Endovion (NS3728) is a pharmacological anion channel inhibitor (like chloride channel) and the specific VRAC/VSOAC blocker. Endovion (NS3728) is also an Anoctamin-1 (ANO 1) channel inhibitor.
IC50&Target
Chloride channel, VRAC/VSOAC.
ANO1.
体外研究
Endovion (NS3728, 10-100 μM) reduces TNFα-induced apoptosis and increases p53-protein level as well as downstream signaling, e.g., expression of p21, Bax, Noxa, MDM2, and activation of Caspase-9/-3 in Cisplatin-sensitive cells.
Endovion (NS3728, 10 μM) inhibits cell proliferation in Capan-1, AsPC-1 and BxPC-3 cell lines.
Western Blot Analysis
Cell Line:
Wild-type, resistant, and transiently transfected A2780 cells.
Concentration:
10-100 μM.
Incubation Time:
18 or 4.5 h.
Result:
Reduced the maximal taurine rate constant more than 90% compared with the untreated control cells.
Resulted in an increased LRRC8A protein expression.
Significantly reduceed p53 and protein level in A2780WT cells.
Cell Proliferation Assay
Cell Line:
Capan-1, AsPC-1, BxPC-3 and H6c7 cell lines.
Concentration:
10 μM.
Incubation Time:
24 h.
Result:
Resulted in the most pronounced inhibition in all cell lines with 77 ± 26 % in Capan-1, 67 ± 9 % in AsPC-1, and 54 ± 8 % in BxPC-3 cells at +67 mV.
分子式
C16H9BrF6N6O
分子量
495.18
CAS号
265646-85-3
运输条件
Room temperature in continental US; may vary elsewhere.