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550602

PKM2 Activator II, DASA

Name: PKM2 Activator II, DASA
Brand: MM

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

UNSPSC Code:

12352200

NACRES:

NA.51

MDL number:

MFCD32671972

Assay:

≥99% (HPLC)

Form:

powder

Quality level:

100

Storage condition:

OK to freeze, protect from light

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Properties

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

InChI

1S/C18H18F2N2O6S2/c19-14-2-1-3-15(20)18(14)30(25,26)22-8-6-21(7-9-22)29(23,24)13-4-5-16-17(12-13)28-11-10-27-16/h1-5,12H,6-11H2

InChI key

SHWNKRPMUBFWKE-UHFFFAOYSA-N

Description

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

Preparation Note

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

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

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Class IIa Histone Deacetylases Drive Toll-like Receptor-Inducible Glycolysis and Macrophage Inflammatory Responses via Pyruvate Kinase M2.

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

Global Trade Item Number

SKU	GTIN
550602-10MG	04055977268874