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Arylpiperazine 5k is an inhibitor of fatty acid transport protein 1 (FATP1; IC50 = 4.6 nM for the human protein).1 It reduces the accumulation of neutral and polar lipids in MDA-MB-231 breast cancer cells induced by linoleic acid (Item Nos. 90150 | 90150.1 | 21909) when used at a concentration of 12.5 µM.2 Arylpiperazine 5k (12.5 µM) decreases ATP (Item No. 14498) and BODIPY-palmitate (Item No. 26749) levels in BJAB human lymphoma cells with a deletion of CD37, which is also a negative regulator of fatty acid uptake, but not in wild-type BJAB cells.3 It induces cell death in MDA-MB-231, MCF-7, HCC1806, and BT474 human breast cancer cells when used at a concentration of 12.5 µM.
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1. Arylpiperazines as fatty acid transport protein 1 (FATP1) inhibitors with improved potency and pharmacokinetic properties. Bioorg. Med. Chem. Lett. 23(9), 2560-2565 (2013).
2. Unraveling FATP1, regulated by ER-
3. Fatty acid metabolism in aggressive B-