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-164793
    TGFBR1-IN-2
    Modulator
    TGFBR1-IN-2 (Compound AQA) is a TGFBR1 inhibitor and an antibacterial agent. TGFBR1-IN-2 is a substrate for cytochrome P450s. TGFBR1-IN-2 contains the pyridyl-6-methyl moiety necessary for Mycobacterium tuberculosis inhibition and has potent inhibitory activity against non-replicating and persistent Mycobacterium tuberculosis.
    TGFBR1-IN-2
  • HY-B0189
    Mosapride
    Inducer 99.87%
    Mosapride is an orally active gastroenterokinetic compound. Mosapride is a 5HT4 agonist. Mosapride is a CYP inducer. Mosapride has a concentration-dependent inhibitory effect on Kv4.3, and its IC50 value is 15.2 μM. Mosapride can be used in the study of gastrointestinal diseases.
    Mosapride
  • HY-N4089
    Quercetin 3-gentiobioside
    Inhibitor 99.56%
    Quercetin 3-gentiobioside is a flavonoid found in Artemisia iwayomogi. Quercetin 3-gentiobioside inhibits aromatase with an Ki of 46.77 nM. Quercetin 3-gentiobioside inhibits aldose reductase (AR) and the formation of advanced glycation end products (AGEs), with IC50 values of 10.60 μM and 109.46 μM, respectively. Quercetin 3-gentiobioside inhibits proliferation of cancer cells and fibroblast-like synoviocytes. Quercetin 3-gentiobioside can be used for the research of cancer, such as lung carcinoma.
    Quercetin 3-gentiobioside
  • HY-N0926A
    Columbamine chloride
    Inhibitor 99.62%
    Columbamine (Columbamin; Dehydroisocorypalmine) chloride is an organic heterotetracyclic alkaloid extracted from plants. Columbamine chloride is a metabolite of Berberine (HY-N0716). Columbamine chloride inhibits the cytochrome P450 (CYP) isoform CYP3A4 (IC50 = 30.6 µM). Columbamine chloride induces apoptosis in cancer cells. Columbamine chloride can be used for antioxidant, anti-inflammatory, antitumor, antifungal, antiparasite, hepatoprotective, neuroprotective, hypolipidemic and hypoglycemic study.
    Columbamine chloride
  • HY-N7005
    Clitorin
    Inhibitor 99.45%
    Clitorin is an orally active flavonoid compound that can be isolated from Carica papaya. Clitorin is an inhibitor of EGFR (IC50: 89.58 nM) and aromatase (IC50: 77.41 nM). Clitorin has antioxidant and anti-tumor activities. In the DPPH and ABTS radical scavenging assays, Clitorin has IC50 values of 91.96 ppm and 250.45 ppm, respectively. In addition, Clitorin can regulate lipogenesis and fatty acid oxidation and can be used in the research of non-alcoholic fatty liver disease.
    Clitorin
  • HY-18719B
    Endoxifen hydrochloride
    Inhibitor 98.04%
    Endoxifen hydrochloride is a key active metabolite of Tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen hydrochloride has the potential for breast cancer study.
    Endoxifen hydrochloride
  • HY-B0189B
    Mosapride citrate dihydrate
    Inducer 99.59%
    Mosapride (TAK-370) citrate dehydrate is a gastroprokinetic agent with 5-hydroxytryptamine4 receptor agonist activity and has been widely used in the research of a variety of gastrointestinal disorders. Mosapride citrate dihydrate potently inhibits Kv4.3 in a concentration-dependent manner with IC50 values of 15.2 μM. Mosapride citrate dihydrateselectively stimulates upper GI motility in vivo.
    Mosapride citrate dihydrate
  • HY-N2420
    Flavokawain A
    Inhibitor 99.73%
    Flavokawain A is a chalcone compound and an orally active inhibitor of PRMT5 and cytochrome P450. Flavokawain A has anti-inflammatory, anti-tumor, and immunomodulatory effects. Flavokawain A can inhibit the proliferation of tumor cells and induce apoptosis. Flavokawain A can be used in the research of diseases such as bladder cancer.
    Flavokawain A
  • HY-N1431
    Tabersonine
    Activator 98.13%
    Tabersonine is a selective, orally active NLRP3 inhibitor. Tabersonine 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 also inhibits K63-linked ubiquitination of TRAF6, blocking NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. Tabersonine 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 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
  • HY-N4205
    Tetrahydropiperine
    Inhibitor 99.41%
    Tetrahydropiperine is an orally effective, selective inhibitor of NF-κB and MAPKs<、b>, and an activator of the PI3K/Akt/mTOR<、b> pathway. Tetrahydropiperine reduces the production of pro-inflammatory cytokines such as TNF-α, IL-6, and nitric oxide (NO) by inhibiting the nuclear translocation of NF-κB and the phosphorylation of MAPKs such as ERK, JNK, and p38. At the same time, Tetrahydropiperine inhibits excessive autophagy by activating the PI3K/Akt/mTOR pathway, protecting neurons from oxidative damage. Tetrahydropiperine has anti-inflammatory, anti-apoptotic, and neuroprotective effects, and is mainly used in the study of inflammatory diseases (such as endotoxemia, arthritis) and neurological diseases such as ischemic stroke.
