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Cytochrome P450

Cytochrome P450 (CYP) inhibitors act on heme enzymes that oxidize drugs, steroids and other lipophilic compounds. The name comes from the 450 nm absorption peak of a carbon monoxide-bound pigment, described in liver microsomes in 1964. Hepatic enzymes such as CYP3A4, CYP2C9 and CYP1A2 metabolize a large share of drugs and many environmental chemicals. Other members synthesize steroid hormones, among them CYP17A1, which is required for androgen production. The P450 system can also convert chemicals into toxic or carcinogenic metabolites, which links it closely to toxicology. Abiraterone inhibits CYP17A1, while clarithromycin and itraconazole serve as CYP3A4 inhibitors in drug-interaction studies. Alizarin is listed for its inhibition of enzymes in the CYP1 family.

3 Items

  • PROTAC CYP1B1 degrader-1
    Cat. No.
    A69764
    CAS No.
    2411389-67-6

    PROTAC CYP1B1 degrader-1

    PROTAC CYP1B1 Degrader-1 is a targeted degrader designed to selectively eliminate cytochrome P450 1B1 (CYP1B1), utilizing a α-naphthoflavone chimera derivative. This compound exhibits IC50 values of 95.1 nM for CYP1B1 and 9838.6 nM for CYP1A2, demonstrating its specificity in degrading CYP1B1. It serves as a valuable tool for investigating the role of CYP1B1 in prostate cancer and may aid in overcoming CYP1B1-mediated drug resistance in therapeutic applications.

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    1 mg
    $360.00
    5 mg
    $1,105.00
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  • PROTAC CYP1B1 degrader-2
    Cat. No.
    A69932
    CAS No.
    2836297-26-6

    PROTAC CYP1B1 degrader-2

    PROTAC CYP1B1 degrader-2 is a VHL E3 ligase-based degrader targeting CYP1B1, exhibiting a DC50 of 1.0 nM in A549/Taxol cells after 24 hours. This compound effectively inhibits the growth, migration, and invasion of cancer cells, making it a valuable tool for research into the therapeutic potential of targeting CYP1B1 in cancer treatment. Its unique mechanism of action offers insights into the modulation of protein levels in various biological contexts.

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  • YXG-158
    Cat. No.
    A84993
    CAS No.
    2952994-34-0

    YXG-158

    YXG-158 is an orally active androgen receptor (AR) degrader and CYP17A1 inhibitor. It exhibits AR degradation activity with a DC50 value of 1.28 μM and inhibits CYP17A1 with an IC50 value of 100 nM. This compound is particularly relevant for research applications focused on enzalutamide-resistant prostate cancer, providing a valuable tool for investigating therapeutic strategies in this context.

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