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CYP activity

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159

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5

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N0453
    Hypericin
    2 Publications Verification

    Apoptosis Influenza Virus Antibiotic Monoamine Oxidase PKC Cytochrome P450 Dopamine β-hydroxylase Reverse Transcriptase Telomerase Infection Neurological Disease Cancer
    Hypericin is a naturally occurring substance found in Hyperlcurn perforatum L. Hypericin is an inhibitor of PKC (protein kinase C), MAO (monoaminoxidase), dopamine-beta-hydroxylase, reverse transcriptase, telomerase and CYP (cytochrome P450). Hypericin shows antitumor, antiviral, antidepressive activities, and can induce apoptosis .
    Hypericin
  • HY-N0482
    Phillyrin
    1 Publications Verification

    Cytochrome P450 Influenza Virus Bacterial Infection Inflammation/Immunology Cancer
    Phillyrin is isolated from Forsythia suspensa Vahl (Oleaceae), has antibacterial and anti-inflammatory activities. Phillyrin has potential inductive effects on rat CYP1A2 and CYP2D1 activities, without affecting CYP2C11 and CYP3A1/2 activities . Phillyrin has anti-influenza A virus activities .
    Phillyrin
  • HY-155493

    Cytochrome P450 Cancer
    CYP19A1/CYP11B2-IN-1 (Compound X21) is a potent and selective aromatase and aldosterone synthase dual inhibitor with IC50s of 2.3 nM and 29 nM for aromatase (CYP19A1) and aldosterone synthase (CYP11B2), respectively. CYP19A1/CYP11B2-IN-1 has excellent antiproliferative and pro-apoptotic activity against the cancer cell. CYP19A1/CYP11B2-IN-1 can be used for research of breast cancer .
    CYP19A1/CYP11B2-IN-1
  • HY-116862

    DBF

    Cytochrome P450 Fluorescent Dye Others
    Dibenzylfluorescein (DBF) is a fluorogenic probe (Fluoresecent dye) that acts as a substrate for specific cytochrome P450 (CYP) isoforms, including CYP3A4, CYP2C8, CYP2C9, CYP2C19, and aromatase (CYP19). Dibenzylfluorescein is typically used near its Km value of 0.87-1.9 µM (Ex=485nm,Em=535nm). Dibenzylfluorescein is used to detect changes in CYP catalytic activity caused by drugs or disease .
    Dibenzylfluorescein
  • HY-162370

    Cytochrome P450 Infection Cancer
    CYP51-IN-16 (compound C6) is a phenylpyrimidine CYP51 inhibitor, and shows antifungal activity in in vitro. CYP51-IN-16 inhibits tumor cell growth .
    CYP51-IN-16
  • HY-18642

    PF-4981517

    Cytochrome P450 Others
    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-N0893S

    HZIV 81-2 d6

    Cytochrome P450 Autophagy Inflammation/Immunology Cancer
    Tetrahydrocurcumin-d6 is a deuterium labeled Tetrahydrocurcumin. Tetrahydrocurcumin is a Curcuminoid which displays inhibitory activity for CYP2C9 and CYP3A4[1].
    Tetrahydrocurcumin-d6
  • HY-162051

    Cytochrome P450 Cancer
    CYP1B1-IN-6 (compound 19) is a fluorescence molecular probes which inhibits CYP1B1 activity. CYP1B1-IN-6 can identify tumor sites in fluorescence imaging and photoacoustic imaging modes .
    CYP1B1-IN-6
  • HY-163359

    Cytochrome P450 HDAC Cancer
    CYP17A1/HDAC6-IN-1 (compound 12) is a potent inhibitor of CYP17A1/HDAC6, with IC50 of 0.284μM and 0.6015 μM,respectively. CYP17A1/HDAC6-IN-1 has anti-tumor activity .
    CYP17A1/HDAC6-IN-1
  • HY-144325

    Cytochrome P450 Infection
    CYP121A1-IN-1 is a potent CYP121A1 inhibitor with favorable activity against Mycobacterium tuberculosis (H37Rv MIC90∼6.25 μM, ∼2.2 μg/mL). CYP121A1-IN-1 can markedly reduce the production of mycocyclosin via inhibiting the CYP121A1 mediated turnover of cyclo(l-tyrosyl-l-tyrosyl) to mycocyclosin .
    CYP121A1-IN-1
  • HY-149617

