5.37983

Pantothenate Kinase Inhibitor

• 別名: 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
• 実験式（ヒル表記法）: C₂₁H₂₁N₅O
• 分子量: 359.42
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• アッセイ: ≥97% (HPLC)
• 品質水準: 100
• 形状: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: orange
• 溶解性: DMSO: 10 mg/mL
• 保管温度: 2-8°C

詳細

詳細

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.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
pantothenate kinase

Reversible: yes

Target IC₅₀: 70, 92 and 25 nM for PanK1&beta

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

その他情報

Sharma, L.K., et al. 2015. J. Med. Chem.58, 1563.

法的情報

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable