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Chemical Structure| 1203494-49-8 Chemical Structure| 1203494-49-8

Structure of DASA-58
CAS No.: 1203494-49-8

Chemical Structure| 1203494-49-8

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DASA-58 is a potential allosteric activator of pyruvate kinase isozyme (PKM2), useful for research in metabolism and various cancers.

Synonyms: ML-203; NCGC00185916

4.5 *For Research Use Only !

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Product Details of DASA-58

CAS No. :1203494-49-8
Formula : C19H23N3O6S2
M.W : 453.53
SMILES Code : NC1=CC=CC(S(=O)(N2CCN(S(=O)(C3=CC=C(OCCO4)C4=C3)=O)CCC2)=O)=C1
Synonyms :
ML-203; NCGC00185916
MDL No. :MFCD29472280
InChI Key :GMHIOMMKSMSRLY-UHFFFAOYSA-N
Pubchem ID :44543605

Safety of DASA-58

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
MDA MB 468 15 µM 72 hours No significant increase in pyruvate kinase activity Cancer Metab. 2021 Jan 22;9(1):5.
Bone marrow-derived macrophages (BMDMs) 50 µM 1 hour DASA-58 effectively reversed the FSTL1o/e-induced increase in glycolysis and reversed FSTL1o/e-induced macrophage M1 polarisation and NF-κB activation. Gut. 2022 Dec;71(12):2539-2550.
Bone marrow-derived macrophages (BMDMs) 50 µM 1 hour pretreatment followed by 24 hours LPS stimulation To evaluate the effect of DASA-58 on LPS-induced glycolysis and oxidative phosphorylation. Results showed that DASA-58 significantly inhibited LPS-induced glycolysis but had no significant effect on oxidative phosphorylation. Cell Metab. 2015 Jan 6;21(1):65-80.
RAW264.7 cells 20 µM 16 hours DASA-58 and NAC weakened the inhibition of IRD on the aerobic glycolysis while CUT129 and RO8191 partly reduced it. J Inflamm Res. 2021 Feb 5;14:341-354.
Peritoneal macrophages 50 µM 24 hours To evaluate the effect of DASA-58 on peritoneal macrophages, results showed similar effects as in BMDMs, with increased FASN and CD36 protein expression. J Lipid Res. 2020 Mar;61(3):351-364.
Bone marrow-derived macrophages (BMDMs) 50 µM 24 hours To evaluate the effect of DASA-58 on PKM2 activation, results showed that DASA-58 significantly downregulated LXR-α, ABCA1, and ABCG1 protein expression and augmented FASN and CD36 protein expression. J Lipid Res. 2020 Mar;61(3):351-364.
K562 cells 40 µM 24 hours DASA-58 significantly reversed the cytotoxicity of DHA on K562 cells Drug Des Devel Ther. 2020 May 27;14:2091-2100.
Gastric cancer organoids 50 µM 3 hours Size-exclusion chromatography analysis showed that DASA-58 treatment resulted in a shift of PKM2 protein into a more tetrameric configuration, especially in NTC organoids. Proc Natl Acad Sci U S A. 2022 Oct 4;119(40):e2123231119.
MCF7 15 µM 72 hours Increased pyruvate kinase activity without affecting cell survival Cancer Metab. 2021 Jan 22;9(1):5.
T47-D 15 µM 72 hours Increased pyruvate kinase activity without affecting cell survival Cancer Metab. 2021 Jan 22;9(1):5.
HCC 1443 15 µM 72 hours Increased pyruvate kinase activity without affecting cell survival Cancer Metab. 2021 Jan 22;9(1):5.
Mouse primary astrocytes 50 µM 30 min pretreatment followed by 12 hours stimulation Inhibited PKM2 nuclear translocation, reduced astrocyte glycolytic activity and proliferation Elife. 2024 Sep 12;13:RP98181.
Peritoneal cells (PECs) 50 µM 30 minutes pretreatment followed by 24 hours LPS stimulation To evaluate the effect of DASA-58 on LPS-induced pro-IL-1β expression. Results showed that DASA-58 significantly inhibited LPS-induced pro-IL-1β expression. Cell Metab. 2015 Jan 6;21(1):65-80.
CD4+ T cells 25 µM 48 hours To evaluate the effect of DASA-58 on TH17 cell differentiation, results showed that DASA-58 inhibited IL-17A production but promoted GM-CSF production. Sci Signal. 2020 Oct 27;13(655):eaay9217.
HNSCC cell lines (SCC-9, FaDu, Detroit 562, HN, BHY, SCC-154) 30 µM 5 hours or 16 hours To evaluate the effect of DASA-58 on the glycolytic rate of HNSCC cells. Results showed that DASA-58 increased basal and compensatory glycolysis in some cell lines (e.g., BHY, SCC-154) and decreased the oxygen consumption rate. Int J Mol Sci. 2022 Jan 11;23(2):775.
MDA MB 231 15 µM 72 hours Increased pyruvate kinase activity without affecting cell survival Cancer Metab. 2021 Jan 22;9(1):5.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
ICR mice LPS-induced acute lung injury model Oral 20–80 mg/kg Once daily for 5 days Inhibited LPS-induced acute lung injury and inflammatory response J Inflamm Res. 2021 Feb 5;14:341-354.
Mice LPS-induced sepsis model and Salmonella typhimurium infection model Intraperitoneal injection 50mg/kg Single dose, observed for 2 hours or 24 hours To evaluate the effect of DASA-58 in vivo on LPS and Salmonella typhimurium-induced inflammatory responses. Results showed that DASA-58 significantly inhibited LPS-induced IL-1β production while boosting IL-10 production, leading to impaired bacterial clearance. Cell Metab. 2015 Jan 6;21(1):65-80.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.20mL

0.44mL

0.22mL

11.02mL

2.20mL

1.10mL

22.05mL

4.41mL

2.20mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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