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550601 Pyruvate Kinase Activator - CAS 1346113-84-5 - Calbiochem

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

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

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

550601
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₅H₁₁ClF₂N₂O₃S

Products

Catalogue NumberPackaging Qty/Pack
550601-25MG Glass bottle 25 mg
Description
OverviewA cell-permeable and biologically stable (t1/2 = 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 (Km = 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; ACmax = 88%), displaying much reduced activity toward PKL (≤25% at 57 µM) and no effect toward PKM1 or PKR.
Catalogue Number550601
Brand Family Calbiochem®
SynonymsPKM2 Activator I, N-(4-Chloro-3-fluorophenyl)-7-fluoro-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
References
ReferencesWalsh, M.J., et al. 2011. Bioorg. Med. Chem. Lett. 21, 6322.
Product Information
FormWhite powder
Hill FormulaC₁₅H₁₁ClF₂N₂O₃S
Chemical formulaC₁₅H₁₁ClF₂N₂O₃S
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥98% by HPLC
Physicochemical Information
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
Catalogue Number GTIN
550601-25MG 04055977268867

Documentation

Pyruvate Kinase Activator - CAS 1346113-84-5 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

Pyruvate Kinase Activator - CAS 1346113-84-5 - Calbiochem Certificates of Analysis

TitleLot Number
550601

References

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

Revision02-October-2012 JSW
SynonymsPKM2 Activator I, N-(4-Chloro-3-fluorophenyl)-7-fluoro-2-oxo-1,2,3,4-tetrahydroquinoline-6-sulfonamide
DescriptionA cell-permeable (Papp x 106 = 9.38 and 7.91 cm/s, respectively, for "A-B" and "B-A" in Caco-2 permeability assay) and biologically stable (t1/2 = 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 (Km = 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; ACmax = 88%), displaying much reduced activity toward PKL (≤25% at 57 µM) and no effect toward PKM1 or PKR.
FormWhite powder
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₁₅H₁₁ClF₂N₂O₃S
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (100 mg/ml; clear, colorless solution)
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
ReferencesWalsh, M.J., et al. 2011. Bioorg. Med. Chem. Lett. 21, 6322.