| S8279 |
(Rac)-Shikonin
|
(±)-Shikonin是一种 Pyruvate kinase M2 (PKM2) 有效的、特异的抑制剂。它是紫草的主要成分，紫草是一种中草药，具有多种生物活性。在细胞荧光淬灭试验中，Shikonin也是TMEM16A氯离子通道的抑制剂。Shikonin 通过抑制 tumor necrosis factor-α (TNF-α) 发挥抗炎作用，并可通过抑制 proteasome 来阻止 nuclear factor-κB (NF-κB) 信号途径的激活。 |
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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)
|
PKM2 inhibitor (Compound 3K, PKM2-IN-1)是PKM2抑制剂，IC50为2.95 μM。对PKM1的IC50值比对PKM2的IC50值高4-5倍。 |
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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
|
DASA-58是一种特异性且有效的Pyruvate kinase M2 (PKM2)激活剂。
|
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International Journal of Biological Sciences, October 24, 2022, 6210-6225
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PLoS Pathogens, March 15, 2021, e1008866
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Aging (Albany NY), February 25, 2020, 3976-3992
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| S7302 |
TEPP-46 (ML265)
|
TEPP-46 (ML265, CID-44246499, NCGC00186528)是一种有效的PKM2激活剂，AC50为92 nM。相对于PKM1、PKR和PKL，对PKM2具有高选择性。 |
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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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| S6508 |
Mitapivat (AG-348)
|
Mitapivat (AG-348)是丙酮酸激酶PKM2的激活剂。PKM2参与糖酵解。 |
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International Immunopharmacology, 2025, 114841
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Proceedings of the National Academy of Sciences, 2022, e2210779119
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Proc Natl Acad Sci U S A, 2022, 119(40):e2210779119
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| E1328 |
TP-1454
|
TP-1454 是 PKM2 的激活剂，在生化测定中 AC50 为 10 Nm。TP-1454 通过影响T 调节细胞来调节肿瘤免疫反应。 |
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| E2829 |
Alkannin
|
Alkannin是一种肿瘤特异性M2型丙酮酸激酶(pyruvate kinase-M2, PKM2)的特异性有效抑制剂，但不抑制PKM1和丙酮酸激酶l (pyruvate kinase-L, PKL)。 |
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| S5545 |
DL-Serine
|
Serine is a non-essential amino acid and a natural ligand and allosteric activator of pyruvate kinase M2. |
|
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| S7928 |
DASA-58
|
DASA-58是一种特异性且有效的Pyruvate kinase M2 (PKM2)激活剂。
|
- International Journal of Biological Sciences, October 24, 2022, 6210-6225
- PLoS Pathogens, March 15, 2021, e1008866
- Aging (Albany NY), February 25, 2020, 3976-3992
|
|
| S7302 |
TEPP-46 (ML265)
|
TEPP-46 (ML265, CID-44246499, NCGC00186528)是一种有效的PKM2激活剂，AC50为92 nM。相对于PKM1、PKR和PKL，对PKM2具有高选择性。 |
- Theranostics, 2025, 15(8):3439-3461
- Free Radic Biol Med, 2025, 237:65-75
- Ecotoxicol Environ Saf, 2025, 294:118113
|
|
| S6508 |
Mitapivat (AG-348)
|
Mitapivat (AG-348)是丙酮酸激酶PKM2的激活剂。PKM2参与糖酵解。 |
- International Immunopharmacology, 2025, 114841
- Proceedings of the National Academy of Sciences, 2022, e2210779119
- Proc Natl Acad Sci U S A, 2022, 119(40):e2210779119
|
|
| E1328 |
TP-1454
|
TP-1454 是 PKM2 的激活剂，在生化测定中 AC50 为 10 Nm。TP-1454 通过影响T 调节细胞来调节肿瘤免疫反应。 |
|
|
| S5545 |
DL-Serine
|
Serine is a non-essential amino acid and a natural ligand and allosteric activator of pyruvate kinase M2. |
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