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504537 PKM2 Activator III - CAS 1260074-86-9 - Calbiochem

PKM2 Activator III - CAS 1260074-86-9 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: Pyruvate Kinase M2 Activator III, N-(4-(4-(2-Methoxyphenyl)piperazine-1-carbonyl)phenyl)quinoline-8-sulfonamide

Primary Target: PKM2
504537
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Áttekintés

Replacement Information

Kulcsspecifikációk táblázata

CAS #Empirical Formula
1260074-86-9C₂₇H₂₆N₄O₄S

Products

KatalógusszámCsomagolás Menny./csomag
5.04537.0001 Üvegpalack 10 mg
Description
OverviewA cell-permeable quinoline-sulfonamide that acts as a potent allosteric PKM2 activator both in cell-free enzymatic assays (AC50 = 17 nM with 40 ng PKM2/200 µL) and in cultures (AC50 = 45 nM in A549 cells) via a high affinity, 2:1 stoichiometric binding, effectively locking PKM2 in an active tetrameric state resistant to known intracellular negative regulators of FBP-activated PKM2 tetramer. PKM2 stimulation by compound treatment is shown to result in decreased serine biosynthesis (by 56%; 500 nM for 24 h) with concomitant increase in serine influx as a compensating mechanism for maintaining cellular serine level necessary for supporting A549 proliferation. Simultaneous PKM2 activation and culture serine withdrawal results in cytostatic A549 growth arrest, but not apoptosis.
Catalogue Number504537
Brand Family Calbiochem®
SynonymsPyruvate Kinase M2 Activator III, N-(4-(4-(2-Methoxyphenyl)piperazine-1-carbonyl)phenyl)quinoline-8-sulfonamide
References
ReferencesKung, C., et al. 2012. Chem. Biol. 19, 1187.
Product Information
CAS number1260074-86-9
FormOff-white powder
Hill FormulaC₂₇H₂₆N₄O₄S
Chemical formulaC₂₇H₂₆N₄O₄S
ReversibleN
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetPKM2
Purity≥99% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Katalógusszám GTIN
5.04537.0001 04055977244861

Documentation

PKM2 Activator III - CAS 1260074-86-9 - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

References

Hivatkozások áttekintése
Kung, C., et al. 2012. Chem. Biol. 19, 1187.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision09-August-2013 JSW
SynonymsPyruvate Kinase M2 Activator III, N-(4-(4-(2-Methoxyphenyl)piperazine-1-carbonyl)phenyl)quinoline-8-sulfonamide
DescriptionA cell-permeable quinoline-sulfonamide that acts as a potent allosteric PKM2 activator both in cell-free enzymatic assays (AC50 = 17 nM with 40 ng recombinant PKM2/200 µL) and in cultures (AC50 = 45 nM in A549 cells) via a high affinity (no dissociation in >1.5 h), 2:1 (compound to PKM2 tetramer) stoichiometric binding, effectively locking PKM2 in an active tetrameric state that is resistant to known intracellular negative regulators of PKM2 tetramer induced by the natural activator FBP (fructose 1,6-bisphosphate). PKM2 stimulation by compound treatment is shown to result in decreased serine biosynthesis (by 56%; 500 nM for 24 h) with concomitant increase in serine influx as a compensating mechanism for maintaining cellular serine level necessary for supporting A549 proliferation. Simultaneous PKM2 activation by drug treatment and culture serine withdrawal results in depletion of cellular serine pool (by ~70% in 24 h) and induction of cytostatic A549 growth arrest (by 56%; 72 h 1 µM drug treatment in BME + NEAA - Ser), but not apoptosis. Serine-dependent proliferation inhibition upon PKM2 activation is reported to be cell-specific, while it is observed in A549 and H460 cultures, SW480 and H522 are not affected.
FormOff-white powder
Intert gas (Yes/No) Packaged under inert gas
CAS number1260074-86-9
Chemical formulaC₂₇H₂₆N₄O₄S
Structure formulaStructure formula
Purity≥99% by HPLC
SolubilityDMSO (5 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesKung, C., et al. 2012. Chem. Biol. 19, 1187.