Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC 50 s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca 2+ influx and Ca 2+ cell overload
In Vitro
Englerin A (0.15-2500 nM; 48 h) characteristic concentration-dependent suppresses cells growth of the A-498 cells treated with the control siRNA while has little effect on the growth of cells treated with TRPC4 siRNAs. Englerin A (0.001nM-10 μM; 48 h) inhibits cells viability in HEK293T cells overexpressing TRPC5. Englerin A (3 nM; 1-240 s) evokes sustained elevation of the intracellular Ca 2+ concentration within 1 min in HEK 293 cells over-expressing human TRPC4. Englerin A (0.1-1000 nM; 1-300 s) evokes intracellular Ca 2+ elevations in A498 cells as well with an EC 50 of 10 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Englerin A (5 mg/kg; i.p daily except Sunday) markedly inhibits tumor growth during the 2-week treatment period in mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC 50 s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca 2+ influx and Ca 2+ cell overload.
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.
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