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Tryptolinamide

Chemical Structure : Tryptolinamide

CAS No.: 260798-40-1

Tryptolinamide (TLAM)

Catalog No.: PC-49511Not For Human Use, Lab Use Only.

Tryptolinamide (TLAM) is a small-molecule compound that activates mitochondrial respiration in cybrids generated from patient-derived mitochondria and fibroblasts from patient-derived iPSCs, inhibits phosphofructokinase-1 (PFK1) with an ATP-uncompetitive and F6P-competitive manner (Ki=5.0 uM).

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    Biological Activity

    Tryptolinamide (TLAM) is a small-molecule compound that activates mitochondrial respiration in cybrids generated from patient-derived mitochondria and fibroblasts from patient-derived iPSCs, inhibits phosphofructokinase-1 (PFK1) with an ATP-uncompetitive and F6P-competitive manner (Ki=5.0 uM).
    TLAM attenuates 2DG toxicity and modulates cellular metabolism in cancer cells.
    TLAM activates mitochondrial respiration via the AMPK/fatty-acid oxidation pathway.
    TLAM inhibits the enzymatic activity of all PFK1 isoforms (PFKM, PFKP and PFKL) but not PFK2 (PFKFB3).
    TLAM ameliorate the defective phenotypes of iPSCs derived from patients with mitochondrial disease by inhibiting PFK1.

    Physicochemical Properties

    M.Wt 404.39
    Formula C21H19F3N2O3
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    3-(1-(trifluoromethyl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-2-carbonyl)bicyclo[2.2.1]hept-5-ene-2-carboxylic acid

    References

    1. Kobayashi H, et al. Nat Chem Biol. 2021 Mar;17(3):335-343.

    2. Kobayashi H, et al. Cancer Sci. 2023 Jan 5. doi: 10.1111/cas.15713.

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