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Isoforms Recommended: CYP1
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CYP 1A1

" in MedChemExpress (MCE) Product Catalog:

173

Inhibitors & Agonists

4

Fluorescent Dyes

1

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32

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16

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2

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1

Click Chemistry

6

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N0904
    Ginsenoside C-K
    5 Publications Verification

    Ginsenoside compound K; Ginsenoside K

    COX NO Synthase Cytochrome P450 Inflammation/Immunology
    Ginsenoside C-K, a bacterial metabolite of G-Rb1, exhibits anti-inflammatory effects by reducing iNOS and COX-2. Ginsenoside C-K exhibits an inhibition against the activity of CYP2C9 and CYP2A6 in human liver microsomes with IC50s of 32.0±3.6 μM and 63.6±4.2 μM, respectively.
    Ginsenoside C-K
  • HY-N0043
    Ginsenoside Rd
    1 Publications Verification

    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
    Maximum Cited Publications
    18 Publications Verification

    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-Y0110
    2-Naphthol
    1 Publications Verification

    Environmental Pollutants Endogenous Metabolite Others
    2-Naphthol is a metabolite of naphthalene, catalyzed by cytochrome P450 (CYP) isozymes (CYP 1A1, CYP 1A2, CYP 2A1, CYP 2E1 and CYP 2F2).
    2-Naphthol
  • HY-N2194
    Bergamottin
    5+ Cited Publications

    5-Geranoxypsoralen; Bergamotine; Bergaptin

    Cytochrome P450 Cancer
    Bergamottin is a potent and competitive CYP1A1 inhibitor with a Ki of 10.703 nM.
    Bergamottin
  • HY-122277

    Ro 03-7410

    Drug Metabolite Metabolic Disease
    1'-Hydroxy bufuralol is the main metabolite of Bufuralol (HY-105124) by the cytochrome P450 isoenzymes 2D1 and 2D2 (CYP2D1/2). 1'-Hydroxy bufuralol can be used to determine CYP2D1/2 enzyme activity .
    1'-Hydroxy bufuralol
  • HY-19340
    TMS
    5+ Cited Publications

    (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-B0973

    DBT; Diphenylene sulfide

    Cytochrome P450 Aryl Hydrocarbon Receptor Metabolic Disease
    Dibenzothiophene is an orally active and a noncompetitive CYP1A inhibitor. Dibenzothiophene inhibits CYP1A-mediated EROD activity with a Km of 0.592 μM. Dibenzothiophene interacts with the AHR pathway. Dibenzothiophene enhances the embryotoxicity of β-naphthoflavone (HY-114740). Dibenzothiophene shows acute toxicity in mice. Dibenzothiophene is mainly used for the study of the mechanism of developmental toxicity in organisms .
    Dibenzothiophene
  • HY-134217

    Aryl Hydrocarbon Receptor Cancer
    KYN-101 is a potent, selective and orally active AHR inhibitor. KYN-101 decreases the CYP1A1 mRNA expression. KYN-101 shows anti-cancer activity .
    KYN-101
  • HY-N2425

    Cholinesterase (ChE) Metabolic Disease
    Rhodiosin is a double inhibitor of CYP2D6 and AChE, and can be isolated from Rhodiolis rhodiolis root. The IC50 for CYP2D6 is 0.761 μM, and the Ki is 0.769 μM. Rhodiosin has antioxidant and neuroprotective activity and can regulate HIF-1α signaling pathway to protect the central nervous system
    Rhodiosin
  • HY-B0822

    Environmental Pollutants Cytochrome P450 GABA Receptor Apoptosis Neurological Disease
    Fipronil is a broad-spectrum insecticide effective against Lepidoptera species as well as thrips, locusts, ants, cockroaches, fleas and ticks. Fipronil selectively inhibits GABA receptor with IC50s of 30 nM and 1600 nM for cockroach and rat GABA receptors, respectively. Glutamate-gated chloride channels (GluCls), which are present in cockroaches but not in mammals, are sensitive to the blocking effect of Fipronil. Fipronil also induces apoptosis in HepG2 cells and promotes the expression of CYP1A1 and CYP3A4 mRNA in human hepatocytes .
    Fipronil
  • HY-N5132

