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CYP1A1 and CYP1B1 inhibitor

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25

Inhibitors & Agonists

1

Fluorescent Dyes

2

Natural
Products

2

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B1234
    Octinoxate

    Octyl methoxycinnamate

    		 Environmental Pollutants Estrogen Receptor/ERR Androgen Receptor Cytochrome P450 Thyroid Hormone Receptor 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-W017113
    2-Mercaptobenzothiazole
    1 Publications Verification

    		 Environmental Pollutants Endogenous Metabolite 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-19340
    TMS
    Maximum Cited Publications
    9 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-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-101284
    DMU2105

    		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-157942
    CYP1B1-IN-7

    		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-159006
    CYP1B1 ligand 3

    		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-175836
    CYP1B1-IN-12

    		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-152079
    CYP1B1-IN-3

    		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-152196
    CYP1B1-IN-5

    		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-174425
    CYP1B1-IN-9

    		Cytochrome P450 Cancer
    CYP1B1-IN-9 is a highly selective and competitive CYP1B1 Inhibitor with IC50 values of 1.48 nM, > 100 μM, and > 80 μM for CYP1B1, CYP1A1, and CYP1A2, respectively. CYP1B1-IN-9 significantly inhibits the migration and invasion of A549/T cells. CYP1B1-IN-9 has the ability to resensitize Paclitaxel (HY-B0015)-resistant cells, and good metabolic stability and safety, and shows favorable pharmacokinetic parameters. CYP1B1-IN-9 can be used for the study of tumor-drug resistance .
    CYP1B1-IN-9
  • HY-126308
    (E/Z)-DMU2139

    		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-B1234S
    Octinoxate-13C,d3

    		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-175760
    CYP1B1-IN-11

    		Cytochrome P450 Cancer
    CYP1B1-IN-11 (Compound M2) is a selective CYP1B1 inhibitor with an IC50 of 0.00605 pM. CYP1B1-IN-11 effectively reverses DMBA (HY-W011845)-induced Paclitaxel (HY-B0015) resistance and CYP1B1-IN-11 suppresses tumor cells invasion and migration. CYP1B1-IN-11 can be used for tumor drug resistance research .
    CYP1B1-IN-11
  • HY-162051
    CYP1B1-IN-6

    		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-161403
    CYP1B1-IN-8

    		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
    CYP1B1-IN-1

    		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
    CYP1B1-IN-2

    		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-101285R
    DMU2139 (Standard)

    		Cytochrome P450 Reference Standards Cancer
    DMU2139 (Standard) is the analytical standard of DMU2139 (HY-101285). This product is intended for research and analytical applications. DMU2139 is a potent and specific CYP1B1 inhibitor, with IC50s of 9 nM and 795 nM for CYP1B1 and CYP1A1, respectively.
    DMU2139 (Standard)
  • HY-101284R
    DMU2105 (Standard)

    		Cytochrome P450 Reference Standards Cancer
    DMU2105 (Standard) is the analytical standard of DMU2105 (HY-101284). This product is intended for research and analytical applications. DMU2105 is a potent and specific CYP1B1 inhibitor, with IC50s of 10 nM and 742 nM for CYP1B1 and CYP1A1, respectively.
    DMU2105 (Standard)
  • HY-158429
    PROTAC CYP1B1 degrader-2

    		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
    (E/Z)-DMU2105

    		Cytochrome P450 Cancer
    (E/Z)-DMU2105 (Compound 7k) is a potent and highly selective CYP1B1 inhibitor. (E/Z)-DMU2105 inhibits human CYP1B1 enzyme bound to yeast-derived microsomes with an IC50 value of 10 nM. (E/Z)-DMU2105 also potently inhibits CYP1B1 expressed within ‘live’ recombinant yeast and human HEK293 kidney cells with an IC50 value of 63.65 nM. (E/Z)-DMU2105 can be used for the research of cancer, glaucoma, ischemia and obesity .
    (E/Z)-DMU2105
  • HY-W713284
    2-Ethylhexyl (E)-3-(4-(methoxy-d3)phenyl)acrylate

    		Isotope-Labeled Compounds Cytochrome P450 Estrogen Receptor/ERR Androgen Receptor Thyroid Hormone Receptor Endocrinology
    2-Ethylhexyl (E)-3-(4-(methoxy-d3)phenyl)acrylate is the deuterium labeled Octinoxate (HY-B1234). 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 .
    2-Ethylhexyl (E)-3-(4-(methoxy-d3)phenyl)acrylate
  • HY-181550A
    CYP1B1-IN-14 TFA

    		Cytochrome P450 P-glycoprotein Cancer
    CYP1B1-IN-14 TFA is a metabolically stable hCYP1B1 competitive inhibitor with an IC50 of 1.32 nM and a Ki of 0.72 μM. CYP1B1-IN-14 TFA reverses the resistance of cancer cells to Paclitaxel (HY-B0015). CYP1B1-IN-14 TFA acts synergistically with Paclitaxel (HY-B0015) to inhibit tumor growth in xenograft models without obvious toxicity. CYP1B1-IN-14 TFA can be used for the research of cancers such as paclitaxel-resistant lung cancer .
    CYP1B1-IN-14 TFA
  • HY-175554
    CYP1B1-IN-10

    		Cytochrome P450 Aryl Hydrocarbon Receptor Cancer
    CYP1B1-IN-10 (Compound 15C) is a highly selective human cytochrome P450 1B1 (hCYP1B1) inhibitor (IC50=0.11 μM). CYP1B1-IN-10 is promising for research of hormone-dependent tumors (e.g., breast and ovarian cancers) .
    CYP1B1-IN-10

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