Pantothenate Kinase Inhibitor

A reversible inhibitor of pantothenate kinase

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库存: 现货

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1mg

￥562.00

450.00

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5mg

￥1962.00

1570.00

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10mg

￥3087.00

2470.00

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25mg

￥6937.00

5550.00

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货号: ajcx23232
CAS: 902614-04-4
别名: 3-(2,4-二甲基吡啶并[2',3':3,4]吡唑并[1,5-A]嘧啶-3-基)-N-(3-(甲硫基)苯基)丙酰胺
分子式: C21H21N5OS
分子量: 391.5
纯度: >98%
溶解度: DMF: 1 mg/ml,DMSO: 1 mg/ml,DMSO:PBS (pH 7.2) (1:4): 0.25 mg/ml
储存: Store at -20°C
库存: 现货

Background

Pantothenate Kinase Inhibitor (PANKi) is a reversible inhibitor of pantothenate kinase (PanK; IC₅₀s = 70, 92, and 25 nM for PanK1β, PanK2, and PanK3, respectively), the rate-limiting enzyme in the synthesis of coenzyme A .¹ It binds to the ATP-PanK3 complex with an apparent binding constant of 300 nM and exhibits mixed-type inhibition with respect to ATP and pantothenate. PANKi inhibits CoA biosynthesis in C3A cells (IC₅₀ = 0.9 µM) with no effect on cell viability when used at concentrations up to 8 µM. PANKi (5 µM) synergizes with BSO to induce ferroptosis in PANC-1 cells and sensitizes the cells to imidazole ketone erastin-induced ferroptosis.²

1.Sharma, L.K., Leonardi, R., Lin, W., et al.A high-throughput screen reveals new small-molecule activators and inhibitors of pantothenate kinasesJ. Med. Chem.58(3)1563-1568(2015) 2.Badgley, M.A., Kremer, D.M., Maurer, H.C., et al.Cysteine depletion induces pancreatic tumor ferroptosis in miceScience368(6486)85-89(2020)