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Isoforms Recommended: CYP1
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CYP1A1

" in MedChemExpress (MCE) Product Catalog:

72

Inhibitors & Agonists

2

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19

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7

Isotope-Labeled Compounds

2

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-D0145
    7-Ethoxyresorufin
    1 Publications Verification

    Resorufin ethyl ether

    Cytochrome P450 NO Synthase Others
    7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochrome P450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase .
    7-Ethoxyresorufin
  • HY-N4205

    Cytochrome P450 Cancer
    Tetrahydropiperine, a cyclohexyl analogue of piperine, is the first natural aryl pentanamide from Piper longum . Tetrahydropiperine (compound 14) inhibits the cytochrome P450 (CYP) isoform CYP1A1/arylhydrocarbon hydroxylase (AHH; IC50=23 µM) .
    Tetrahydropiperine
  • 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-N2625A

    Cytochrome P450 Cancer
    Harmalol hydrochloride, a beta carboline alkaloid, presents in several medicinal plants such as Peganum harmala. Harmalol hydrochloride, main metabolite of Harmaline, significantly inhibits the dioxin-mediated induction of CYP1A1 at the transcriptional and posttranslational levels. Harmalol hydrochloride possesses antioxidant and hydroxyl radical-scavenging properties .
    Harmalol hydrochloride
  • HY-120377

    Others 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-RS03441

    Small Interfering RNA (siRNA) Others

    CYP1A1 Human Pre-designed siRNA Set A contains three designed siRNAs for CYP1A1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    CYP1A1 Human Pre-designed siRNA Set A
    CYP1A1 Human Pre-designed siRNA Set A
  • HY-E70468

    Cytochrome P450 Metabolic Disease
    Human CYP1A1, High-Reductase, a recombinant CYP1A1, is one of the most important cytochrome P450 (CYP) enzymes. Human CYP1A1, High-Reductase is involved in the metabolism of several genotoxic/carcinogenic environmental xenobiotics .
    Human CYP1A1,High-Reductase
  • HY-E70472

    Cytochrome P450 Metabolic Disease
    Human CYP1A1, High-Reductase, a recombinant CYP1A1, is one of the most important cytochrome P450 (CYP) enzymes. Human CYP1A1, High-Reductase is involved in the metabolism of several genotoxic/carcinogenic environmental xenobiotics .
    Human CYP1A1,Low-Reductase
  • 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-N2689

    (R)-6′,7′-DHB

    Cytochrome P450 Cancer
    (R)-6',7'-Dihydroxybergamottin ((R)-6′,7′-DHB) is a competitive inhibitor of human and rat CYP1A1 activity with Kis of 55 μM and 1.72 μM, respectively. (R)-6',7'-Dihydroxybergamottin has the potential for cancer research .
    (R)-6',7'-Dihydroxybergamottin
  • HY-N0922

    DL-Methysticin; (±)-Methystici

    Cytochrome P450 Neurological Disease
    Methysticin is a major kavalactone in kava extract to induce CYP1A1.
    Methysticin
  • 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-N4205R

    Cytochrome P450 Cancer
    Tetrahydropiperine (Standard) is the analytical standard of Tetrahydropiperine. This product is intended for research and analytical applications. Tetrahydropiperine, a cyclohexyl analogue of piperine, is the first natural aryl pentanamide from Piper longum . Tetrahydropiperine (compound 14) inhibits the cytochrome P450 (CYP) isoform CYP1A1/arylhydrocarbon hydroxylase (AHH; IC50=23 µM) .
    Tetrahydropiperine (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-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-N8382

    Cytochrome P450 Neurological Disease
    Chalepensin, a furanocoumarin, is a competitive CYP2A6 inhibitor. Chalepensin also inhibits human CYP1A1, CYP1A2, CYP2A13, CYP2C9, CYP2D6, CYP2E1, and CYP3A4 to different extents .
    Chalepensin
  • HY-N2625AR

    Cytochrome P450 Others
    Harmalol (hydrochloride) (Standard) is the analytical standard of Harmalol (hydrochloride). This product is intended for research and analytical applications. Harmalol hydrochloride, a beta carboline alkaloid, presents in several medicinal plants such as Peganum harmala. Harmalol hydrochloride, main metabolite of Harmaline, significantly inhibits the dioxin-mediated induction of CYP1A1 at the transcriptional and posttranslational levels. Harmalol hydrochloride possesses antioxidant and hydroxyl radical-scavenging properties .
    Harmalol (hydrochloride) (Standard)
  • 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-N0382
    Galangin
    Maximum Cited Publications
    11 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-N2194R

    Cytochrome P450 Cancer
    Bergamottin (Standard) is the analytical standard of Bergamottin. This product is intended for research and analytical applications. Bergamottin is a potent and competitive CYP1A1 inhibitor with a Ki of 10.703 nM.
    Bergamottin (Standard)
  • HY-148592

