenase and the subsequent formation of thromboxane A2.
    • $34
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  • Mofarotene
    T68104125533-88-2
    Mofarotene (Ro-40-8757) is a small molecule compound that shows considerable antitumor activity in many cancer cell lines and can be used for the treatment of tumors and respiratory diseases.Mofarotene is a retinoic acid analog that binds to and activates retinoic acid receptors (RARs), which alters the expression of certain genes, leading to reduced cell differentiation and cell proliferation in susceptible cells.
    • $109
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  • CD3254
    T14912196961-43-0
    CD3254 is a selective and potent retinoid X receptor-like (RXR) agonist that inhibits neuronal cell death with OGD/reoxygenation.
    • $50
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  • AC-261066
    T14089870773-76-5
    AC-261066 is an orally available and isoform-selective agonist of RARβ2 with a pEC50 of 8.0.
    • $30
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  • Tarenflurbil
    T584351543-40-9
    Tarenflurbil ((R)-Flurbiprofen) is the non-cyclooxygenase inhibiting R-enantiomer of the non-steroidal anti-inflammatory drug flurbiprofen, which was assessed as a remedy for Alzheimer's disease.
    • $50
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  • Liarozole
    T11847L115575-11-6
    Liarozole (R75251 dihydrochloride) is a cytochrome P450 (CYP450) dependent inhibitor, orally active, it also a potent inhibitor of estrogen (via inhibition of aromatase) and testicular androgen synthesis (inhibition of 17 ,20-lyase).Liarozole dihydrochloride is an imidazole derivative; it is being investigated as a non-hormonal agent in prostate cancer and in the treatment of various other cancers and skin disorders.
    • $76
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  • BMS641
    T26854369364-50-1
    BMS641 (BMS-209641) is a selective and potent RARβ agonist.BMS641 has a high affinity for RARβ and synergistically activates RARβ and RARgamma to induce cellular maturation into specialized neuronal subtypes.
    • $159
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  • AGN 194310
    T14143229961-45-9
    AGN 194310 (VTP-194310) is retinioic acid receptors (RARs) pan-antagonist. The Kd values of 3 nM, 2 nM, 5 nM for RARα, RARβ, RARγ, respectively[1][2].
    • $596
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  • AGN 196996
    T10261958295-17-5
    AGN 196996 is a potent and selective inhibitor of RARα (Ki: 2 nM).AGN 196996 has very low affinity for RARβ and RARγ, with a Ki of 1087 nM and 8523 nM, respectively.
    • $90
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  • LE135
    T22920155877-83-1
    LE135 is a potent RAR antagonist that binds selectively to RARα (Ki of 1.4 μM) and RARβ (Ki of 220 nM), and has a higher affinity to RARβ. LE135 is highly selective over RARγ, RXRα, RXRβ and RXRγ. LE135 is also a potent TRPV1 and TRPA1 receptors activator with EC50s of 2.5 μM and 20 μM, respectively.
    • $39
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  • HX 531
    T22843188844-34-0
    RXR antagonist
    • $39
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  • BMS453
    T21714166977-43-1
    BMS453 (BMS-189453), a synthetic retinoid, is a potent and selective agonist of RARβ and a potent testicular toxin. BMS453 inhibits breast cell growth predominantly through the induction of active TGFβ.
    • $58
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  • CD2665
    T14911170355-78-9
    CD2665 is an orally active antagonist of retinoic acid receptor (RAR). For RARγ and RARβ, the Kis are 110 nM and 306 nM.
    • $83
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  • BMS270394
    T26846262433-54-5
    BMS270394 is a RARγ agonist used in the study of breast cancer and dermatologic diseases.
    • $399
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  • CD 1530
    T21686107430-66-0
    CD 1530 is a selective and potent RARγ agonist (Kd:150 nM) with potential anticancer activity, shows insecticidal activity against Cryptobacterium hidradii nematodes, and can be used to study oral carcinogenesis.
    • $69
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  • PA452
    T16425457657-34-0
    PA452 is a selective antagonist of retinoic X receptor (RXR) and suppresses the effect of Retinoic acid on Th1/Th2 development.
    • $84
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  • Talarozole
    T7370201410-53-9
    Talarozole (R115866) is an oral systemic all-trans retinoic acid metabolism blocking agent (RAMBA). Talarozole inhibits both CYP26A1 and CYP26B1 with IC50s of 5.4 and 0.46 nM, respectively.Talarozole for the treatment of acne, psoriasis and other keratinization disorders.
    • $66
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  • BMS 753
    T22049215307-86-1
    BMS 753 is an agonist of isotype-selective retinoic acid receptor α (RARα, Ki= 2 nM).
    • $58
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  • Fenretinide
    T187265646-68-6
    Fenretinide (4-HPR) is an orally-active synthetic retinoid derivative with potential antineoplastic and chemopreventive activities.
    • $34
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  • CD437
    T4371125316-60-1
    CD437 (AHPN) is a specifc Retinoic Acid Receptor γ (RARγ) agonist.
    • $34
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  • Bigelovin
    TN67353668-14-2
    Bigelovin is a selective retinoid X receptor α agonist. Bigelovin suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation.It is also known as a potent cytotoxic sesquiterpene lactone from Inula sp.
    • $93
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  • TTNPB
    T128871441-28-6
    TTNPB (Ro 13-7410,AGN-191183), a potent RAR agonist, inhibits binding of [3H]tRA of human RARα (IC50: 5.1 nM), β (IC50: 4.5 nM), and γ (IC50: 9.3 nM), respectively.
    • $33
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  • trifarotene
    T7586895542-09-3
    Trifarotene (CD5789) is a potent and selective RARγ agonist with 65-fold and 16-fold selectivitiy for the RARγ (EC50=7.7 nM) over RARα (EC50=500 nM) and RARβ (EC50=125 nM).
    • $36
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  • LG-100064
    T11844153559-46-7
    LG-100064 is an agonist of retinoid-X-receptor (RXR)(EC50s of 330 nM, 200 nM, and 260 nM for RXRα, RXRβ and RXRγ)
    • $39
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  • MM 11253
    T23005345952-44-5
    MM 11253 is a RARγ antagonist with IC50 of 44nM.
    • $34
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  • LY 178002
    T15825107889-32-7
    LY 178002 is an effective inhibitor of 5-lipoxygenase (5-LPO), phospholipase A2 (IC50: 0.6 μM for 5-lipoxygenase). LY 178002 also inhibits cellular production of LTB4 by human polymorphonuclear leukocytes and displays relatively weak inhibition on cycloox
    • $1,520
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