Englerin A

• CAT Number: I045313
• CAS Number: 1094250-15-3
• Molecular Formula: C26H34O6
• Molecular Weight: 442.54
• Purity: ≥95%
• Synonyms: [(1S,2R,5R,6R,7S,8R,10R)-10-(2-hydroxyacetyl)oxy-1,5-dimethyl-8-propan-2-yl-11-oxatricyclo[6.2.1.02,6]undecan-7-yl] (E)-3-phenylprop-2-enoate
• InChI: InChI=1S/C26H34O6/c1-16(2)26-14-20(30-22(29)15-27)25(4,32-26)19-12-10-17(3)23(19)24(26)31-21(28)13-11-18-8-6-5-7-9-18/h5-9,11,13,16-17,19-20,23-24,27H,10,12,14-15H2,1-4H3/b13-11+/t17-,19-,20-,23-,24+,25+,26-/m1/s1
• InChIKey: GACOFEKSDCOVMV-RRYXBOBMSA-N
• SMILES: CC1CCC2C1C(C3(CC(C2(O3)C)OC(=O)CO)C(C)C)OC(=O)C=CC4=CC=CC=C4

Englerin A (Cat No.: I045313) is a sesquiterpene natural product isolated from Phyllanthus engleri, known for its potent and selective cytotoxicity against renal cancer cells. It activates transient receptor potential canonical (TRPC) channels, particularly TRPC4 and TRPC5, leading to calcium influx and cancer cell death. Englerin A’s unique mechanism and tumor selectivity make it a promising lead compound in anticancer drug development. Its complex structure and limited natural availability have spurred synthetic efforts to produce analogs for pharmacological and therapeutic research.

Reference

[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.
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[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.
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[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.
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[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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