Home Metabolism PKM activator DL-Serine

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DL-Serine PKM activator

Cat.No.S5545

Serine is a non-essential amino acid and a natural ligand and allosteric activator of pyruvate kinase M2.
DL-Serine PKM activator Chemical Structure

Chemical Structure

Molecular Weight: 105.09

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Quality Control

Batch: S554501 Water]8 mg/mL]false]DMSO]Insoluble]false]]]false Purity: 98%
98

Chemical Information, Storage & Stability

Molecular Weight 105.09 Formula

C3H7NO3

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 302-84-1 -- Storage of Stock Solutions

Synonyms N/A Smiles C(C(C(=O)O)N)O

Solubility

In vitro
Batch:

Water : 8 mg/mL

DMSO : Insoluble
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

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[2]. 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[1].
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
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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