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Metabolism

Acetyl-CoA Carboxylase

Amino Acids and Derivatives

Angiotensin-converting Enzyme (ACE)

Endogenous Metabolite

Glutathione Peroxidase

(40)

Glyoxalase

(2)

HIF/HIF Prolyl-Hydroxylase

Indoleamine 2,3-Dioxygenase (IDO)

(33)

Isocitrate Dehydrogenase (IDH)

Mitochondrial Metabolism

(94)

N-Acetylglucosaminyltransferase

Procollagen C Proteinase

(1)

Prolyl Endopeptidase (PREP)

Reactive Oxygen Species

Serine/threonin kinase

(47)

Stearoyl-CoA Desaturase (SCD)

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).

Filter HomeSignaling PathwaysMetabolismRetinoid Receptor

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.

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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.

$163

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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.

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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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LY2955303

T158111433497-19-8

LY2955303 is an effective and selective antagonist of retinoic acid receptor gamma (RARγ, Ki = 1.09 nM).

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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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Adapalene

T1093106685-40-9

Adapalene (CD271) is a dual RAR and RXR agonist, utilized in the treatment of skin conditions.

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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), showing higher affinity for RARβ. It is highly selective over RARγ, RXRα, RXRβ, and RXRγ. LE135 also acts as a potent TRPV1 and TRPA1 receptor activator with EC50s of 2.5 μM and 20 μM, respectively.

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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.

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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.

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CD437

T4371125316-60-1

CD437 (AHPN) is a specifc Retinoic Acid Receptor γ (RARγ) agonist.

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Bexarotene

T6410153559-49-0

Bexarotene (LGD1069) is a retinoid analogue that is used to treat the skin manifestations of cutaneous T cell lymphoma (CTCL).

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MM 11253

T23005345952-44-5

MM 11253 is a RARγ antagonist with IC50 of 44nM.

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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.

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AM580

T5854102121-60-8

AM580 (CD336) is a retinoic acid receptor agonist that is selective for RARα( IC50 : 8 nM )

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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.

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Peretinoin

TQ006481485-25-8

Peretinoin (NIK333) is an oral acyclic retinoid with a vitamin A-like structure that targets retinoid nuclear receptors such as RXR and RAR.

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AR7

T395580306-38-3

AR7 is a retinoic acid receptor α (RARα) antagonist.

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AGN 193109

TQ0097171746-21-7

AGN 193109, a retinoid analog, is a potent and specific antagonist of RARs (Kds: 2 nM, 2 nM, and 3 nM for RARα, RARβ, and RARγ).

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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.

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Talarozole

T7370201410-53-9

Talarozole (R115866) is an oral systemic all-trans retinoic acid metabolism blocking agent (RAMBA) that inhibits CYP26A1 and CYP26B1 with IC50s of 5.4 and 0.46 nM, respectively, for treating acne, psoriasis, and other keratinization disorders.

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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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Isotretinoin

T16114759-48-2

Isotretinoin (13-cis-Retinoic acid) binds to and activates nuclear retinoic acid receptors (RARs), which act as transcription factors that promote cell differentiation and apoptosis. This naturally occurring retinoic acid has potential antineoplastic activity, exhibits immunomodulatory and anti-inflammatory responses, and inhibits ornithine decarboxylase, thereby decreasing polyamine synthesis and keratinization.

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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).

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Fenretinide

T187265646-68-6

Fenretinide (4-HPR) is an orally-active synthetic retinoid derivative with potential antineoplastic and chemopreventive activities.

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HX 531

T22843188844-34-0

HX 531 is a RXR antagonist (IC50 of 18 nM). HX 531 prevents HF diet-induced obesity, insulin resistance, and diabetes by reducing tissue TG content in white adipose tissue (WAT), skeletal muscle, and liver in mice.

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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.

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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.

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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.

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trifarotene

T7586895542-09-3

Trifarotene (CD5789) is a potent and selective RARγ agonist, exhibiting 65-fold and 16-fold selectivity for RARγ (EC50=7.7 nM) over RARα (EC50=500 nM) and RARβ (EC50=125 nM).

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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).

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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.

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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.

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palovarotene

T4538410528-02-8

Palovarotene (Ro 3300074) is an agonist of nuclear retinoic acid receptor γ (RAR-γ).

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Acitretin

T133055079-83-9

Acitretin (Ro 10-1670) is a second-generation systemic retinoid used in the treatment of psoriasis.

$111

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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.

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Ro 41-5253

T28589144092-31-9

Ro 41-5253 is an orally active RARα antagonist, ligand, and partial agonist of peroxisome proliferator-activated receptor (PPAR)-γ. It exhibits antitumor activity, inhibits proliferation, and induces apoptosis in MCF-7 and ZR-75.1 estrogen receptor-positive breast cancer cells.

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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.

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UVI 3003

T17209847239-17-2

UVI 3003 is a highly selective antagonist of the retinoid X receptor, inhibiting Xenopus and human RXRα in Cos7 cells with IC50 values of 0.22 μM and 0.24 μM, respectively.

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Oxybenzone

T0499131-57-7

Oxybenzone is a UV filter commonly used in tanning and skin protection agents. It is a derivative of benzophenone and is used as an endocrine disrupting chemical that penetrates the placental and blood-brain barriers. It impairs autophagy, alters epigenetic status and disrupts vitamin X-like receptor signaling in apoptotic neuronal cells.

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1,3,5-Triisopropylbenzene

T67074717-74-8

1,3,5-Triisopropylbenzene is a benzene ring derivative commonly used in fuels, lubricants, and micellar expanders, and can be used as a potential retinoid X nuclear receptor alpha (RXRα) agonist (Activity Value=15µM).

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Tarenflurbil

T584351543-40-9

Tarenflurbil ((R)-Flurbiprofen) is the non-cyclooxygenase inhibiting R-enantiomer of the NSAID flurbiprofen, evaluated as a treatment for Alzheimer's disease.

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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)

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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.

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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.

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LG100268

T19703153559-76-3

LG100268 is a potent, selective, and orally active retinoid X receptor (RXR) agonist that agonizes RXR-α, RXR-β, and RXR-γ at the nanomolar level, selectively exceeding the RAR by three orders of magnitude.LG100268 is capable of inducing transcriptional activation in adipocytes; affecting the RXRs and their chaperone receptor, Foxl2 Dmrt1, to induce flounder masculinization in juvenile flounder; inhibits keratin 17 expression in nigrostriatal epithelial cells; and increases PD-L1 expression in HER2 or triple-negative breast cancer.

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Mofarotene

T68104125533-88-2In house

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.

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