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Metabolism

Acetyl-CoA Carboxylase

Amino Acids and Derivatives

Angiotensin-converting Enzyme (ACE)

Endogenous Metabolite

Glutathione Peroxidase

(43)

Glyoxalase

(2)

HIF/HIF Prolyl-Hydroxylase

Indoleamine 2,3-Dioxygenase (IDO)

(36)

Isocitrate Dehydrogenase (IDH)

Mitochondrial Metabolism

(102)

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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