    Cytochrome P450 Cancer
    Antitumor agent-87 is a potent antitumor agent. Antitumor agent-87 shows a high affinity for CYP1A1 with a Ki value of 0.23 µM. Antitumor agent-87 shows antiproliferative activity. Antitumor agent-87 induces cell cycle arrest at the G2/M phase. Antitumor agent-87 show antitumoral activity .
    Antitumor agent-87
  • 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-E70476

    Cytochrome P450 Metabolic Disease
    Human CYP1B1, Low-Reductase, a recombinant CYP1B1, is a member of the CYP enzyme family. CYP1B1 is constitutively expressed at some extrahepatic tissues, metabolizes a variety of the same, mostly planar, substrates for CYP1A1 and CYP1A2 .
    Human CYP1B1,Low-Reductase
  • HY-B2015

    Cytochrome P450 Parasite Infection
    Carbosulfan inhibited relatively potently CYP3A4 and moderately CYP1A1/2 and CYP2C19 in pooled HLM (human livers).
    Carbosulfan
  • 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-B0822

    GABA Receptor Cytochrome P450 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-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)

    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-N0382S

    Isotope-Labeled Compounds Cytochrome P450 Autophagy Cancer
    Galangin- 13C3 is the 13C-labeled Galangin. Galangin (Norizalpinin) is an agonist/antagonist of the arylhydrocarbon receptor. Galangin (Norizalpinin) also shows inhibition of CYP1A1 activity.
    Galangin-13C3
  • HY-14225

    CRFR Cytochrome P450 Neurological Disease
    BMS-764459 is a CRF1 antagonist. BMS-764459 can be used for the research of neurological disorders such as depression and anxiety. BMS-764459 is also an atypical CYP1A1 inducer .
    BMS-764459
  • HY-152079

    Cytochrome P450 Cancer
    CYP1B1-IN-3 is a potent and selective CYP1B1 inhibitor with IC50 values of 6.6, 347.3, >10000 nM for CYP1B1, CYP1A1, CYP1A2, respectively. CYP1B1-IN-3 inhibits cell migration and invasion. CYP1B1-IN-3 inhibits P-gp, AKT/ERK, FAK/SRC, and EMT pathways .
    CYP1B1-IN-3
  • HY-118216R

    Fungal Cytochrome P450 Infection
    Bitertanol (Standard) is the analytical standard of Bitertanol. This product is intended for research and analytical applications. 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 (Standard)
  • HY-B1234

    Octyl methoxycinnamate

    Androgen Receptor Estrogen Receptor/ERR Thyroid Hormone Receptor Cytochrome P450 Metabolic Disease Endocrinology
    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
  • HY-B2015S

    Cytochrome P450 Parasite Infection
    Carbosulfan-d18 is the deuterium labeled Carbosulfan. Carbosulfan inhibited relatively potently CYP3A4 and moderately CYP1A1/2 and CYP2C19 in pooled HLM (human livers). Carbosulfan activation is predominantly catalyzed in humans by CYP3A4.
    Carbosulfan-d18
  • HY-118474

    NSC 721648

    Aryl Hydrocarbon Receptor Cytochrome P450 Cancer
    GW 610 (NSC 721648), an antitumor agent, is a potent AhR ligand with a Ki of 6.8 nM. GW 610 induces CYP1A1 expression in MCF-7 cells. GW 610 shows potent and selective anticancer activity against lung, colon, and breast cancer cell lines .
    GW 610
  • HY-D0145S

    Resorufin ethyl ether-d5

    Isotope-Labeled Compounds Cytochrome P450 NO Synthase Others
    7-Ethoxyresorufin-d5 is deuterium labeled 7-Ethoxyresorufin. 7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochrome P450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase[1][2].
    7-Ethoxyresorufin-d5
  • HY-N6264R

    Aryl Hydrocarbon Receptor ERK Metabolic Disease
    26-Deoxyactein (Standard) is the analytical standard of 26-Deoxyactein. This product is intended for research and analytical applications. 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 (Standard)
  • 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-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-B1234S

    Cytochrome P450 Thyroid Hormone Receptor Androgen Receptor Estrogen Receptor/ERR Isotope-Labeled Compounds Metabolic Disease Endocrinology
    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-13C,d3
  • HY-W775354

    1,2,3,4,7,8-HxCDF

    Cytochrome P450 Aryl Hydrocarbon Receptor Others
    1,2,3,4,7,8-Hexachlorodibenzofuran (1,2,3,4,7,8-HxCDF) promotes the gene expressions of CYP1A1, CYP1B1, and aryl hydrocarbon receptor repressor (AhRR) in human peripheral blood lymphocytes (PBLs). 1,2,3,4,7,8-Hexachlorodibenzofuran activates the ethoxyresorufin-Odeethylase, achieves 20% of the maximum response caused by TCDD with a BMR20TCDD of 0.115-0.143 nM .
    1,2,3,4,7,8-Hexachlorodibenzofuran
  • HY-W517092

