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CYP1A1 and CYP1B1 inhibitor

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17

Inhibitors & Agonists

1

Fluorescent Dye

2

Natural
Products

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • 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-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-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-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-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-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-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-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-161403

    Cytochrome P450 Cancer
    CYP1B1-IN-8 (Compound 14b) is a CYP1B1 inhibitor (IC50: 4.14 × 10 –5 nM). CYP1B1-IN-8 reduces the resistance in A549 cells to Paclitaxel (HY-B0015), and inhibits cell migration and invasion .
    CYP1B1-IN-8
  • HY-150557

    Cytochrome P450 Cancer
    CYP1B1-IN-1 (Compound 9e) is a selective cytochrome P450 1B1 (CYP1B1) inhibitor with an IC50 of 0.49 nM .
    CYP1B1-IN-1
  • HY-150558

    Cytochrome P450 Cancer
    CYP1B1-IN-2 (compound 9j) is a potent and selective CYP1B1 (cytochrome P450 1B1) inhibitor, with an IC50 of 0.52 nM .
    CYP1B1-IN-2
  • 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-158429

    PROTACs Cytochrome P450 Cancer
    PROTAC CYP1B1 degrader-2 (compound PV2) is a von Hippel-Landau (VHL) E3 ligase-based CYP1B1 degrader with the DC50 of 1.0 nM at 24 h in A549/Taxol cells. PROTAC CYP1B1 degrader-2 inhibits growth, migration, and invasion of A549/Taxol cell(Sturcture Note:(Blue: VHL ligand (HY-112078), Black: linker (HY-W007700), Pink: CYP1B1 ligand (HY-159006) .
    PROTAC CYP1B1 degrader-2
  • HY-101284A

    Others Cancer
    (E/Z)-DMU2105 is the E/Z isomer of DMU2105 (HY-101284). DMU2105 is a CYP1B1 inhibitor .
    (E/Z)-DMU2105
  • HY-126308

    Cytochrome P450 Cancer
    (E/Z)-DMU2139 (Compound 180) is the E/Z isomer of DMU2139 (HY-101285). (E/Z)-DMU2139 is a potent and specific CYP1B1 inhibitor (IC50: 4 nM) .
    (E/Z)-DMU2139
  • 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

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