    Cytochrome P450 PD-1/PD-L1 Infection
    CYP51/PD-L1-IN-4 (compound 14a-2) is a potent dual-target (CYP51/PD-L1) inhibitor, with IC50 values of 0.17 and 0.021 μM, respectively. CYP51/PD-L1-IN-4 exhibits excellent antifungal and antidrug-resistant fungal activity in vitro. CYP51/PD-L1-IN-4 can be used for fungal infections research .
    CYP51/PD-L1-IN-4
  • HY-N0598

    20(S)-Ginsenoside F1

    Cytochrome P450 Endogenous Metabolite Cancer
    Ginsenoside F1, an enzymatically modified derivative of Ginsenoside Rg1, demonstrates competitive inhibition of CYP3A4 activity and weaker inhibition of CYP2D6 activity.
    Ginsenoside F1
  • HY-N2071
    Cedrol
    1 Publications Verification

    (+)-Cedrol; α-Cedrol

    Cytochrome P450 Fungal Infection Inflammation/Immunology Cancer
    Cedrol is a bioactive sesquiterpene, a potent competitive inhibitor of cytochrome P-450 (CYP) enzymes. Cedrol inhibits CYP2B6-mediated bupropion hydroxylase and CYP3A4-mediated midazolam hydroxylation with Ki of 0.9 μM and 3.4 μM, respectively. Cedrol also has weak inhibitory effect on CYP2C8, CYP2C9, and CYP2C19 enzymes . Cedrol is found in cedar essential oil and poetesses anti-septic, anti-inflammatory, anti-spasmodic, tonic, astringent, diuretic, insecticidal, and anti-fungal activities .
    Cedrol
  • HY-B0822S1

    GABA Receptor Cytochrome P450 Inflammation/Immunology
    Fipronil- 13C6 is the 13C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
    Fipronil-13C6
  • HY-156150

    Fungal Cytochrome P450 PD-1/PD-L1 Infection
    CYP51/PD-L1-IN-2 (compound L20) is a quinazoline compound with antifungal activity. CYP51/PD-L1-IN-2 is a dual inhibitor of CYP51 (IC50: 0.263 μM) and PD-L1 (IC50: 0.017 μM), which can induce early apoptosis of fungal cells in the cell cycle. CYP51/PD-L1-IN-2 also significantly reduced intracellular IL-2, NLRP3, and NF-κBp65 protein levels, induced mitochondrial damage and ROS accumulation, and ultimately led to fungal lysis and death .
    CYP51/PD-L1-IN-2
  • HY-156151

    Fungal Cytochrome P450 PD-1/PD-L1 Infection
    CYP51/PD-L1-IN-3 (compound L21) is a quinazoline compound with antifungal activity. CYP51/PD-L1-IN-3 is a dual inhibitor of CYP51 (IC50: 0.205 μM) and PD-L1 (IC50: 0.039 μM), which can induce early apoptosis of fungal cells in the cell cycle. CYP51/PD-L1-IN-3 also significantly reduced intracellular IL-2, NLRP3, and NF-κBp65 protein levels, induced mitochondrial damage and ROS accumulation, and ultimately led to fungal lysis and death .
    CYP51/PD-L1-IN-3
  • HY-156149

    Fungal Cytochrome P450 PD-1/PD-L1 Infection
    CYP51/PD-L1-IN-1 (compound L11) is a quinazoline compound with antifungal activity. CYP51/PD-L1-IN-1 is a dual inhibitor of CYP51 (IC50: 0.884 μM) and PD-L1 (IC50: 0.083 μM), which can induce early apoptosis of fungal cells in the cell cycle. CYP51/PD-L1-IN-1 also significantly reduced intracellular IL-2, NLRP3, and NF-κBp65 protein levels, induced mitochondrial damage and ROS accumulation, and ultimately led to fungal lysis and death .
    CYP51/PD-L1-IN-1
  • HY-135331

    Androgen Receptor Cytochrome P450 Cancer
    N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration .
    N-Desmethyl-Apalutamide
  • HY-70013
    Abiraterone
    Maximum Cited Publications
    17 Publications Verification

    CB-7598

    Cytochrome P450 Cancer
    Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochrome p450 enzyme CYP17 with IC50s of 2.5 nM and 15 nM, respectively.
    Abiraterone
  • HY-128920