    Cytochrome P450 Others
    (-)-Fenchone is a bicyclic monoterpene and serves as a substrate for human liver microsomal cytochrome P450 enzymes CYP2A6 and CYP2B6. (-)-Fenchone is not metabolized by human CYP1A1, CYP1A2, CYP1B1, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, or CYP3A4 enzymes. (-)-Fenchone undergoes hydroxylation to produce 6-exo-hydroxyfenchone, 6-endo-hydroxyfenchone, and 10-hydroxyfenchone. During the metabolism of (-)-Fenchone, CYP2A6 may play a more important role than CYP2B6 .
    (-)-Fenchone
  • HY-Y0110S1

    Endogenous Metabolite Others
    2-Naphthol-d7 is the deuterium labeled 2-Naphthol . 2-Naphthol is a metabolite of naphthalene, catalyzed by cytochrome P450 (CYP) isozymes (CYP 1A1, CYP 1A2, CYP 2A1, CYP 2E1 and CYP 2F2) .
    2-Naphthol-d7
  • HY-152118

    Cytochrome P450 Cancer
    CYP1B1-IN-4 is a 2,4-diarylthiazole compound with selectively CYP1B1 inhibition (IC50=0.2 nM). CYP1B1-IN-4 has little cytotoxicity and high stability in both human and rat liver microsomes .
    CYP1B1-IN-4
  • HY-101285
    DMU2139
    1 Publications Verification

    Cytochrome P450 Cancer
    DMU2139 is a potent and specific CYP1B1 inhibitor, with IC50s of 9 nM and 795 nM for CYP1B1 and CYP1A1, respectively.
    DMU2139
  • HY-122277S

    Ro 03-7410-d9

    Isotope-Labeled Compounds Drug Metabolite Metabolic Disease
    1'-Hydroxy bufuralol-d9 is a deuterium labeled 1'-Hydroxy bufuralol (HY-122277). 1'-Hydroxy bufuralol is the main metabolite of Bufuralol (HY-105124) by the cytochrome P450 isoenzymes 2D1 and 2D2 (CYP2D1/2). 1'-Hydroxy bufuralol can be used to determine CYP2D1/2 enzyme activity .
    1'-Hydroxy bufuralol-d9
  • HY-W007700

    PROTAC Linkers Cancer
    8-Bromooctanoic acid is a PROTAC linker, and can be used for synthesis of PROTAC CYP1B1 degrader-2 (HY-158429) .
    8-Bromooctanoic acid
  • HY-120377

    HBV Cancer
    CYP1A1 inhibitor 8a is a compound that potently and selectively inhibits the CYP1A1 enzyme and has the potential to prevent cancer. CYP1A1 inhibitor 8a exhibits more than 10-fold selectivity for CYP1A1 and more than 100-fold selectivity over other enzymes in the CYP1 subfamily. CYP1A1 inhibitor 8a can effectively antagonize B[a]P-mediated activation of the aryl hydrocarbon receptor (AhR) in yeast cells and protect human cells from CYP1A1-mediated B[a]P toxicity. CYP1A1 inhibitor 8a has the potential to be developed as a cancer chemopreventive agent .
    CYP1A1 inhibitor 8a
  • HY-156530

    Cytochrome P450 Endocrinology
    CYP11A1-IN-1 (compound 30) is an inhibitor of CYP11A1, with IC50 value of 201-2000 nM. CYP11A1-IN-1 can be used for research in steroid receptor, particularly androgen receptor, dependent diseases and conditions, such as prostate cancer .
    CYP11A1-IN-1
  • HY-W072025

    Cytochrome P450 Keap1-Nrf2 Heme Oxygenase (HO) Reactive Oxygen Species (ROS) Inflammation/Immunology
    CYP2E1-IN-1 (Compound 10) is an orally active cytochrome P450 2E1 (CYP2E1) inhibitor with a Kd of 7.02 μM, an IC50 of 1.64 μM, and a Ki of 0.897 μM. CYP2E1-IN-1 activates the Nrf2/HO-1 signaling pathway and inhibits ROS production, thereby alleviating pancreatic injury. CYP2E1-IN-1 has significant anti-inflammatory and antioxidant activities and can effectively reduce inflammation and oxidative stress in severe acute pancreatitis (SAP). CYP2E1-IN-1 can be used in the study of SAP and other inflammatory-related diseases .
    CYP2E1-IN-1
  • HY-108938

