We use analytics and advertising cookies, which you can accept or reject; see our privacy policy.

Current choice:

Keap1-Nrf2

Keap1-Nrf2 pathway activators and inhibitors act on the master regulator of the cellular antioxidant response. Kelch-like ECH-associated protein 1 (Keap1) binds nuclear factor erythroid 2-related factor 2 (Nrf2) and keeps it from accumulating in the nucleus. In 1997, Nrf2 and small Maf proteins were shown to induce detoxifying genes through antioxidant response elements (AREs). Electrophiles modify Keap1 cysteines, releasing Nrf2 to induce genes such as NAD(P)H quinone dehydrogenase 1 (NQO1). Activators include sulforaphane, an isothiocyanate isolated from broccoli in 1992, and dimethyl fumarate, oltipraz and the triterpenoid omaveloxolone. ML-385 inhibits Nrf2 itself, while dicoumarol blocks the downstream enzyme NQO1. Related oxidative stress tools are listed under Reactive Oxygen Species (ROS).

2 Items

  • Nrf2 degrader 1
    Cat. No.
    A24725
    CAS No.
    3025286-00-1

    Nrf2 degrader 1

    Nrf2 Degrader 1 is a potent PROTAC that targets and degrades Nrf2, a key regulator of antioxidant response and cell survival. This compound demonstrates significant anticancer activity, effectively inhibiting the growth of A549 and LK-2 cancer cell lines with IC50 values of 100 nM and 40 nM, respectively. It is a valuable tool for studying the role of Nrf2 in cancer biology and has potential applications in therapeutic development.

    In stock View Details
    5 mg
    $695.00
    10 mg
    $1,135.00
    All 5 sizes
  • VVD-130037
    Cat. No.
    A79492
    CAS No.
    3034880-93-5

    VVD-130037

    Synonyms: BAY-3605349

    VVD-130037 is a covalent molecular glue and allosteric degrader of NRF2, targeting the KEAP1 protein. By binding to KEAP1, it enhances the formation of the KEAP1-CUL3 E3 ligase complex, leading to increased ubiquitination and subsequent degradation of NRF2. This compound demonstrates KEAP1 target-binding activity in both in vitro assays and mouse models, making it a useful tool in research involving NRF2-dependent cancers, solid tumors with KEAP1 mutations, and advanced solid tumors.

    In stock View Details
    1 mg
    $50.00
    5 mg
    $130.00
    All 6 sizes

2 Items

Added to your cart

View Cart Checkout

    Loading...