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550602

Sigma-Aldrich

PKM2 Activator II, DASA

The PKM2 Activator II, DASA modulates the biological activity of PKM2. This small molecule/inhibitor is primarily used for Biochemicals applications.

Synonym(s):

PKM2 Activator II, DASA, Pyruvate Kinase M2 Activator II, 1-(2,6-Difluorophenylsulfonyl)-4-(2,3-dihydrobenzo[b][1,4]dioxin-6-ylsulfonyl)piperazine

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About This Item

Empirical Formula (Hill Notation):
C18H18F2N2O6S2
CAS Number:
1186654-00-1
Molecular Weight:
460.47
MDL number:
MFCD32671972
UNSPSC Code:
12352200
NACRES:
NA.51

Quality Level

100

Assay

≥99% (HPLC)

form

powder

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

white

solubility

DMSO: 50 mg/mL

shipped in

ambient

storage temp.

2-8°C

SMILES string

FC(C=CC=C1F)=C1S(N2CCN(S(C3=CC4=C(OCCO4)C=C3)(=O)=O)CC2)(=O)=O

General description

A cell-permeable diarylsulfonamide (DASA) compound that acts as a potent and selective activator of tumor-specific M2 isozyme of pyruvate kinase (PKM2; AC50 = 65 nM). Pretreatment of A549 (adenocarcinomic human alveolar basal epithelial cells) with DASA-10 (~10 µM) prevents hydrogen peroxide, diamide, and hypoxia-induced inactivation of PKM2. DASA treatment is shown to cause a diminution in cellular glutathione levels, and higher oxidative stress-induced cell death.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Anastasiou, D., et al. 2011. Science334, 1278.
Boxer, M.B., et al. 2010. J. Med. Chem.53, 1048.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Elizabeth K Wiese et al.
Nature metabolism, 3(7), 954-968 (2021-07-07)
Pharmacological activation of the glycolytic enzyme PKM2 or expression of the constitutively active PKM1 isoform in cancer cells results in decreased lactate production, a phenomenon known as the PKM2 paradox in the Warburg effect. Here we show that oxaloacetate (OAA)
Kaustav Das Gupta et al.
Cell reports, 30(8), 2712-2728 (2020-02-27)
Histone deacetylases (HDACs) drive innate immune cell-mediated inflammation. Here we identify class IIa HDACs as key molecular links between Toll-like receptor (TLR)-inducible aerobic glycolysis and macrophage inflammatory responses. A proteomic screen identified the glycolytic enzyme pyruvate kinase M isoform 2

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