    Cytochrome P450 Fungal Parasite Infection
    SDZ285428 is a CYP51 inhibitor. SDZ285428 inhibits Trypanosoma cruzi (TC) CYP51 with I/E2 <1 (5 min) and I/E2=9 (1 h). SDZ285428 inhibits Trypanosoma brucei (TB) CYP51 with I/E2 <1 (5 min) and I/E2=35 (1 h) .
    SDZ285428
  • HY-128859

    Cytochrome P450 Metabolic Disease
    EMT inhibitor-2 (Compound 1) inhibits epithelial-mesenchymal transition (EMT) induced by substances such as IL-1β and TGF-β released from the immunocytes. EMT inhibitor-2 inhibits CYP3A4 testosteron and CYP2C9 with IC50s of 49.72 and 5.54 μM, respectively .
    EMT inhibitor-2
  • HY-130353

    N-desethylamiodarone hydrochloride; LB 33020 hydrochloride

    Potassium Channel Autophagy Cardiovascular Disease
    Desethylamiodarone hydrochloride (N-desethylamiodarone hydrochloride) is a major active metabolite of Amiodarone. Desethylamiodarone hydrochloride is formed by CYP3A isoenzymes. Amiodarone is an antiarrhythmic agent for inhibition of ATP-sensitive potassium channel with an IC50 of 19.1 μM .
    Desethylamiodarone hydrochloride
  • HY-N10344

    Cytochrome P450 Quinone Reductase Cancer
    Glucoarabin is a bioactive glucosinolate. In Hepa1c1c7 cells, hydrolyzed Glucoarabin (hGSL 9) upregulates the phase II detoxification enzyme quinone reductase (NQO1), with no effect on cytochrome P450 (CYP) 1A1 activity .
    Glucoarabin
  • HY-157942

    Cytochrome P450 Cancer
    CYP1B1-IN-7 (compound 2a) is a selective inhibitor of CYP1B1 (IC50: 75 nM). CYP1B1-IN-7 also reverses resistance (IC50: 29 μM) and exhibits cytotoxicity in the CYP1B1-overexpressing MCF-7 cell line that is resistant to Docetaxel (HY-B0011) .
    CYP1B1-IN-7
  • HY-N8382

    Cytochrome P450 Parasite Insecticide Infection
    Chalepensin is a nematicide and CYP inhibitor. Chalepensin inhibits CYP2A6, CYP1A1, CYP1A2, CYP2A13, CYP2C9, CYP2D6, CYP2E1, and CYP3A4 to varying degrees, with IC50 values of 82.3 μM, 2.86 μM, 3.01 μM, 0.21 μM, 6.58 μM, 1.67 μM, 61.1 μM, and 61.7 μM, respectively. Chalepensin potently and selectively kills third-stage infective larvae of Strongyloides venezuelensis .
    Chalepensin
  • HY-152159

    Cytochrome P450 Cancer
    CYP4Z1-IN-1 (compound 7c) is a potent CYP4Z1 inhibitor, with an IC50 of 41.8 nM. CYP4Z1-IN-1 decreases the expression of breast CSCs stemness markers, spheroid formation, and metastatic ability as well as tumor-initiation capability in a concentration-dependent manner in vitro and in vivo .
    CYP4Z1-IN-1
  • HY-159006

    Cytochrome P450 Cancer
    CYP1B1 ligand 3 (Compound A1) is a selective inhibitor for cytochrome P450 enzyme CYP1B1 with an IC50 of 11.9 nM. CYP1B1 ligand 3 can be utilized for the synthesis of PROTAC CYP1B1 degrader-2 (HY-158429) .
    CYP1B1 ligand 3
  • HY-W008003

    Cytochrome P450 Others
    2-Hydroxybenzimidazole is an inactive compound targeting CYP1A1 and is mainly used as a control compound in the structure-activity relationship study of benzimidazole derivatives. 2-Hydroxybenzimidazole does not have the ability to induce CYP1A1 expression like its thiol or amino substituted derivatives .
    2-Hydroxybenzimidazole
  • 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-W130610R

