Englerin A

• 常用名: Englerin A
• 英文名: Englerin A
• CAS号: 1094250-15-3
• 分子量: 442.54500
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₆H₃₄O₆
• 熔点: N/A
• 闪点: N/A

Englerin A用途

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名称

• 英文名: (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

Englerin A生物活性

• 描述: 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。
• 相关类别:
  信号通路 >> 跨膜转运 >> TRP频道
  研究领域 >> 癌症
• 靶点实验:

  hTRPC4:11.2 nM (EC50)

  hTRPC5:7.6 nM (EC50)

• 体外研究: Englerin A(0.15-2500 nM；48 h)特征性浓度依赖性抑制经对照siRNA处理的A-498细胞的生长,但对TRPC4 siRNA处理的细胞生长几乎没有影响[3]。Englerin A(0.001nM-10μM；48 h)抑制过度表达TRPC5的HEK293T细胞的细胞活力[3]。在人细胞内持续表达浓度超过1-2μm的细胞内钙离子浓度。EnglerinA(0.1-1000nm；1-300s)引起A498细胞内Ca2+升高,EC50为10nM[1]。
• 体内研究: Englerin A(5 mg/kg；除周日外每天静脉注射)在2周的治疗期内显著抑制小鼠的肿瘤生长[4]。
• 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.

Englerin A物理化学性质

• 分子式: C₂₆H₃₄O₆
• 分子量: 442.54500
• 精确质量: 442.23600
• PSA: 82.06000
• LogP: 3.76540
• InChIKey: GACOFEKSDCOVMV-RRYXBOBMSA-N
• SMILES: CC1CCC2C1C(OC(=O)C=Cc1ccccc1)C1(C(C)C)CC(OC(=O)CO)C2(C)O1
• 外观性状: 固体
• 储存条件: 室温， 密封， 干燥

Englerin A靶点实验

查看更多实验

实验名称：Growth inhibition of human A498 cells incubated for 48 hrs by sulforhodamine B assay 来源：ChEMBL 靶标：A498 External Id：CHEMBL4622711

实验名称：Growth inhibition of human RXF393 cells incubated for 48 hrs by sulforhodamine B assa... 来源：ChEMBL 靶标：RXF 393 External Id：CHEMBL4622713

实验名称：Growth inhibition of human UO31 cells incubated for 48 hrs by sulforhodamine B assay 来源：ChEMBL 靶标：UO-31 External Id：CHEMBL4622712

实验名称：USP8 deubiquitinase inhibition: Primary qHTS 来源：24642 靶标：ubiquitin specific peptidase 8 External Id：USP8 FAST DUB HTS Primary

实验名称：Agonist activity at human TRPC4/TRPC1 expressed in HEK293 Tet cells assessed as incre... 来源：ChEMBL 靶标：Short transient receptor potential channel 4 External Id：CHEMBL4622715

实验名称：Agonist activity at human TRPC4/TRPC1 expressed in HEK293 Tet cells assessed as incre... 来源：ChEMBL 靶标：Short transient receptor potential channel 4 External Id：CHEMBL4622714

实验名称：USP17 deubiquitinase inhibition: Primary qHTS 来源：24642 靶标：ubiquitin specific peptidase 17 like family member 5 External Id：USP17 FAST DUB HTS Primary

实验名称：Acute toxicity in iv dosed mouse assessed as maximum tolerated dose by up and down me... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4622717

实验名称：Activation of PKC in human 786-0 cells at 10 nM 来源：ChEMBL 靶标：Protein kinase C alpha type External Id：CHEMBL3806370

实验名称：USP7 deubiquitinase inhibition: Primary qHTS 来源：24642 靶标：ubiquitin specific peptidase 7 External Id：USP7 FAST DUB HTS Primary

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Englerin A英文别名

• 6',7',10,11-tetramethoxyemetan hydrobromide
• EMETINE HBR