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-N8405
    Isolimonexic acid
    Inhibitor
    Isolimonexic acid is a limonoid isolated from lemon (Citrus lemon L. Burm) seed, has anti-cancer and anti-aromatase (IC50=25.60 μM) properties.
    Isolimonexic acid
  • HY-164510
    N-Formyldemecolcine
    N-Formyldemecolcine is a colchicine precursor that contains the characteristic tropolone ring and pharmacophore of colchicine. N-Formyldemecolcine can be synthesized de novo by genetically engineering transgenic Nicotiana benthamiana and atypical cytochrome P450s that catalyze the production of colchicine's unique carbon scaffold.
    N-Formyldemecolcine
  • HY-13834
    GW844520
    Inhibitor
    GW844520 is an orally active inhibitor of cytochrome bc1 complex. GW844520 can be used in malaria and anti-plasmodium related research.
    GW844520
  • HY-B2169R
    Melperone (Standard)
    Inhibitor
    Melperone (Standard) is the analytical standard of Melperone (HY-B2169). This product is intended for research and analytical applications. Melperone is a butyrophenone with atypical antipsychotic properties. Melperone is a multireceptor antagonist with Kds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with Kd values ​​of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone is also a CYP2D6 inhibitor. Melperone can be used for the study of schizophrenia, and agitation in the elderly.
    Melperone (Standard)
  • HY-W010195R
    2,6-Dimethylquinoline (Standard)
    Inhibitor
    2,6-Dimethylquinoline, a nature constituent from the roots of Peucedantu praeruptorum, is a CYP1A2 inhibitor with an IC50 of 3.3 µM. 2,6-Dimethylquinoline also inhibits CYP2B6 activity with an IC50 of 480 µM.
    2,6-Dimethylquinoline (Standard)
  • HY-B2169S2
    Melperone-d4 hydrochloride
    Inhibitor 99.84%
    Melperone-d4 hydrochloride is the deuterium labeled Melperone hydrochloride (HY-103109). Melperone hydrochloride is a butyrophenone with atypical antipsychotic properties. Melperone hydrochloride is a multireceptor antagonist with Kds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone hydrochloride has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with Kd values ​​of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone hydrochloride is also a CYP2D6 inhibitor. Melperone hydrochloride can be used for the study of schizophrenia, and agitation in the elderly.
    Melperone-d<sub>4</sub> hydrochloride
  • HY-B0035B
    Sulfamethazine 100 µg/mL in acetonitrile
    Activator
    Sulfamethazine 100 μg/mL in acetonitrile (Sulfadimidine 100 μg/mL in acetonitrile) is an antimicrobial agent that induces CYP3A4 expression and is acetylated by N-acetyltransferase. It exhibits sex-dependent pharmacokinetics and is metabolized by CYP2C11 in males.
    Sulfamethazine 100 µg/mL in acetonitrile
  • HY-W327449R
    Feruloylputrescine (Standard)
    Inhibitor
    Feruloylputrescine is an oral active phenolamide found in citrus plants and formed through the decarboxylation of L-Arginine. Feruloylputrescine inhibits monooxygenase (cntA) and reductase (cntB) and trimethylamine production. Feruloylputrescine can be used for cardiovascular diseases research.
    Feruloylputrescine (Standard)
  • HY-B0852S2
    Tebuconazole-d6
    Tebuconazole-d6 is a deuterium labeled Tebuconazole (HY-B0852). Tebuconazole is an orally active agricultural azole fungicide which can also inhibit CYP51 with IC50s of 0.9 and 1.3 μM for Candida albicans CYP51 (CaCYP51) and truncated Homo sapiens CYP51 (Δ60HsCYP51), respectively. Tebuconazole induces lipid accumulation and oxidative stress in HepG2 Cells. Tebuconazole decreases MAC-T cells viability and proliferation, induces ER-stress-mediated apoptosis and increases oxidative stress levels in MAC-T cells.
    Tebuconazole-d<sub>6</sub>
  • HY-174417
    NNRT-IN-10
    Inhibitor
    NNRT-IN-10 is a potent, selective and orally active non-nucleoside HIV-1 reverse transcriptase (NNRTI) inhibitor with with an EC50 values ranging from 1.16 to 18.3 nM for HIV and its mutant strains. NNRT-IN-10 exhibits good pharmacokinetic properties and favorable safety profiles. NNRT-IN-10 can be used for the study of AIDS, caused by HIV-1.
