| S6508 |
Mitapivat (AG-348)
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Mitapivat (AG-348) is an activator of a pyruvate kinase PKM2, an enzyme involved in glycolysis.
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International Immunopharmacology, 2025, 114841
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Proc Natl Acad Sci U S A, 2022, 119(40):e2210779119
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| S8279 |
(Rac)-Shikonin
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(±)-Shikonin, a potent and specific Pyruvate kinase M2 (PKM2) inhibitor, is a major component of zicao (purple gromwell, the dried root of Lithospermum erythrorhizon), a Chinese herbal medicine with various biological activities. It is also an inhibitor of TMEM16A chloride channel activity using cell-based fluorescent-quenching assay. Shikonin exerts an anti-inflammatory effect by inhibiting tumor necrosis factor-α (TNF-α) and prevents activation of nuclear factor-κB (NF-κB) pathway via proteasome inhibition.
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Signal Transduct Target Ther, 2025, 10(1):341
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J Exp Clin Cancer Res, 2025, 44(1):299
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Free Radic Biol Med, 2025, 237:65-75
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| S8616 |
PKM2-IN-1 (Compound 3k)
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PKM2 inhibitor(Compound 3K, PKM2-IN-1) displays PKM2 inhibitory activity with the IC50 value of 2.95 μM. The IC50 value for PKM1 is 4-5-fold higher than that for PKM2.
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Lipids Health Dis, 2025, 24(1):14
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J Cancer Res Clin Oncol, 2025, 151(3):126
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Elife, 2024, 12RP87674
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| S7928 |
DASA-58
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DASA-58 is a specific and potent Pyruvate kinase M2 (PKM2) activator.
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J Biol Chem, 2025, 301(5):108439
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Invest Ophthalmol Vis Sci, 2025, 66(15):23
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Cell Death Dis, 2023, 14(12):821
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| S7302 |
TEPP-46 (ML265)
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TEPP-46 (ML265, CID-44246499, NCGC00186528) is a potent activator of PKM2 in both biochemical (AC50 = 92 nM) and cell-based assays with high selectivity over PKM1, PKR and PKL.
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Theranostics, 2025, 15(8):3439-3461
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Free Radic Biol Med, 2025, 237:65-75
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Ecotoxicol Environ Saf, 2025, 294:118113
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| E1328 |
TP-1454
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TP-1454 is an activator of PKM2 with AC50 of 10 Nm in biochemical assays. This compound modulates tumor-immune responses by destabilizing T-regulatory cells.
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| E2829 |
Alkannin
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Alkannin is a potent and specific inhibitor of tumor-specific pyruvate kinase-M2 (PKM2), without inhibiting PKM1 and pyruvate kinase-L (PKL).
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| S5545 |
DL-Serine
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Serine is a non-essential amino acid and a natural ligand and allosteric activator of pyruvate kinase M2.
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