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).

3 Items

  • ACA-28
    Cat. No.
    A24158

    ACA-28

    ACA-28 (compound 2a) is a potent modulator of the ERK MAPK signaling pathway that exerts anticancer effects through a unique mechanism involving ERK hyperactivation. Rather than inhibiting ERK activity directly, ACA-28 induces sustained ERK activation, which paradoxically triggers apoptosis in cancer cells. It demonstrates selective cytotoxicity, inhibiting the growth of melanoma cells (SK-MEL-28) with an IC₅₀ of 5.3 μM, while showing lower toxicity toward normal human melanocytes (NHEM), with an IC₅₀ of 10.1 μM. ACA-28's ability to exploit ERK signaling dysregulation for selective induction of apoptosis makes it a promising candidate for further development in cancer therapy, particularly in ERK-dependent malignancies.

    5 mg
    $252.00
    10 mg
    $434.00
    All 4 sizes
  • AChE/Nrf2 modulator 1
    Cat. No.
    A78719

    AChE/Nrf2 modulator 1

    AChE/Nrf2 Modulator 1 is an orally active compound that targets both acetylcholinesterase (AChE) and the nuclear factor erythroid 2-related factor 2 (Nrf2). It exhibits significant Nrf2 inductive activity along with potent AChE inhibitory effects, presenting IC50 values of 0.07 μM for eel AChE and 0.38 μM for human AChE. This compound is primarily utilized in research focused on Alzheimer's disease, providing insights into neuroprotective mechanisms and cholinergic system modulation.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • VVD 065
    Cat. No.
    A79511

    VVD 065

    VVD 065 is an allosteric modulator of the Keap1-Cul3 E3 ligase complex that functions as a molecular glue. By activating KEAP1, VVD 065 promotes the degradation of NRF2, an essential regulator of antioxidant defenses. This compound has demonstrated the ability to inhibit tumor growth in non-small cell lung cancer and esophageal squamous cell carcinoma xenograft models. VVD 065 serves as a valuable tool for research on cancer biology and therapeutic strategies targeting oxidative stress responses.

    5 mg
    $690.00
    10 mg
    $1,135.00
    All 4 sizes

3 Items

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