    NNRT-IN-10
  • HY-126308
    (E/Z)-DMU2139
    Inhibitor
    (E/Z)-DMU2139 (Compound 180) is the E/Z isomer of DMU2139 (HY-101285). (E/Z)-DMU2139 is a potent and specific CYP1B1 inhibitor (IC50: 4 nM).
    (E/Z)-DMU2139
  • HY-128706
    (+)-Menthofuran
    Inhibitor
    (+)-Menthofuran (compound 1) is a furan terpenoid that can be found in mint oils.
    (+)-Menthofuran
  • HY-W008364R
    Olivetol (Standard)
    Inhibitor
    Olivetol (Standard) is the analytical standard of Olivetol. This product is intended for research and analytical applications. 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 (Standard)
  • HY-157170
    CYP450-IN-1
    Inhibitor
    CYP450-IN-1 (compound 2e) is a potent inhibitor of CYP450.
    CYP450-IN-1
  • HY-14247R
    Fadrozole hydrochloride (Standard)
    Inhibitor
    Fadrozole (hydrochloride) (Standard) is the analytical standard of Fadrozole (hydrochloride). This product is intended for research and analytical applications. Fadrozole hydrochloride (CGS 16949A) is a potent, selective and nonsteroidal inhibitor of aromatase with an IC50 of 6.4 nM.
    Fadrozole hydrochloride (Standard)
  • HY-178162
    CYP51-IN-27
    Inhibitor
    CYP51-IN-27 is a sterol 14α-demethylase CYP51 inhibitor with an IC50 of 0.3434 μg/mL. CYP51-IN-27 exhibits antifungal activity and inhibits the production of fungal ergosterol. CYP51-IN-27 can be used for the research of infection, such as rice sheath blight.
    CYP51-IN-27
  • HY-N1431A
    Tabersonine hydrochloride
    Activator
    Tabersonine hydrochloride is a selective, orally active NLRP3 inhibitor. Tabersonine hydrochloride directly binds to the NACHT domain of NLRP3, inhibiting its ATPase activity and oligomerization, thereby blocking ASC spot formation and caspase-1 activation, and reducing the release of pro-inflammatory cytokines such as IL-1β. Tabersonine hydrochloride also inhibits K63-linked ubiquitination of TRAF6, blocking NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. Tabersonine hydrochloride can inhibit inflammatory responses, induce apoptosis of liver cancer cells through mitochondrial pathways and death receptor pathways, reduce mitochondrial membrane potential, promote cytochrome c release, and activate caspase proteins. Tabersonine hydrochloride is mainly used in the study of NLRP3-driven inflammatory diseases (such as acute lung injury, sepsis, peritonitis) and tumors such as liver cancer.
    Tabersonine hydrochloride
  • HY-15565R
    APD668 (Standard)
    Inhibitor
    APD668 (Standard) is the analytical standard of APD668. This product is intended for research and analytical applications. APD668 is a potent, selective and orally active agonist of G-protein coupled receptor GPR119, with EC50s of 2.7 nM and 33 nM for hGPR119 and rGPR119, respectively. APD668 shows no significant inhibition of any of the five major CYP isoforms with the exception of CYP2C9 (Ki=0.1 μM). APD668 can be used for the research of steatohepatitis and diabetes.
    APD668 (Standard)
  • HY-13832R
    Atovaquone (Standard)
    Inhibitor
    Atovaquone (Standard) is the analytical standard of Atovaquone. This product is intended for research and analytical applications. Atovaquone (Atavaquone) is a potent, selective and orally active inhibitor of the parasite’s mitochondrial cytochrome bc1 complex. Atovaquone is against human and  P. falciparum cytochrome bc1 activity with IC50 values of 460 nM and 2.0 nM, respectively. Atovaquone is an antimalarial agent and has the potential for the investigation of neumocystis pneumonia, toxoplasmosis, malaria, and babesia.
    Atovaquone (Standard)
  • HY-B1234S
    Octinoxate-13C,d3
    Inhibitor
    Octinoxate-13C,d3 is the deuterium labeled Octinoxate (HY-W245806). Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to type II deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibits CYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an anti-estrogenic and anti-androgenic effect in vitro and in vivo.
    Octinoxate-<sup>13</sup>C,d<sub>3</sub>
Cat. No. Product Name / Synonyms Application Reactivity

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