8-Bromo-ATP

8-Bromo-ATP (8-Bromoadenosine 5'-triphosphate), an ATP analogue, is a purinergic P2X receptor agonist. 8-Bromo-ATP shows cytotoxic to multiple myeloma cells with an IC50 of 23.1 μM[1][2][3].

Research Areas >> Cancer

Signaling Pathways >> Membrane Transporter/Ion Channel >> P2X Receptor

8-Bromo-ATP (10-50 μM; 5 days) treatment shows cytotoxic to multiple myeloma[3]. Fluorescence measurements are made possible through the use of 8-Bromo-ATP, which selectively quenched certain tryptophan residues of the ATPase. 8-Bromo-ATP enhances the rate of dephosphorylation of native ATPase 2-3-fold when added in the absence of divalent cations[2]. Cell Viability Assay[3] Cell Line: MM 1.s cells Concentration: 10 μM, 20 μM, 30 μM, 40 μM, 50 μM Incubation Time: 5 days Result: Showed cytotoxic to multiple myeloma.

[1]. Howson, W, et al. Synthesis and biological evaluation of ATP analogues acting at putative purinergic P2X-receptors (on the guinea pig bladder). Eur. J. Med. Chem. 23(5), 433-439 (1988).

[2]. P Champeil, et al. ATP regulation of sarcoplasmic reticulum Ca2+-ATPase. Metal-free ATP and 8-bromo-ATP bind with high affinity to the catalytic site of phosphorylated ATPase and accelerate dephosphorylation. J Biol Chem. 1988 Sep 5;263(25):12288-94.

[3]. Li Wang, et al. Cationic phospholiposomes: efficient delivery vehicles of anticancer derivatives of ATP to multiple myeloma cells. J Liposome Res. 2011 Dec;21(4):306-14.