550601
Pyruvate Kinase Activator
The Pyruvate Kinase Activator controls the biological activity of Pyruvate Kinase. This small molecule/inhibitor is primarily used for Activators/Inducers applications.
別名:
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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この商品について
実験式（ヒル表記法）:
C15H11ClF2N2O3S
CAS番号:
分子量:
372.77
MDL number:
UNSPSC Code:
41106200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
powder
Storage condition:
OK to freeze, protect from light
Quality Segment
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
General description
A 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.
A 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.
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)
保管分類
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
適用法令
試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。
550601-MG: + 550601-25MG:
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