    Cytochrome P450 Cancer
    Phortress free base (NSC 710305) is a P450 CYP1A1-activated antitumor prodrug with antitumor activity . Phortress free base leads to DNA damage and cell cycle arrest .
    Phortress free base
  • HY-100665
    Dehydroaripiprazole
    1 Publications Verification

    OPC-14857; DM-14857

    5-HT Receptor Neurological Disease
    Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole .
    Dehydroaripiprazole
  • HY-148595

    Cytochrome P450 Cancer
    Antitumor agent-88 exhibits potent antimitotic activity and arrests cell in the G2/M phase. Antitumor agent-88 disrupts the microtubule and the cytoskeleton in CYP1A1-expressing breast cancer cells. Antitumor agent-88 is also a competitive inhibitor of CYP1A1 (Ki: 1.4 μM) .
    Antitumor agent-88
  • HY-W019847

    Cytochrome P450 Infection Metabolic Disease
    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-113575

    OPC-14857 hydrochloride; DM-14857 hydrochloride

    5-HT Receptor Neurological Disease
    Dehydroaripiprazole (OPC-14857) hydrochloride is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole hydrochloride. Dehydroaripiprazole hydrochloride has with antipsychotic activity equivalent to Aripiprazole .
    Dehydroaripiprazole hydrochloride
  • HY-N0693
    Schisandrin A
    5+ Cited Publications

    Schizandrin-A; Wuweizisu-A; Deoxyschizandrin

    Cytochrome P450 Autophagy Virus Protease Inflammation/Immunology Cancer
    Schisandrin A inhibits CYP3A activity with an IC50 of 6.60 μM and Ki of 5.83 μM, respectively.
    Schisandrin A
  • HY-119804

    Cytochrome P450 Neurological Disease
    Licopyranocoumarin is an isoflavonoid that shows CYP3A4 inhibitory activity with an IC50 of 32 μM. Licopyranocoumarin has potent neuroprotective activities .
    Licopyranocoumarin
  • HY-70013S

    CB-7598-d4

    Cytochrome P450 Cancer
    Abiraterone-d4 is the deuterium labeled Abiraterone. Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochrome p450 enzyme CYP17 with IC50s of 2.5 nM and 15 nM, respectively.
    Abiraterone-d4
  • HY-10882
    Clotrimazole
    5 Publications Verification

    Fungal Bacterial Autophagy Antibiotic Infection Cancer
    Clotrimazole is an imidazole derivative, an antifungal compound and is a CYP (cytochrome P450) inhibitor. Clotrimazole has antibacterial activity.
    Clotrimazole
  • HY-122277

    Cytochrome P450 Metabolic Disease
    1'-Hydroxy bufuralol, the main metabolite of bufuralol, can reflect CYP2D activity .
    1'-Hydroxy bufuralol
  • HY-W754151

    Isotope-Labeled Compounds Others
    N-Desmethyl apalutamide-d4 is the deuterium-labeled N-Desmethyl-Apalutamide (HY-135331). N-Desmethyl Apalutamide is an active metabolite of Apalutamide. N-Desmethyl Apalutamide is a less potent antagonist of the androgen receptor and is responsible for one-third of the activity of Apalutamide. The formation of N-Desmethyl Apalutamide mediated predominantly by CYP2C8 and CYP3A4. N-Desmethyl Apalutamide is moderate to strong CYP3A4 and CYP2B6 inducer and has an excellent plasma-proteins bound concentration .
    N-Desmethyl apalutamide-d4
  • HY-19340
    TMS
    5 Publications Verification

    (E)-2,3',4,5'-tetramethoxystilbene

    Cytochrome P450 Cancer
    TMS ((E)-2,3',4,5'-tetramethoxystilbene) is a selective and competitive CYP1B1 inhibitor with an IC50 of 6 nM and a Ki value of 3 nM. TMS shows a lesser extent inhibitory effect on CYP1A1 (IC50=300 nM) and CYP1A2 (IC50=3.1 μM). TMS is a methylated derivative of resveratrol and has anti-cancer activity .
    TMS
  • HY-W010195

    Cytochrome P450 Others
    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
  • HY-120425

    Others Infection
    Ethiprole is an insecticide.Metabolic sulfones are produced faster than Fipronil (HY-B0822) in CYP3A4-expressing cells and in vivo in mouse brain and liver.Ethiprole's sulfide, sulfoxide, sulfone and desulfinyl derivatives have better biological activity .
    Ethiprole
  • HY-N0921

