1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. Cytochrome P450

Cytochrome P450

CYPs

Cytochrome p450 comprises a superfamily of heme-thiolate proteins named for the spectral absorbance peak of their carbon-monoxide-bound species at 450 nm. Having been found in every class of organism, including Archaea, the p450 superfamily is believed to have originated from an ancestral gene that existed over 3 billion years ago. Repeated gene duplications have subsequently given rise to one of the largest of multigene families. These enzymes are notable both for the diversity of reactions that they catalyze and the range of chemically dissimilar substrates upon which they act. Cytochrome p450s support the oxidative, peroxidative and reductive metabolism of such endogenous and xenobiotic substrates as environmental pollutants, agrochemicals, plant allelochemicals, steroids, prostaglandins and fatty acids. In humans, Cytochrome p450s are best known for their central role in phase I drug metabolism where they are of critical importance to two of the most significant problems in clinical pharmacology: drug interactions and interindividual variability in drug metabolism.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-B0105A
    (+)-Ketoconazole
    Inhibitor 99.79%
    (+)-Ketoconazole ((+)-R 41400) is an imidazole anti-fungal agent, a CYP3A4 inhibitor.
    (+)-Ketoconazole
  • HY-W014701
    1,4-Dihydroxy-2-naphthoic acid
    Agonist 99.60%
    1,4-Dihydroxy-2-naphthoic acid is an aryl hydrocarbon receptor (AhR) agonist. 1,4-Dihydroxy-2-naphthoic acid is also a bacterially derived metabolite and has anti-inflammatory activity.
    1,4-Dihydroxy-2-naphthoic acid
  • HY-113062
    20α-Dihydroprogesterone
    Inhibitor
    20α-Dihydroprogesterone is the metabolite of Progesterone (HY-N0437). 20α-Dihydroprogesterone inhibits cell proliferation and migration in breast tissue. 20α-Dihydroprogesterone inhibits aromatase in cell MCF-7aro with IC50 about 5 μM.
    20α-Dihydroprogesterone
  • HY-141860
    PSMA-Val-Cit-PAB-MMAE
    Inhibitor 99.52%
    PSMA-Val-Cit-PAB-MMAE is a small-molecule conjugate targeting PSMA, with Monomethyl auristatin E (MMAE) (HY-15162) as its cytotoxic payload. PSMA-Val-Cit-PAB-MMAE binds to PSMA, thereby being delivered into PSMA-expressing prostate cancer cells. Subsequently, the Val-Cit linker is cleaved under the mediation of cathepsin B, releasing active MMAE. PSMA-Val-Cit-PAB-MMAE inhibits CYP3A4 activity (IC50 = 11.2 μM), induces intracellular ROS production and oxidative stress, disrupts the cytoskeleton through microtubule destabilization, and induces prostate cancer cell death. PSMA-Val-Cit-PAB-MMAE can be used in research related to prostate cancer.
    PSMA-Val-Cit-PAB-MMAE
  • HY-N0688
    Linderane
    Inhibitor 98.61%
    Linderane, isolated from the root of Lindera aggregata, is an irreversible inhibitor cytochrome P450 2C9 (CYP2C9). Linderane has the potential to relieve pain and cramp.
    Linderane
  • HY-125904
    4-Hydroxyretinoic acid
    4-Hydroxyretinoic acid (4-HRA) is a derivative of Retinoic acid (HY-14649). 4-Hydroxyretinoic acid is formed via the catalysis of retinol by cytochrome P-450 isoenzymes. 4-Hydroxyretinoic acid also serves as a substrate for UDP-glucuronosyltransferase (s) and recombinant UGT2B7. 4-Hydroxyretinoic acid binds to the nuclear receptor RAR (Retinoic Acid Receptor), activates RAR and RXR-alpha, subsequently regulates gene expression and cell differentiation, and induces cancer cell apoptosis (Apoptosis). 4-Hydroxyretinoic acid also participates in multiple physiological processes such as immunoregulation, neuroprotection and antioxidation.
    4-Hydroxyretinoic acid
  • HY-109619
    D4-abiraterone
    Inhibitor 99.85%
    D4-abiraterone is a major metabolite of abiraterone. D4-abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid-5a-reductase (SRD5A) and also an antagonist of androgen receptor.
    D4-abiraterone
  • HY-116214
    Cyprodinil
    Inducer 98.84%
    Cyprodinil (CGA-219417) is a broad-spectrum anilinopyrimidine fungicide and an activator of the aryl hydrocarbon receptor. Cyprodinil also has anti-androgenic and androgenic activities. Cyprodinil can inhibit the biosynthesis of methionine in plant-pathogenic fungi and protect fruits and vegetables from a variety of pathogens.
    Cyprodinil
  • HY-D0932
    Sudan IV
    Activator 98.0%
    Sudan IV is an agonist of the aryl hydrocarbon receptor (AhR) that activates downstream signaling pathways and induces CYP1A1 expression. Sudan IV promotes CYP1A1 gene transcription by activating AhR-ARNT heterodimers and binding to exogenous response elements (XREs) on DNA, thereby enhancing drug metabolizing enzyme activity. Sudan IV can be used to study the toxicity mechanisms of industrial dyes and the effects of interactions with serum proteins (such as bovine serum albumin (BSA)) on their distribution in vivo. Sudan IV is a fat-soluble diazo dye that can be used to stain lipids, triglycerides, and lipoproteins on frozen sections.
