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-B1184S2
    Mephenytoin-d8
    Mephenytoin-d8 is the deuterium labeled Mephenytoin. Mephenytoin, an anticonvulsant, is the CYP2C19 and CYP2B6 substrate.
    Mephenytoin-d<sub>8</sub>
  • HY-163816
    Antiproliferative agent-53-d3
    Inhibitor
    Antiproliferative agent-53-d3 (Compound C1) is an inhibitor for theta-mediated end joining (TMEJ) in HEK293 cell with an IC50 of 0.14 µM. Antiproliferative agent-53-d3 is the inhibitor for CYP2C19 and CYP2C9 with IC50 of 0.77 and 3.1 µM. Antiproliferative agent-53-d3 inhibits the proliferation of DNA repair-compromised cells, with IC50 of 8.1 µM for BRCA2-/- DLD-1. Antiproliferative agent-53-d3 exhibits good pharmacokinetic characteristics in CD-1 mice.
    Antiproliferative agent-53-d<sub>3</sub>
  • HY-B1717A
    Oxolamine hydrochloride
    Inhibitor
    Oxolamine hydrochloride (SKF-9976 hydrochloride) is an orally active antitussive. Oxolamine hydrochloride can inhibit CYP2B1/2. Oxolamine hydrochloride has anti-inflammatory effects on the respiratory organs of guinea pigs. Oxolamine hydrochloride increases the AUC of Warfarin (HY-B0687) and prolongs its terminal half-life. Oxolamine hydrochloride can be used in respiratory disease research.
    Oxolamine hydrochloride
  • HY-156875
    20-HETE inhibitor-1
    Inhibitor
    20-HETE inhibitor-1 (comp 83) is a 20-HETE formation inhibitor
    20-HETE inhibitor-1
  • HY-145546
    14(15)-EpETE
    14(15)-EpETE is the epoxide of cytochrome P450 (CYP450) and is involved in the regulation of vascular tone and renal function.
    14(15)-EpETE
  • HY-P1735
    Moth Cytochrome C (MCC) (88-103)
    Moth Cytochrome C (MCC) (88-103), derived from the carboxyl terminus of moth cytochrome c, induces positive selection of TCR transgenic thymocytes.
    Moth Cytochrome C (MCC) (88-103)
  • HY-N0598R
    Ginsenoside F1 (Standard)
    Inhibitor
    Ginsenoside F1 (Standard) is the analytical standard of Ginsenoside F1. This product is intended for research and analytical applications. Ginsenoside F1, an enzymatically modified derivative of Ginsenoside Rg1, demonstrates competitive inhibition of CYP3A4 activity and weaker inhibition of CYP2D6 activity.
    Ginsenoside F1 (Standard)
  • HY-N10754
    Aschantin
    Inhibitor
    Aschantin, a bisepoxylignan, can be isolated from Magnolia biondii. Aschantin has antiplasmodial, Ca2+-antagonistic, platelet activating factor-antagonistic, and chemopreventive activities. Aschantin is a mTOR kinase inhibitor. Aschantin is also an inhibitor of Cytochrome P450 and UGT enzyme.
    Aschantin
  • HY-172173
    CYP17A1-IN-1
    Inhibitor
    CYP17A1-IN-1 (Compound 14) is the inhibitor for CYP17A1 with an IC50 of 26 nM. CYP17A1-IN-1 exhibits cytotoxicity in androgen-sensitive prostate cancer cell LNCaP, inhibits the migration of cell DU-145.
    CYP17A1-IN-1
  • HY-B1751D
    Quinidine sulfate dihydrate
    Inhibitor
    Quinidine sulfate dihydrate is an antiarrhythmic agent. Quinidine sulfate dihydrate is a potent, orally active, selective cytochrome P450db inhibitor. Quinidine sulfate dihydrate is also a K+ channel blocker with an IC50 of 19.9 μM, and can induce apoptosis. Quinidine sulfate dihydrate can be used for malaria research.