    1,2,3,4,7,8,9-HpCDF

    Aryl Hydrocarbon Receptor Cytochrome P450 Metabolic Disease Inflammation/Immunology
    1,2,3,4,7,8,9-Heptachlorodibenzofuran (1,2,3,4,7,8,9-HpCDF) is a compound that induces the expression of CYP1A1 and CYP1B1 genes in human peripheral blood lymphocytes, while also promoting the expression of the aryl hydrocarbon receptor repressor (AhRR). 1,2,3,4,7,8,9-Heptachlorodibenzofuran can increase ethoxyresorufin-O-deethylase (EROD) activity in isolated human peripheral blood lymphocytes in a concentration-dependent manner, which serves as a marker of CYP1A1 activity. Furthermore, 1,2,3,4,7,8,9-Heptachlorodibenzofuran exhibits immunosuppressive effects by reducing the number of splenic plaque-forming cells in mice and increasing aryl hydrocarbon hydroxylase (AHH) activity in liver microsomes of mice injected with sheep red blood cells. 1,2,3,4,7,8,9-Heptachlorodibenzofuran can be used in research in the fields of immunology, metabolic diseases, and environmental toxicology .
    1,2,3,4,7,8,9-Heptachlorodibenzofuran
  • HY-124421

    NSC-703786

    Aryl Hydrocarbon Receptor Others
    5F-203 (NSC-703786) is a cytotoxic molecule that forms DNA adducts and cell cycle arrest. 5F-203 induces aryl hydrocarbon receptor (AhR) signaling and elevates expression of CYP1A1. 5F-203 also increases the levels of reactive oxygen species as well as activates JNK, ERK, and p38 .
    5F-203
  • HY-B0822R

    GABA Receptor Cytochrome P450 Apoptosis Neurological Disease
    Fipronil (Standard) is the analytical standard of Fipronil. This product is intended for research and analytical applications. 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 (Standard)
  • 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-W017113

    Endogenous Metabolite Aryl Hydrocarbon Receptor Metabolic Disease
    2-Mercaptobenzothiazole is an activator of the aryl hydrocarbon receptor (AhR) , inhibiting thyroid hormone synthesis and dopamine beta-hydroxylase activity . 2-Mercaptobenzothiazole promotes bladder cancer cell invasion by altering the conformation of the AhR ligand binding domain (LBD), activating AhR transcription, and upregulating the mRNA and protein expression of target genes CYP1A1 and CYP1B1 . 2-Mercaptobenzothiazole inhibits thyroid peroxidase (TPO) with an IC50 value of 11.5 μM, induces histological changes such as follicular cell hypertrophy in Xenopus laevis tadpoles, delaying metamorphosis . 2-Mercaptobenzothiazole increases chromosomal aberrations and sister chromatid exchanges (SCEs) in Chinese hamster ovary (CHO) cells, and enhances carcinogenicity in F344/N rats . 2-Mercaptobenzothiazole inhibits norepinephrine synthesis in mice and completely blocks the conversion of exogenous dopamine to norepinephrine in rat cardiomyocytes .
    2-Mercaptobenzothiazole
  • HY-W762015

    1,2,3,6,7,8-HxCDF

    Cytochrome P450 Cancer
    1,2,3,6,7,8-Hexachlorodibenzofuran (1,2,3,6,7,8-HxCDF) is a dioxin-like polychlorinated dibenzofuran (PCDF). 1,2,3,6,7,8-Hexachlorodibenzofuran induces expression of the genes encoding aryl hydrocarbon hydroxylase (AHH) and ethoxyresorufin-O-deethylase (EROD) in H-4-II-E rat hepatoma cells (EC50s = 1.47 and 1.24 nM, respectively). 1,2,3,6,7,8-Hexachlorodibenzofuran reduces weight, induces thymic atrophy, and induces the expression of genes encoding the cytochrome P450 (CYP) isoform CYP1A1 and 4-chlorobiphenyl hydroxylase in rats (EC50s = 3.2, 0.9, 0.35, and 0.21 µmol/kg, respectively) .
    1,2,3,6,7,8-Hexachlorodibenzofuran
  • 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-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-146393

    PROTACs Cytochrome P450 Cancer
    PROTAC CYP1B1 degrader-1 (Compound 6C), a α-naphthoflavone chimera derivative, is able to eliminate cytochrome P450 (CYP)1B1-mediated agent resistance via targeted CYP1B1 degradation, with IC50s of 95.1 and 9838.6 nM for CYP1B1 and CYP1A2, respectively. PROTAC CYP1B1 degrader-1 can be used for the research of CYP1B1-overexpressing prostate cancer .
    PROTAC CYP1B1 degrader-1

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