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

Cytochrome P450

CYPs

Cytochrome P450

Related Products

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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.

Cytochrome P450 Isoform Specific Products:

Cytochrome P450 Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-N2259
    Curcumenol
    		Inhibitor 99.98%
    Curcumenol ((+)-Curcumenol) is a potent CYP3A4 inhibitor with an IC50 of 12.6 μM, which is one of constituents in the plants of medicinally important genus of Curcuma zedoaria, with neuroprotection, anti-inflammatory, anti-tumor and hepatoprotective activities. Curcumenol ((+)-Curcumenol) suppresses Akt-mediated NF-κB activation and p38 MAPK signaling pathway in LPS-stimulated BV-2 microglial cells.
    Curcumenol
  • HY-W008364
    Olivetol
    		Inhibitor 99.81%
    Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoid receptors CB1 and CB2. Olivetol also inhibits CYP2C19 and CYP2D6 activity, with IC50s of 15.3 μM, 7.21 μM and Kis of 2.71 μM, 2.87 μM, respectively.
    Olivetol
  • HY-18719E
    Endoxifen
    		Inhibitor 99.51%
    Endoxifen is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen has the potential for breast cancer study.
    Endoxifen
  • HY-N0692
    Schisandrol B
    		Inhibitor 99.92%
    Schisandrol B (Gomisin-A) is a major active constituent of Schisandra chinensis with hepato-protective effects. Schisandrol B inhibits reactive oxygen species (ROS) production. Schisandrol B inhibits the activity of P-glycoprotein and CYP3A and also has anti-inflammatory, anti-diabetic and antioxidant activities.
    Schisandrol B
  • HY-21065
    Tienilic acid
    		99.69%
    Tienilic acid (Ticrynafen; ANP 3624) acts as a diuretic hypotensive agent. However, Tienilic acid induces hepatotoxicity. Tienilic acid is converted into electrophilic metabolites by cytochrome P450 (CYP) in vitro.
    Tienilic acid
  • HY-139109
    IR-783
    		99.87%
    IR-783 (ADS 780WS) is a heptamethine cyanine dye. IR-783 induces Mitochondrial membrane potential loss, ATP depletion, mitochondrial permeability transition pore opening, Cytochrome c release and Apoptosis in breast cancer cells. IR-783 promotes the translocation of Drp1 from the cytosol to mitochondria. IR-783 increases the expression of mitochondrial fission proteins such as MFF and Fission-1. IR-783 possesses imaging, cancer-targeting and anticancer properties. IR-783 exerts anticancer effects against breast cancer. IR-783 can be used in breast cancer-related research.
    IR-783
  • HY-111052
    AZD7325
    		Activator 99.95%
    AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes. AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro. AZD7325 has the potential for the investigation of anxiety and dravet syndrome. PAM: positive allosteric modulator.
    AZD7325
  • HY-B0725
    Doxepin Hydrochloride
    		Inhibitor 99.64%
    Doxepin hydrochloride is an orally active tricyclic antidepressant agent. Doxepin hydrochloride is a potent and selective histamine receptor H1 antagonist. Doxepin hydrochloride is also a potent CYP450 inhibitor and significantly inhibits CYP450 2C19 and 1A2. Doxepin inhibits reuptake of serotonin and norepinephrine as a tricyclic antidepressant.
    . Doxepin has therapeutic effects in atopic dermatitis，chronic urticarial，can improve cognitive processes， protect central nervous system.
    . Doxepin has also been proposed as a protective factor against oxidative stress.
    .
    Doxepin Hydrochloride
  • HY-14874
    Topiroxostat
    		Inhibitor 99.06%
    Topiroxostat (FYX-051) is a potent and orally active xanthine oxidoreductase (XOR) inhibitor with an IC50 value of 5.3 nM and a Ki value of 5.7 nM. Topiroxostat exhibits weak CYP3A4-inhibitory activity (18.6%). Topiroxostat has the potential for hyperuricemia treatment.
    Topiroxostat
  • HY-W013268
    (S)-(+)-N-3-Benzylnirvanol
    		Inhibitor 99.76%
    (S)-(+)-N-3-Benzylnirvanol ((+)-N-3-Benzylnirvanol) is a selective and competitive cytochrome P450 (CYP) isoform CYP2C19 inhibitor with a Ki of 250 nM. (S)-(+)-N-3-Benzylnirvanol has low activity against CYP1A2, CYP2A6, CYP2C8, CYP2C9, CYP2D6, CYP2E1, and CYP3A4.
    (S)-(+)-N-3-Benzylnirvanol
  • HY-17643
    Oteseconazole
    		Inhibitor 99.81%
    Oteseconazole (VT-1161) is a potent and orally active anti-fungal agent. Oteseconazole potently binds to and inhibits Candida albicans cytochrome P45051 (CYP51) activity (Kd ≤39 nM), shows no obvious effect on human CYP51. Oteseconazole also can be used for the research of dermatophytes.
