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> DASA-58 [1203494-49-8]

DASA-58 [1203494-49-8]

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Référence HY-19330-1mL

Conditionnement : 10mM/1mL

Marque : MedChemExpress

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Description

DASA-58 is a potential pyruvate kinase isozyme (PKM2) allosteric activator. DASA-58 can be used for the research of metabolism and kinds of cancer[1].

In Vitro

DASA-58 (15 μM; 2 h) potentiates the antitumor effects of other metabolic stressors[1].
DASA-58 (15 μM; 24 h, 72 h) enhances pyruvate kinase activity in breast cancer cells without a clear effect on proliferation[1].
DASA-58 (30 μM, 60 μM; 0-72 h) enhances extracellular acidification and lactate levels in BCa cell lines and induce extracellular acidification levels in prostate cancer cell lines[1].
DASA-58 (15 μM, 30 μM; 0-72 h) affects respiration levels in BCa cells without an indication of mitochondrial damage[1].
DASA-58 (15 μM; 0-72 h) not rescues TXNIP levels in any combintion and mitochondrial inhibitors enhance PKM2 effects on activating AMPK signaling (T172 phosphorylation of AMPK) [1].
DASA-58 (15 μM; 0-72 h) leads to depletion in TXNIP levels independent of AMPK and ER signaling, and not through enhanced proteasomal degradation but rather depleted upstream glycolytic intermediates[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

DASA-58 Related Antibodies

Cell Viability Assay[1]

Cell Line: Five breast cancer cell lines (BCa cells)
(MDA MB 231, MDA MB 468, HCC 1443, T47-D, MCF7, LnCap, PC3, and DU145)
Concentration: 15 μM
Incubation Time: 2 h
Result: Could be exploited by other metabolic stressors.

Western Blot Analysis[1]

Cell Line: BCa cells
Concentration: 15 μM
Incubation Time: 24 h, 72 h
Result: Showed comparable PKM2 protein levels in five breast cancer cell lines, except HCC1443 cells and MDA MB 468 that showed the highest and lowest PKM2 protein levels, respectively.
Not changed PKM2 levels in five breast cancer cell lines but seemingly reduced TXNIP levels in cells expressing detectable TXNIP levels.
Masse moléculaire

453.53

Formule

C19H23N3O6S2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NC1=CC=CC(S(=O)(N2CCN(S(=O)(C3=CC=C(OCCO4)C4=C3)=O)CCC2)=O)=C1
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvant et solubilité
In Vitro: 

DMSO : 125 mg/mL (275.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2049 mL 11.0246 mL 22.0493 mL
5 mM 0.4410 mL 2.2049 mL 4.4099 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.59 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (4.59 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Pureté et documentation
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