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).
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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
pantothenate kinase
Reversible: yes
Target IC50: 70, 92 and 25 nM for PanK1&beta
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
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
Molecular Weight: 359.42. Empirical Formula: C21H21N5O. Assay: ≥. 97% (HPLC). Quality Level: 100. form: solid. manufacturer/tradename: Calbiochem®. . storage condition: OK to freeze, protect from light. color: orange. solubility: DMSO: 10 . mg/mL. storage temp.: 2-8°C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.- UPC:
- 51111758
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 5379830001