PKM
Inhibitory Selectivity
Isoform-specific Inhibitors
PKM Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S8279 |
Shikonin (C.I. 75535)Shikonin (C.I. 75535, Anchusin, Anchusa acid, Alkanna Red, Isoarnebin 4, NSC 252844), 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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| S8616 |
PKM2 inhibitor(compound 3k)PKM2 inhibitor(Compound 3K) 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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| S7302 |
TEPP-46 (ML265)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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| S7928 |
DASA-58DASA-58 is a specific and potent Pyruvate kinase M2 (PKM2) activator. |
Surface staining of total thymocytes from LckCre/Sin1fl/fl mice treated with vehicle or the PKM2 activator DASA-58. Upper panels are CD4 and CD8 staining. Lower panels are gated on the CD4 and CD8 DN subset for further CD44 and CD25 expression analyses. Numbers in the panels show the relative percentage of cells in that area.
|
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S8279 |
Shikonin (C.I. 75535)Shikonin (C.I. 75535, Anchusin, Anchusa acid, Alkanna Red, Isoarnebin 4, NSC 252844), 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. |
||
| S8616 |
PKM2 inhibitor(compound 3k)PKM2 inhibitor(Compound 3K) 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. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S7302 |
TEPP-46 (ML265)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. |
||
| S7928 |
DASA-58DASA-58 is a specific and potent Pyruvate kinase M2 (PKM2) activator. |
Surface staining of total thymocytes from LckCre/Sin1fl/fl mice treated with vehicle or the PKM2 activator DASA-58. Upper panels are CD4 and CD8 staining. Lower panels are gated on the CD4 and CD8 DN subset for further CD44 and CD25 expression analyses. Numbers in the panels show the relative percentage of cells in that area.
|