    Sudan IV
  • HY-N0918
    Desmethoxyyangonin
    Inducer 99.00%
    Desmethoxyyangonin is one of the six major kavalactones found in the Piper methysticum (kava) plant. Desmethoxyyangonin is a selective inhibitor of monoamine oxidase-B (MAO-B) (IC50: 0.123  µM). Desmethoxyyangonin exerts anti-inflammatory effects by inhibiting Jak2/STAT3 and IKK signaling pathways. Desmethoxyyangonin induces CYP3A23 expression and leads to skeletal muscle relaxation.
    Desmethoxyyangonin
  • HY-B1462R
    Chlorzoxazone (Standard)
    Modulator
    Chlorzoxazone (Standard) is the analytical standard of Chlorzoxazone. This product is intended for research and analytical applications.
    Chlorzoxazone (Standard)
  • HY-116568
    Prothioconazole
    Inhibitor 99.52%
    Prothioconazole is an orally active broad-spectrum fungicide. Prothioconazole weakly inhibits CaCYP51 activity in Candida albicans, with an apparent IC50 of approximately 120 μM. Prothioconazole disrupts Microtubule stability by reducing the acetylation level of α-tubulin. Prothioconazole induces Mitochondrial dysfunction, oxidative stress, DNA damage, and Apoptosis. Prothioconazole accumulates 14-methylated sterols and depletes ergosterol in cells, culture media, plants, and animals. Prothioconazole interferes with pyruvate metabolism and glycolysis/gluconeogenesis processes in mouse liver, downregulates Fasn mRNA expression, and induces hepatotoxicity and renal metabolic disorders. Prothioconazole reduces the fertility of female mice. Prothioconazole inhibits body weight gain and increases liver/kidney indices in mice. Prothioconazole can be used in studies related to candidiasis.
    Prothioconazole
  • HY-W040468
    2-Phenyl-2-(1-piperidinyl)propane
    Inhibitor 99.72%
    2-Phenyl-2-(1-piperidinyl)propane is a selective and reversible human CYP2B6 inhibitor with an IC50 of 5.1 μM and a Ki of 5.6. 2-Phenyl-2-(1-piperidinyl)propane inhibits CYP2D6 (IC50=74 μM), CYP3A (IC50=200 μM).
    2-Phenyl-2-(1-piperidinyl)propane
  • HY-W027773
    7-Methoxy-4-(trifluoromethyl)coumarin
    98.0%
    7-Methoxy-4-(trifluoromethyl)coumarin (MFC) is a fluorescent substrate for cytochrome P450 and can quantify CYP activity.
    7-Methoxy-4-(trifluoromethyl)coumarin
  • HY-17614
    Ezutromid
    98.87%
    Ezutromid (SMT C1100) is a first-in-class, orally active benzoxazole utrophin modulator with an EC50 of 0.91 μM. Ezutromid can be used for the research Duchenne muscular dystrophy (DMD). Ezutromid inhibits CYP1A2 enzymic activity in human liver microsomes (HLM) with an IC50 of 5.4 μM.
    Ezutromid
  • HY-101285
    DMU2139
    Inhibitor 98.0%
    DMU2139 is a potent and specific CYP1B1 inhibitor, with IC50s of 9 nM and 795 nM for CYP1B1 and CYP1A1, respectively.
    DMU2139
  • HY-134988
    EDP-305
    Inhibitor
    EDP-305 is an orally active, potent and selective farnesoid X receptor (FXR) agonist, with EC50 values of 34 nM (chimeric FXR in CHO cells) and 8 nM (full-length FXR in HEK cells). EDP-305 shows a potent and consistent antifibrotic effect. EDP-305 can be used for primary biliary cholangitis (PBC) and non-alcoholic steatohepatitis (NASH) research.
    EDP-305
  • HY-14405A
    Casopitant mesylate
    Inhibitor 99.83%
    Casopitant mesylate (GW679769B) is a potent, selective, brain permeable and orally active neurokinin 1 (NK1) receptor antagonist. Casopitant mesylate is a second in the class of antiemetics that acts to antagonise the emetogenic effect of Substance P (HY-P0201). Casopitant mesylate is also a substrate and a weak-to-moderate inhibitor of CYP3A4. Casopitant mesylate can be used for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV).
    Casopitant mesylate
  • HY-D0055
    3-Cyano-7-ethoxycoumarin
    98.0%
    3-Cyano-7-ethoxycoumarin is a fluorescent cytochrome P-450 substrate that generates a blue fluorescent product upon enzymatic cleavage. 3-Cyano-7-ethoxycoumarin is used to detect the activity of mixed-function oxidases in isolated rat hepatocytes. 3-Cyano-7-ethoxycoumarin serves as a biological dye and indicator for research.
    3-Cyano-7-ethoxycoumarin
  • HY-B1042
    Oxolamine citrate
    Inhibitor 99.87%
    Oxolamine citrate (SKF-9976 citrate) is an orally active antitussive. Oxolamine citrate can inhibit CYP2B1/2. Oxolamine citrate has anti-inflammatory effects on the respiratory organs of guinea pigs. Oxolamine citrate increases the AUC of Warfarin (HY-B0687) and prolongs its terminal half-life. Oxolamine citrate can be used in respiratory disease research.
    Oxolamine citrate
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