    Liposome Reference Standards Akt mTOR Others
    Ginsenoside C-K (Standard) is the analytical standard of Ginsenoside C-K. This product is intended for research and analytical applications. Ginsenoside C-K, a bacterial metabolite of G-Rb1, exhibits anti-inflammatory effects by reducing iNOS and COX-2. Ginsenoside C-K exhibits an inhibition against the activity of CYP2C9 and CYP2A6 in human liver microsomes with IC50s of 32.0±3.6 μM and 63.6±4.2 μM, respectively.
    Stearamide (Standard)
  • HY-101284

    Cytochrome P450 Cancer
    DMU2105 is a potent and specific CYP1B1 inhibitor, with IC50s of 10 nM and 742 nM for CYP1B1 and CYP1A1, respectively.
    DMU2105
  • HY-W472509

    11-Hydroxy-5,8,12,14-eicosatetraenoic acid

    Cytochrome P450 Cardiovascular Disease
    11-HETE (11-Hydroxy-5,8,12,14-eicosatetraenoic acid) is the activator for cytochrome P450. 11-HETE upregulates the mRNA expressions of CYP1B1, CYP1A1, CYP4A11, CYP4F11, and CYP4F2, induces cell hypertrophy in RL-14 cell, and exhibits potential to be used in cardiovascular diseases .
    11-HETE
  • HY-122508

    Drug Metabolite Neurological Disease
    Hydroxyebastine is an Ebastine (HY-B0674) (a histamine H1-receptor antagonist) metabolite. Hydroxyebastine is metabolized to Carebastine (HY-121356) by CYP2J2 and CYP3A4 .
    Hydroxyebastine
  • HY-129247

    MDM-2/p53 Aryl Hydrocarbon Receptor Cytochrome P450 Cancer
    Versicolorin A is a biosynthetic precursor of Aflatoxin B1 (HY-N6615). Versicolorin A induces phosphorylation of p53. Versicolorin A activates the aryl hydrocarbon receptor AhR and significantly induces the expression of CYP1A1. Versicolorin A exerts genotoxic and cytotoxic effects. Versicolorin A enhances the genotoxicity of aflatoxin B1 in cells by promoting CYP450-mediated bioactivation of aflatoxin B1. Versicolorin A can be used in research related to colorectal cancer and hepatocellular carcinoma .
    Versicolorin A
  • HY-N0904R

    Ginsenoside compound K(Standard); Ginsenoside K (Standard)

    Reference Standards COX NO Synthase Cytochrome P450 Inflammation/Immunology
    Ginsenoside C-K (Standard) is the analytical standard of Ginsenoside C-K. This product is intended for research and analytical applications. Ginsenoside C-K, a bacterial metabolite of G-Rb1, exhibits anti-inflammatory effects by reducing iNOS and COX-2. Ginsenoside C-K exhibits an inhibition against the activity of CYP2C9 and CYP2A6 in human liver microsomes with IC50s of 32.0±3.6 μM and 63.6±4.2 μM, respectively.
    Ginsenoside C-K (Standard)
  • HY-Y0110S

    Endogenous Metabolite Others
    2-Naphthol-d8 is the deuterium labeled 2-Naphthol . 2-Naphthol is a metabolite of naphthalene, catalyzed by cytochrome P450 (CYP) isozymes (CYP 1A1, CYP 1A2, CYP 2A1, CYP 2E1 and CYP 2F2) .
    2-Naphthol-d8
  • HY-Y0110R

    Reference Standards Endogenous Metabolite Others
    2-Naphthol (Standard) is the analytical standard of 2-Naphthol. This product is intended for research and analytical applications. 2-Naphthol is a metabolite of naphthalene, catalyzed by cytochrome P450 (CYP) isozymes (CYP 1A1, CYP 1A2, CYP 2A1, CYP 2E1 and CYP 2F2).
    2-Naphthol (Standard)
  • HY-175836