    Oteseconazole
  • HY-109123
    Soticlestat
    		Inhibitor 99.83%
    Soticlestat (TAK-935; OV935) is a first-in-class, potent, selective, and orally active cholesterol 24-hydroxylase (CH24H) inhibitor. Soticlestat has the potential for epilepsy syndromes research.
    Soticlestat
  • HY-A0016
    Dronedarone
    		Inhibitor 99.93%
    Dronedarone (SR 33589), a derivative of amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone is a substrate for and a moderate inhibitor of CYP3A4.
    Dronedarone
  • HY-N0762
    Isobavachin
    		Inhibitor 99.88%
    Isobavachin is an orally active, blood-brain barrier-penetrating prenylated flavonoid present in Psoralea corylifolia. Isobavachin inhibits human CYP2B6, CYP2C9, CYP2C19, UGT1A1, UGT1A9, and UGT2B7. Isobavachin suppresses MAPK activation, NF-κB nuclear translocation, overexpression of iNOS/COX-2, FcεRI-mediated signaling pathways, and RANKL-induced osteoclastogenesis. Isobavachin induces autophagy, cytotoxicity, neuronal differentiation, and NRF2 activation; it alleviates oxidative damage, inflammatory responses, apoptosis, iron accumulation, mitochondrial biogenesis, and mast cell degranulation. Isobavachin is applicable to research related to liver injury, inflammatory diseases, osteoporosis, liver cancer, prostate cancer, glioma, periodontitis-induced bone loss, and Alzheimer's disease.
    Isobavachin
  • HY-A0087
    Octocrylene
    		Activator 98.68%
    Octocrylene is an organic ultraviolet (UV) filter that absorbs mainly UVB radiation and shorter UVA wavelengths. Octocrylene acts as a partial agonist of PPARγ, which alters the gene transcription profile of lipid metabolism enzymes. In addition, Octocrylene is cytotoxic and genotoxic to human skin fibroblasts and mediates the biosynthesis of estrogens such as estriol in zebrafish larvae, while affecting antioxidant pathways including glutathione transferase and peroxisomes.
    Octocrylene
  • HY-18642
    CYP3cide
    		Inhibitor 99.92%
    CYP3cide (PF-4981517) is a potent, selective and time-dependent inhibitor of cytochrome P4503A4 (CYP3A4). The IC50 values for Midazolam 1’-hydroxylase activity are 0.03 μM, 17 μM, and 71 μM for CYP3A4, CYP3A5, and CYP3A7, respectively. CYP3cide can be used to distinguish the contributions of CYP3A4 versus CYP3A5 on agent metabolism.
    CYP3cide
  • HY-B0105B
    Levoketoconazole
    		Inhibitor 99.39%
    Levoketoconazole ((-)-Ketoconazole) is the 2S,4R enantiomer derived from racemic Ketoconazole (HY-B0105). Levoketoconazole is a potent and orally active cortisol synthesis inhibitor. Levoketoconazole inhibits key steps in cortisol and testosterone synthesis by inhibiting CYP11B1, CYP11A1, and CYP17A1. Levoketoconazole can be used for research on endogenous Cushing’s syndrome.
    Levoketoconazole
  • HY-N5011
    5,7-Dimethoxyflavone
    		Inhibitor 99.86%
    5,7-Dimethoxyflavone is one of the major components of Kaempferia parviflora, has anti-obesity, anti-inflammatory, and antineoplastic effects. 5,7-Dimethoxyflavone inhibits cytochrome P450 (CYP) 3As. 5,7-Dimethoxyflavone is also a potent Breast Cancer Resistance Protein (BCRP) inhibitor.
    5,7-Dimethoxyflavone
  • HY-B1311
    Proadifen hydrochloride
    		Inhibitor 99.95%
    Proadifen (SKF-525A) hydrochloride is a non-competitive Cytochrome P450 inhibitor with an IC50 value of 19 μM. Proadifen hydrochloride reduces monoamine oxidase A (MAO-A) activity and reverses the antidepressantlike behavioral effect of Imipramine (HY-B1490A) and Desipramine (HY-B1272A) in rats. Proadifen hydrochloride also reduces N, N-dimethyltryptamine (DMT) metabolism in liver microsomes and inhibits N-demethylationand Acridone (HY-W007771) formation. Proadifen hydrochloride augments Lipopolysaccharide (LPS) (HY-D1056)-induced fever and exacerbates Prostaglandin E2 (PGE2) (HY-101952) levels in the rat. Proadifen hydrochloride is promising for research of metabolism-related deseases, ovarian carcinoma, inflammation and dopamine neurons-related deseases.
    Proadifen hydrochloride
  • HY-N2229
    Rhapontigenin
    		Inhibitor 99.66%
    Rhapontigenin is a natural analog of resveratrol with anticancer, antioxidant, antifungal and antibacterial activities. Rhapontigenin is amechanism-based, potent and selective cytochrome P450 1A1 inactivator (IC50  = 400 nM). Rhapontigenin exhibits 400-fold and 23-fold selectivity for P450 1A1 over P450 1A2 and P450 1B1, respectively.
    Rhapontigenin
Cat. No. Product Name / Synonyms Application Reactivity
Cytochrome P450 Isoform Comparison

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