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].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Englerin A (5 mg/kg; i.p daily except Sunday) markedly inhibits tumor growth during the 2-week treatment period in mice^[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

442.54

Solid

C₂₆H₃₄O₆

1094250-15-3

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

Room temperature in continental US; may vary elsewhere.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]