Protein Disulfide Isomerase (PDI)

PDI inhibitors target the endoplasmic reticulum enzyme that forms and reshuffles protein disulfide bonds. Protein disulfide isomerase (PDI) catalyzes thiol-disulfide exchange while secreted and membrane proteins fold in the endoplasmic reticulum (ER). Its sequence, reported in 1985, revealed two regions resembling thioredoxin, each with a redox-active cysteine pair. The enzyme is studied in cancer cell survival, thrombus formation and protein misfolding disorders. PACMA 31 was described in 2012 as an irreversible inhibitor that binds the active-site cysteines of PDI. LOC14, reported in 2015, binds PDI reversibly, shifts it to an oxidized state and protected neurons in disease models. ML359, E64FC26 and PDI-IN-1 are further small-molecule inhibitors of PDI in the set.

9 Items

  • 3-Methyltoxoflavin
    Cat. No.
    A19466

    3-Methyltoxoflavin

    Synonyms: GNF-Pf-2272

    3-Methyltoxoflavin is a potent Protein disulfide isomerase (PDI) inhibitor, with an IC50 of 170 nM.

    1 mg
    $40.00
    5 mg
    $100.00
    All 7 sizes
  • LOC14
    Cat. No.
    A20491

    LOC14

    LOC14 is a potent Protein disulfide isomerase (PDI) inhibitor with EC50 and Kd values of 500 nM and 62 nM, respectively.

    5 mg
    $40.00
    10 mg
    $70.00
    All 5 sizes
  • E64FC26
    Cat. No.
    A30244

    E64FC26

    E64FC26 is a potent inhibitor of the protein disulfide isomerase (PDI) family, demonstrating IC50 values of 1.9 μM for PDIA1, 20.9 μM for PDIA3, 25.9 μM for PDIA4, 16.3 μM for TXNDC5, and 25.4 μM for PDIA6. This compound exhibits significant anti-myeloma activity, making it a valuable tool for cancer research focused on targeting PDI-related pathways. Its ability to modulate protein folding processes positions E64FC26 as a promising candidate in studies aimed at understanding the role of PDIs in various diseases.

    1 mg
    $130.00
    5 mg
    $325.00
    All 6 sizes
  • PDI-IN-5
    Cat. No.
    A53751

    PDI-IN-5

    PDI-IN-5 is an allosteric-covalent inhibitor targeting protein disulfide isomerase (PDI), featuring a 2-chloro-pyrrolopyrimidin-4-one scaffold with an IC50 of 0.4 μM. This compound demonstrates selectivity for ERp57 and GPX4, and has been shown to inhibit glioblastoma cell proliferation. PDI-IN-5 is valuable for research focused on glioblastoma and studies involving protein folding and oxidative stress responses.

    Out of stock

    All 3 sizes
  • PACMA 31
    Cat. No.
    A56846

    PACMA 31

    PACMA 31 is an irreversible inhibitor of protein disulfide isomerase (PDI) that demonstrates an IC50 of 10 μM. By forming covalent bonds with the active site cysteines of PDI, PACMA 31 effectively suppresses ovarian tumor growth while preserving the integrity of normal tissues. Additionally, PACMA 31 serves as a versatile click chemistry reagent, featuring an alkyne group that facilitates copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, making it suitable for various biochemical applications.

    2 mg
    $25.00
    5 mg
    $40.00
    All 7 sizes
  • ML359
    Cat. No.
    A56849

    ML359

    ML359 is a selective and reversible inhibitor of protein disulfide isomerase (PDI), with an IC50 of 250 nM. This compound effectively disrupts PDI activity, leading to an inhibition of thrombus formation in vivo. ML359 is valuable in research related to cardiovascular diseases and the modulation of protein folding processes.

    1 mg
    $65.00
    5 mg
    $160.00
    All 6 sizes
  • PDI-IN-3
    Cat. No.
    A56850

    PDI-IN-3

    PDI-IN-3 is a potent inhibitor of protein disulfide isomerase (PDI), a key enzyme involved in protein folding and redox regulation. This compound has been shown to disrupt cellular viability, making it a valuable tool for studying PDI's role in cancer biology and cellular stress responses. Its application in research can help elucidate the mechanisms underlying PDI-related pathways and potential therapeutic interventions.

    1 mg
    $90.00
    5 mg
    $225.00
    All 3 sizes
  • PDI-IN-1
    Cat. No.
    A56853

    PDI-IN-1

    PDI-IN-1 is a cell-permeable inhibitor of human protein disulfide isomerase (PDI), exhibiting an IC50 of 1.7 μM. With demonstrated anti-cancer activity, PDI-IN-1 serves as a valuable tool for research applications targeting cancer biology and the role of protein misfolding in tumor development. It is suitable for in vitro studies aimed at elucidating the therapeutic potential of PDI inhibition in cancer treatment.

    1 mg
    $100.00
    5 mg
    $510.00
    All 5 sizes
  • Dicentrinone
    Cat. No.
    B21847

    Dicentrinone

    Dicentrinone is an orally active inhibitor of Protein Disulfide Isomerase (PDI), with an IC50 value of 43.95 μM. By directly binding to PDI, Dicentrinone effectively suppresses cell proliferation and reduces the viability of cancer cells. Additionally, it exhibits anti-inflammatory and antioxidant properties through the inhibition of leukocyte migration, reduction of plasma leakage and paw edema, and scavenging of free radicals. Dicentrinone is a valuable tool in the study of hepatoma, rheumatism, and arthritis.

    Out of stock

    All 3 sizes

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