research use only
Cat.No.S5545
| Related Targets | Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism |
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| Other PKM Inhibitors | PKM2 inhibitor(compound 3k) DASA-58 TEPP-46 (ML265) Mitapivat (AG-348) (±)-Shikonin TP-1454 ZIP Alkannin |
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In vitro |
Water : 8 mg/mL
DMSO
: Insoluble
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In vivo |
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| Molecular Weight | 105.09 | Formula | C3H7NO3 |
Storage (From the date of receipt) | 3 years -20°C powder |
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| CAS No. | 302-84-1 | -- | Storage of Stock Solutions |
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| Synonyms | N/A | Smiles | C(C(C(=O)O)N)O | ||
| In vitro |
The non-essential amino acid serine supports several metabolic processes that are crucial for the growth and survival of proliferating cells, including protein, amino acid and glutathione synthesis. As an important one-carbon donor to the folate cycle, serine contributes to nucleotide synthesis, methylation reactions and the generation of NADPH for antioxidant defence. Serine activates recombinant PKM2 with a half maximal activation concentration (AC50) of 1.3 mM. Isothermal titration calorimetry was used to determine the dissociation constant (Kd) of the PKM2-serine interaction as 0.20 mM. Serine can bind to and activate human PKM2 and that following serine deprivation, PKM2 activity in cells is reduced. This reduction in PKM2 activity shifts cells to a fuel-efficient mode where more pyruvate is diverted to the mitochondria and more glucose derived carbon is channelled into serine biosynthesis to support cell proliferation.
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References |
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(data from https://clinicaltrials.gov, updated on 2024-05-22)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
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| NCT05485155 | Recruiting | Eosinophilic Esophagitis |
Children''s Hospital Medical Center Cincinnati|CSL Behring|National Institutes of Health (NIH) |
March 1 2024 | Phase 2 |
| NCT05157217 | Recruiting | COVID-19 |
Cairo University|Misr International University |
December 15 2021 | -- |
| NCT05186285 | Unknown status | Healthy |
Keymed Biosciences Co.Ltd |
December 11 2021 | Phase 1 |
| NCT05098327 | Withdrawn | Prostate Cancer|Insulin Resistance|Diabetes Mellitus Type 2|Androgen Deficiency |
State University of New York at Buffalo|National Center for Advancing Translational Sciences (NCATS) |
August 1 2021 | Phase 3 |
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