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].

Product Specifications

CAS Number

[1094250-15-3]

UNSPSC

12352005

Target

TRP Channel

Type

Natural Products

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/englerin-a.html

Purity

99.50

Solubility

DMSO : 50 mg/mL|Methanol : 30 mg/mL (ultrasonic)

Smiles

O=C(O[C@@H]1[C@]2(C(C)C)C[C@@H](OC(CO)=O)[C@](O2)(C)[C@]3([H])CC[C@@H](C)[C@@]13[H])/C=C/C4=CC=CC=C4

Molecular Formula

C26H34O6

Molecular Weight

442.54

References & Citations

[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.