2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Cytochrome P450
  5. CYP26 Isoform

CYP26

CYP26 enzymes are cytochrome P450 retinoic acid hydroxylases that regulate intracellular all-trans-retinoic acid (atRA) concentrations and maintain retinoid homeostasis through rapid metabolic clearance of active retinoids[1][2]. The CYP26 family comprises CYP26A1, CYP26B1, and CYP26C1, which efficiently metabolize atRA and related retinoid isomers, thereby controlling retinoic acid receptor signaling during development and in adult tissues[2][3]. Mechanistically, CYP26-mediated catabolism generates retinoic acid gradients that shape tissue-specific gene expression patterns and protect selected tissues from excessive retinoid signaling during embryogenesis[4][5]. Disruption of CYP26-dependent retinoic acid homeostasis has been linked to developmental abnormalities, altered neuronal retinoid signaling, and pathological changes associated with cancer and other retinoid-responsive diseases[5][6][7]. Compared with related isoforms, CYP26A1 is the predominant hepatic atRA hydroxylase with higher catalytic capacity, whereas CYP26B1 exhibits higher substrate affinity and primarily regulates extrahepatic retinoid clearance[8][9][10]. CYP26C1 also contributes to retinoid metabolism but remains less extensively characterized than CYP26A1 and CYP26B1[2][3]. For experimental applications, selective and dual CYP26 inhibitors, including retinoic acid metabolism blocking agents (RAMBAs) such as talarozole and DX314, increase endogenous atRA exposure and are widely used to investigate tissue-specific retinoid signaling and therapeutic responses in dermatological and cancer-related models[11][12][13].

References:

CYP26 Related Products (6):

Cat. No. Product Name Effect Purity
  • HY-14531
    Talarozole
    		Inhibitor 99.75%
    Talarozole (R115866) is an oral systemic all-trans retinoic acid metabolism blocking agent (RAMBA) which increases intracellular levels of endogenous all-trans retinoic acid (RA). Talarozole inhibits both CYP26A1 and CYP26B1 with IC50s of 5.4 and 0.46 nM, respectively.
  • HY-106019
    Liarozole
    		Inhibitor 98.96%
    Liarozole (R75251; R85246) is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of retinoic acid (IC50=7 μM), resulting in increased tissue levels of retinoic acid. Liarozole shows antitumoral properties.
  • HY-135560
    Nicotelline
    		Inhibitor 98.88%
    Nicotelline (Nicotellin) is a nicotine-related alkaloid, as well as a weak inhibitor of human cDNA-expressed cytochrome P-450 2A6 (CYP2A6). CYP2A6 mediates coumarin 7-hydroxylation, while Nicotelline fails to exhibit inhibition at 300 μM. Nicotelline can be used as a tracer and biomarker of particulate matter (PM) derived from tobacco smoke.
  • HY-106019C
    Liarozole dihydrochloride
    		Inhibitor 99.04%
    Liarozole (R75251) dihydrochloride is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole dihydrochloride inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of RA (IC50=7 μM), resulting in increased tissue levels of RA. Liarozole dihydrochloride shows antitumoral properties.
  • HY-16719
    Dapaconazole
    		Inhibitor 99.76%
    Dapaconazole, as an antifungal agent, inhibits sterol 14α-demethylase cytochrome P450 activity with an IC50 of 1.4 μM.
  • HY-121500
    R-116010
    		Inhibitor
    R-116010 is a potent and selective retinoic acid (RA) metabolism inhibitor and can inhibit hydroxylase CYP26. R-116010 can enhance the anti-tumor effect of retinoic acid drugs. R-116010 can be used for the research of cancer, metabolic and neurological disease, such as neuroblastoma.