Englerin A

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Englerin A 

Englerin A 是一种有效和选择性的 TRPC4 和 TRPC5 通道的活化剂，EC50 值分别为 11.2 和 7.6 nM。Englerin A 通过增加 Ca2+ 内流和 Ca2+ 细胞超负荷来诱导肾癌细胞死亡。

Englerin A

Englerin A Chemical Structure

CAS No. : 1094250-15-3

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生物活性

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].

IC50 & Target[1]

hTRPC4

11.2 nM (EC50)

hTRPC5

7.6 nM (EC50)

体外研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

442.54

Formula

C26H34O6
CAS 号

1094250-15-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [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.

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