    Tetrahydropiperine
  • HY-150084
    (±)14,15-Epoxyeicosatrienoic acid
    99.9%
    (±)14,15-Epoxyeicosatrienoic acid ((±)14(15)-EET) is the Cytochrome P450 metabolite of arachidonic acid. While CYP3A4 may be involved in breast cancer cell growth, (±)14,15-Epoxyeicosatrienoic acid may promote mitosis and anchorage-dependent cloning through STAT3 affected by CYP3A4. (±)14,15-Epoxyeicosatrienoic acid exhibits STAT3-dependent cell growth promotion and may also participate in the autocrine/paracrine pathway that drives cell growth.
    (±)14,15-Epoxyeicosatrienoic acid
  • HY-N9608
    6-Ketocholestanol
    98.68%
    6-Ketocholestanol is a recoupler for mitochondria, chromatophores and cytochrome oxidase proteoliposomes. 6-Ketocholestanol increases the membrane dipole potential.
    6-Ketocholestanol
  • HY-N7266
    Obtusifoliol
    Inhibitor 99.86%
    Obtusifoliol is a specific CYP51 inhibitor, Obtusifoliol shows the affinity with Kd values of 1.2 μM and 1.4 μM for Trypanosoma brucei (TB) and human CYP51, respectively.
    Obtusifoliol
  • HY-W019847
    Azamulin
    Inhibitor
    Azamulin is an irreversible, highly selective inhibitior of human CYP3Aa. Azamulin has CYP3A inhibition activity with IC50 values range from 0.03-0.24 μM. Azamulin can be used for the research of metabolism and antiinfection.
    Azamulin
  • HY-N6066
    Praeruptorin E
    Activator 99.83%
    Praeruptorin E is an orally active pyranocoumarin compound. Praeruptorin E can be isolated from the dried roots of Peucedanum praeruptorum Dunn. Praeruptorin E reduces the expression of NF-κB. Praeruptorin E upregulates the expression of PXR and CYP3A4. Praeruptorin E inhibits Th2 cytokines, TNF-α, IL6, MPO, and blocks the Ca2+ slow channel. Praeruptorin E promotes pulmonary tissue repair and relaxes porcine coronary artery strips. Praeruptorin E protects mice from lipopolysaccharide- and hydrochloric acid-induced acute lung injury. Praeruptorin E can be used in studies related to asthma and acute lung injury.
    Praeruptorin E
  • HY-A0069
    Doxylamine succinate
    Activator 99.76%
    Doxylamine succinate is a first-generation antihistamine and acts as a histamine H1 receptor antagonist. Doxylamine succinate is orally active, possessing analgesic and hypnotic activities. Doxylamine succinate enhances the activities of CYP2B, CYP2A, CYP3A and thyroxine-glucuronosyltransferase via promoting substrate hydroxylation and thyroxine metabolic pathways. Doxylamine succinate decreases serum thyroxine (T4) level and elevates serum thyroid-stimulating hormone (TSH) level. Doxylamine succinate induces liver enlargement and increases the activities of hepatic microsomal cytochrome P450, cytochrome b5 and NADPH-cytochrome c reductase. Doxylamine succinate can be used for the research of nausea, allergy, insomnia.
    Doxylamine succinate
  • HY-157435
    PELI1-IN-1
    Activator 98.02%
    PELI1-IN-1 (compound 3d) is a potent inhibitor of PELI1, E3 ubiquitin ligase. PELI1-IN-1 has anti-tumPELI1-IN-1, a Resveratrol (HY-16561) derivative, is an orally active PELI1 Inhibitor (Kd = 8.2 μM). PELI1-IN-1 markedly interrupts the interaction of PELI1 and SNAIL/SLUG, and inhibits the K63-polyubiquitization of SNAIL/SLUG by PELI1, subsequently downregulating the protein levels of epithelial-mesenchymal transition (EMT) effectors SNAIL/SLUG. PELI1-IN-1 significantly reduces the level of SNAIL, SLUG and Vimentin without affecting the PELI1 expression. PELI1-IN-1 targets the FHA domain of PELI1 and disrupts the interaction, leading to the anti-metastasis of TNBC cells in vitro and in vivo. PELI1-IN-1 shows no evident toxicity in vivo.
    PELI1-IN-1
  • HY-B0854
    Mancozeb
    Modulator
    Mancozeb is a widely used fungicide that is effective against fungal diseases in most cereals, vegetables, fruits and ornamental plants. In addition, Mancozeb can cause liver damage in mice by activating the Keap1/Nrf2 signaling pathway. Mancozeb upregulates lactate dehydrogenase and cytochrome c to alter cell metabolism and induce cell death. Mancozeb has reproductive toxicity and can induce apoptosis in ovarian cells.
    Mancozeb
  • HY-14247A
    Fadrozole
    Inhibitor 99.78%
    Fadrozole (CGS 16949A free base) is a potent, selective and nonsteroidal inhibitor of aromatase with an IC50 of 6.4 nM.
    Fadrozole
  • HY-B1184AR
    (S)-Mephenytoin (Standard)
    (S)-Mephenytoin (Standard) is the analytical standard of (S)-Mephenytoin. This product is intended for research and analytical applications. (S)-Mephenytoin ((+)-Mephenytoin) is an anticonvulsive agent. (S)-Mephenytoin is a substrate of the cytochrome P450 (CYP) isoform CYP2C19. (S)-Mephenytoin can be used for the analysis of cytochrome P450 metabolism.
    (S)-Mephenytoin (Standard)
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