5.37983
Pantothenate Kinase Inhibitor
Synonym(s):
Pantothenate Kinase Inhibitor, 3-(2,4-Dimethylpyrido-[2ʹ,3ʹ:3,4]pyrazolo[1,5-a]pyrimidin-3-yl)-N-(3-(methylthio)phenyl)propanamide, PanK Inhibitor
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About This Item
Empirical Formula (Hill Notation):
C21H21N5O
Molecular Weight:
359.42
NACRES:
NA.77
UNSPSC Code:
12352200
Assay:
≥97% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
assay
≥97% (HPLC)
Quality Segment
form
solid
manufacturer/tradename
Calbiochem®
drug control
Új pszichoaktív anyag / New psychoactive substance (Hungary), 78/2022. (XII. 28.) BM rendelet
storage condition
OK to freeze, protect from light
color
orange
solubility
DMSO: 10 mg/mL
storage temp.
2-8°C
General description
A cell-permeable pyridopyrazolopyrimidine based compound that acts as a potent and reversible inhibitor of pantothenate kinase (IC50 = 70, 92 and 25 nM for PanK1β, PanK2 and PanK3, respectively; radiochemical assay, 2.5 mM [ATP]). Binds to ATP-PanK complex (apparent binding constant ~300 nM for ATP-PanK3) and exhibits mixed-type inhibition with respect to ATP and pantothenate. Shown to dose-dependently decrease [3H]pantothenate incorporation into coenzyme A (apparent IC50 = 900 nM in C3A cells) with negligible off-target toxicity (IC50 >56 µM in Hep-G2 cells).
Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
pantothenate kinase
pantothenate kinase
Reversible: yes
Target IC50: 70, 92 and 25 nM for PanK1&beta
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Sharma, L.K., et al. 2015. J. Med. Chem.58, 1563.
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)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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