    Quinidine sulfate dihydrate
  • HY-N2262R
    8-Geranyloxypsoralen (Standard)
    Inhibitor
    8-Geranyloxypsoralen (Standard) is the analytical standard of 8-Geranyloxypsoralen. This product is intended for research and analytical applications. 8-Geranyloxypsoralen is a furanocoumarin isolated from grapefruit, acts as a potent inhibitor of P450 3A4 (CYP3A4) with an IC50 of 3.93 μM.
    8-Geranyloxypsoralen (Standard)
  • HY-B0407AR
    Chlorpromazine hydrochloride (Standard)
    Inhibitor
    Chlorpromazine (hydrochloride) (Standard) is the analytical standard of Chlorpromazine (hydrochloride). This product is intended for research and analytical applications. Chlorpromazine hydrochloride is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine hydrochloride exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine hydrochloride also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine hydrochloride also can inhibit clathrin-mediated endocytosis.
    Chlorpromazine hydrochloride (Standard)
  • HY-13632S5
    Exemestane-13C,d2
    Inhibitor
    Exemestane-13C,d2 is 13C and deuterated labeled Exemestane (HY-13632). Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research.
    Exemestane-<sup>13</sup>C,d<sub>2</sub>
  • HY-147807
    HIV-1 inhibitor-40
    Inhibitor
    HIV-1 inhibitor-40 (Compound 4ab) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1 with an EC50 of 1.9 nM. HIV-1 inhibitor-40 displays weak CYP sensitivity with IC50 values of 5.16 μM and 4.51 μM against CYP2C9 and CYP2C19, respectively. HIV-1 inhibitor-40 has no apparent in vivo acute toxicity.
    HIV-1 inhibitor-40
  • HY-B0885R
    Econazole (Standard)
    Inhibitor
    Econazole (Standard) ((±)-Econazol (Standard)) is the analytical standard of Econazole (HY-B0885). This product is intended for research and analytical applications. Econazole ((±)-Econazol) is an orally active imidazole antifungal agent, as well as a cytochrome P-450 inhibitor and a blocker of calcium and manganese ion uptake. Econazole is active against a variety of fungi and some Gram-positive bacteria, but has no significant activity against Gram-negative bacteria. Econazole can inhibit the synthesis of prostaglandins and can also induce liver damage.
    Econazole (Standard)
  • HY-170929
    EMT inhibitor-3
    Activator
    EMT inhibitor-3 (compound 11i) is a epithelial-mesenchymal transition (EMT) inhibitor. EMT inhibitor-3 inhibits neuroblastoma SK-N-SH cells with an IC50 of 2.5 μM. EMT inhibitor-3 inhibits SK-N-SH cell proliferation, migration, and invasion. EMT inhibitor-3 increases the Bax/Bcl-2 protein expression ratio, promotes Cytochrome C ( HY-125857) release from mitochondria, and activates caspases 9 and caspases 3, inducing mitochondria-mediated endogenous tumor cell Apoptosis. EMT inhibitor-3 is potential for cancer research.
    EMT inhibitor-3
  • HY-121213
    Erysolin
    Inhibitor
    Erysolin is a CYP1A inhibitor with antigenic toxicity. Erysolin reduces benzo(a)pyrene-induced genotoxicity.
    Erysolin
  • HY-B0940S
    Ethylvanillin-d5
    Ethylvanillin-d5 is a deuterium labeled Ethylvanillin (HY-B0940).
    Ethylvanillin-d<sub>5</sub>
  • HY-B1751A
    Quinidine sulfate
    Inhibitor
    Quinidine Monosulfate is an antiarrhythmic agent. Quinidine Monosulfate is a potent, orally active, selective cytochrome P450db inhibitor. Quinidine Monosulfate is also a K+ channel blocker with an IC50 of 19.9 μM, and can induce apoptosis. Quinidine Monosulfate can be used for malaria research.
    Quinidine sulfate
  • HY-161700
    BMS-737
    BMS-737 (compound 33) is a non-steroidal, reversible small molecule inhibitor. BMS-737 exhibits 11-fold selectivity for CYP17 lyase over CYP17 hydroxylase. BMS-737 is designed to inhibit castration-resistant prostate cancer (CRPC) and significantly reduces testosterone levels without significant effects on orrodermal hormone and glucocorticoid levels.
    BMS-737
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