    Cytochrome P450 Apoptosis Cancer
    CYP1B1-IN-12 is a selective cytochrome P450 1B1 (CYP1B1) inhibitor with an IC50 of 6.05 nM. CYP1B1-IN-12 demonstrates remarkable selectivity, exceeding 1600-fold and 16,000-fold over CYP1A1 and CYP1A2, respectively. CYP1B1-IN-12 can enhance Paclitaxel (HY-B0015)-mediated apoptosis and restore Paclitaxel sensitivity in A549/Taxol-resistant cells. CYP1B1-IN-12 can inhibit the epithelial-mesenchymal transition process and reduce cells migration and invasion. CYP1B1-IN-12 can be used for the research of cancer, such as non-small cell lung cancer (NSCLC) .
    CYP1B1-IN-12
  • HY-146177

    Bacterial Cytochrome P450 Infection
    CYP3A4 enzyme-IN-1 (compound 59) is a potent antibacterial agent, with a MIC of 1 μg/mL for MRSA. CYP3A4 enzyme-IN-1 exhibits low to moderate inhibitory effects on CYP1A2, CYP2E1, CYP2D6, and CYP3A4 enzymes .
    CYP3A4 enzyme-IN-1
  • HY-118216

    Biloxazol

    Fungal Cytochrome P450 Infection
    Bitertanol (Biloxazol) is a potent antifungal agent. Bitertanol also is an CYP1A1, CYP2B, and CYP3A inducer in vivo and an CYP1A inhibitor in vitro .
    Bitertanol
  • HY-152196

    Cytochrome P450 Cancer
    CYP1B1-IN-5 (Compound 6q) is a potent and selective cytochrome P450 1B1 (CYP1B1) inhibitor with an IC50 of 4.7 nM .
    CYP1B1-IN-5
  • 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-N0922

    DL-Methysticin; (±)-Methystici

    Cytochrome P450 Neurological Disease
    Methysticin is a major kavalactone in kava extract to induce CYP1A1.
    Methysticin
  • HY-163015

    DNA/RNA Synthesis Infection
    RNA polymerase-IN-1 (compound 4) is s DNA-dependent RNA polymerase inhibitor. RNA polymerase-IN-1 inhibits CYP isozymes .
    RNA polymerase-IN-1
  • HY-100331

    MCHR1 (GPR24) Cytochrome P450 Metabolic Disease Endocrinology
    MCH-1 antagonist 1 is a potent melanin concentrating hormone (MCH-1) antagonist with a Ki of 2.6 nM. MCH-1 antagonist 1 also inhibits CYP3A4 with an IC50 of 10 μM.
    MCH-1 antagonist 1
  • HY-N6264

    Aryl Hydrocarbon Receptor ERK Metabolic Disease
    26-Deoxyactein is a constituent isolated from Cimicifuga racemosa, prevents TCDD-induced osteoblasts damage. 26-Deoxyactein inhibits increased AhR, CYP1A1 and ERK levels .
    26-Deoxyactein
  • HY-N0382R

    Norizalpinin (Standard); 3,5,7-Trihydroxyflavone (Standard)

    Reference Standards Cytochrome P450 Autophagy Cancer
    Galangin (Standard) is the analytical standard of Galangin. This product is intended for research and analytical applications. Galangin (Norizalpinin) is an agonist/antagonist of the arylhydrocarbon receptor. Galangin (Norizalpinin) also shows inhibition of CYP1A1 activity.
    Galangin (Standard)
  • HY-148595

    Cytochrome P450 Cancer
    CYP1A1-IN-2 (Compound 14) is a competitive inhibitor of CYP1A1 (Ki: 1.4 μM). CYP1A1-IN-2 exhibits potent antimitotic activity and arrests cell in the G2/M phase. CYP1A1-IN-2 disrupts the microtubule and the cytoskeleton in CYP1A1-expressing breast cancer cells .
    CYP1A1-IN-2
  • HY-174333

    Bacterial Cytochrome P450 Infection Cardiovascular Disease
    CYP1A1-IN-1 (Compound 47) is a small-molecule cytochrome P4501A1 (CYP1A1) inhibitor. CYP1A1-IN-1 reduces the bacterial loads of methicillin-resistant Staphylococcus aureus (MRSA) and Acinetobacter baumannii by enhancing macrophage phagocytosis. CYP1A1-IN-1 is promising for research of sepsis caused by multidrug-resistant (MDR) bacteria .
    CYP1A1-IN-1

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