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550601

Pyruvate Kinase Activator

Name: Pyruvate Kinase Activator
Brand: MM

The Pyruvate Kinase Activator controls the biological activity of Pyruvate Kinase. This small molecule/inhibitor is primarily used for Activators/Inducers applications.

Synonym(s):

Pyruvate Kinase Activator, PKM2 Activator I, N-(4-Chloro-3-fluorophenyl)-7-fluoro-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide

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About This Item

Empirical Formula (Hill Notation):

C₁₅H₁₁ClF₂N₂O₃S

CAS Number:

1346113-84-5

Molecular Weight:

372.77

MDL number:

MFCD35064636

UNSPSC Code:

41106200

NACRES:

NA.77

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

Storage condition:

OK to freeze, protect from light

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Properties

Quality Level

100

assay

≥98% (HPLC)

form

powder

manufacturer/tradename

Calbiochem^®

storage condition

OK to freeze, protect from light

color

white

solubility

DMSO: 100 mg/mL, clear, colorless

shipped in

ambient

storage temp.

2-8°C

SMILES string

FC1=CC2=C(CCC(N2)=O)C=C1S(NC3=CC=C(F)C(Cl)=C3)(=O)=O

InChI

1S/C15H11ClF2N2O3S/c16-10-6-9(2-3-11(10)17)20-24(22,23)14-5-8-1-4-15(21)19-13(8)7-12(14)18/h2-3,5-7,20H,1,4H2,(H,19,21)

InChI key

VLIHQHQPGAWJCM-UHFFFAOYSA-N

Description

General description

A cell-permeable (P_app x 10⁶ = 9.38 and 7.91 cm/s, respectively, for "A-B" and "B-A" in Caco-2 permeability assay) and biologically stable (t_1/2 = 277.2 and 117.5 min., respectively, using human and mouse liver microsome preparation) tetrahydroquinoline-sulfonamide that enhances the donor PEP (phosphoenolpyruvate), but not the acceptor ADP, substrate affinity toward PK (pyruvate kinase) isoform PKM2 (K_m = 0.4 vs. 1.9 mM with or without 10 µM activator) and acts as a potent PKM2-selective activator (AC₅₀ = 90 nM using rhPKM2; AC_max = 88%), displaying much reduced activity toward PKL (≤25% at 57 µM) and no effect toward PKM1 or PKR.

A cell-permeable and biologically stable (t_1/2 = 277.2 and 117.5 min., respectively, in human and mouse liver microsome preparation) tetrahydroquinoline-sulfonamide that enhances the donor PEP, but not the acceptor ADP, substrate affinity toward pyruvate kinase isoform PKM2 (K_m = 0.4 vs. 1.9 mM with or without 10 µM activator) and acts as a potent PKM2-selective activator (AC₅₀ = 90 nM using rhPKM2; AC_max = 88%), displaying much reduced activity toward PKL (≤25% at 57 µM) and no effect toward PKM1 or PKR.

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

Walsh, M.J., et al. 2011. Bioorg. Med. Chem. Lett.21, 6322.

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