    (+)-Dihydromethysticin

    Cytochrome P450 Inflammation/Immunology
    Dihydromethysticin is one of the six major kavalactones found in the kava plant; has marked activity on the induction of CYP3A23.
    Dihydromethysticin
  • HY-103223

    NSC 710305

    Cytochrome P450 Cancer
    Phortress is a high affinity AhR ligand that elicits antitumor activity by inducing transcription of CYP1A1 .
    Phortress
  • HY-W011235

    5-HT Receptor Calcium Channel Drug Metabolite Neurological Disease
    Norfluoxetine hydrochloride is an active N-demethylated metabolite of Fluoxetine. Fluoxetine is a selective serotonin (5-HT) reuptake inhibitor that is metabolized to Norfluoxetine hydrochloride by cytochrome P450 (CYP) 2D6, CYP2C19, and CYP3A4. Norfluoxetine hydrochloride inhibits 5-HT uptake and inhibits CaV3.3 T current (IC50 = 5 μM). Norfluoxetine hydrochloride has anticonvulsant activity .
    Norfluoxetine hydrochloride
  • HY-163324A

    Cytochrome P450 Others
    2-Me PeER is a rhodamine dye-based fluorescent probe that detects CYP3A4 activity. In fluorescence-activated cell sorting (FACS) based on CYP3A4 activity, homogeneous and functional human induced pluripotent stem cell (hiPSC)-derived hepatocytes and intestinal epithelial cells can be obtained with the aid of 2-Me PeER .
    2-Me PeER
  • HY-12946A

    BI 653048 phosphate is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM . BI 653048 phosphate inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM) . BI 653048 phosphate is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus .
    BI 653048 phosphate
  • HY-12946

    BI 653048 is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM . BI 653048 inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM) . BI 653048 is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus .
    BI 653048
  • HY-17643

    VT-1161

    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-N0125
    Diosmetin
    5 Publications Verification

    Cytochrome P450 Cancer
    Diosmetin is a natural flavonoid which inhibits human CYP1A enzyme activity with an IC50 of 40 μM in HepG2 cell.
    Diosmetin
  • HY-14874
    Topiroxostat
    5 Publications Verification

    FYX-051

    Xanthine Oxidase Cytochrome P450 Metabolic Disease
    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-100665S

    OPC-14857-d8; DM-14857-d8

    Isotope-Labeled Compounds 5-HT Receptor Neurological Disease
    Dehydroaripiprazole-d8 is deuterium labeled Dehydroaripiprazole. Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole[1][2][3].
    Dehydroaripiprazole-d8
  • HY-N0043

    Gypenoside VIII

    NF-κB COX Calcium Channel Cytochrome P450 Endogenous Metabolite Cardiovascular Disease Inflammation/Immunology Cancer
    Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca 2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
    Ginsenoside Rd
  • HY-N0382
    Galangin
    5+ Cited Publications

    Norizalpinin; 3,5,7-Trihydroxyflavone

    Cytochrome P450 Autophagy Cancer
    Galangin (Norizalpinin) is an agonist/antagonist of the arylhydrocarbon receptor. Galangin (Norizalpinin) also shows inhibition of CYP1A1 activity.
    Galangin
  • HY-148375

    Drug Metabolite Others
    Abiraterone sulfate is a metabolite of Abiraterone (HY-148377). Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity .
    Abiraterone sulfate
  • HY-100665R

    OPC-14857 (Standard); DM-14857 (Standard)

    5-HT Receptor Neurological Disease
    Dehydroaripiprazole (Standard) is the analytical standard of Dehydroaripiprazole. This product is intended for research and analytical applications. Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole .
    Dehydroaripiprazole (Standard)
  • HY-13463BS

    AKR-501-d8 hydrochloride; E5501-d8 hydrochloride; YM477-d8 hydrochloride

    Isotope-Labeled Compounds Thrombopoietin Receptor Cardiovascular Disease
    Avatrombopag-d8 (hydrochloride) is deuterium labeled Avatrombopag (hydrochloride). Avatrombopag (AKR-501) hydrochloride is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag hydrochloride mimics the biological activities of TPO. Avatrombopag hydrochloride increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag hydrochloride is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A[1][2][3].
    Avatrombopag-d8 hydrochloride
  • HY-100901

    Cytochrome P450 Metabolic Disease
    CDD3505 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.
    CDD3505
  • HY-100902

    Cytochrome P450 Metabolic Disease
    CDD3506 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.
    CDD3506

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