Englerin A

Modify Date: 2024-01-08 08:28:20

Englerin A structure	Common Name	Englerin A
	CAS Number	1094250-15-3	Molecular Weight	442.54500
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₂₆H₃₄O₆	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of Englerin A

Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC50s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca2+ influx and Ca2+ cell overload[1][2][3].

Name	(1S,2R,5R,6R,7S,8R,10R)-10-(Glycoloyloxy)-8-isopropyl-1,5-dimethyl-11-oxatricyclo[6.2.1.02,6]undec-7-yl (2E)-3-phenylacrylate
Synonym	More Synonyms

Description	Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC50s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca2+ influx and Ca2+ cell overload[1][2][3].
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> TRP Channel Research Areas >> Cancer
Target	hTRPC4:11.2 nM (EC50) hTRPC5:7.6 nM (EC50)
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[3]. Englerin A (0.001nM-10 μM; 48 h) inhibits cells viability in HEK293T cells overexpressing TRPC5[3]. Englerin A (3 nM; 1-240 s) evokes sustained elevation of the intracellular Ca2+ concentration within 1 min in HEK 293 cells over-expressing human TRPC4[1]. Englerin A (0.1-1000 nM; 1-300 s) evokes intracellular Ca2+ elevations in A498 cells as well with an EC50 of 10 nM[1].
In Vivo	Englerin A (5 mg/kg; i.p daily except Sunday) markedly inhibits tumor growth during the 2-week treatment period in mice[4].
References	[1]. Akbulut Y, et, al. (-)-Englerin A is a potent and selective activator of TRPC4 and TRPC5 calcium channels. Angew Chem Int Ed Engl. 2015 Mar 16;54(12):3787-91. [2]. Rubaiy HN, et, al. Identification of an (-)-englerin A analogue, which antagonizes (-)-englerin A at TRPC1/4/5 channels. Br J Pharmacol. 2018 Mar; 175(5):830-839. [3]. Carson C, et, al. Englerin A Agonizes the TRPC4/C5 Cation Channels to Inhibit Tumor Cell Line Proliferation. PLoS One. 2015 Jun 22;10(6):e0127498. [4]. Sourbier C, et, al. Englerin A stimulates PKCθ to inhibit insulin signaling and to simultaneously activate HSF1: pharmacologically induced synthetic lethality. Cancer Cell. 2013 Feb 11;23(2):228-37.