BeKm 1

BeKm 1

Potent and selective KV11.1 (hERG) channel blocker. Selective for KV11.1 over a panel of 14 other potassium channels. Dose-dependently prolongs QTc interval in isolated rabbit heart.

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CAT No: R1045

CAS No: 524962-01-4

Synonyms/Alias: 524962-01-4;L-Phenylalanine,L-arginyl-L-prolyl-L-threonyl-L-a-aspartyl-L-isoleucyl-L-lysyl-L-cysteinyl-L-seryl-L-a-glutamyl-L-seryl-L-tyrosyl-L-glutaminyl-L-cysteinyl-L-phenylalanyl-L-prolyl-L-valyl-L-cysteinyl-L-lysyl-L-seryl-L-arginyl-L-phenylalanylglycyl-L-lysyl-L-threonyl-L-asparaginylglycyl-L-arginyl-L-cysteinyl-L-valyl-L-asparaginylgl;BeKm 1;BeKm1;BeKm-1;ZVA96201;AKOS027470315;DA-61566;PD080272;

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M.F/Formula	C174H261N51O52S6
M.W/Mr.	4092
Sequence	One Letter Code:RPXDXKCSESYQCFPVCKSRFGKXNGRCVNGFCDCF Three Letter Code:H-DL-Arg-DL-Pro-DL-xiThr-DL-Asp-DL-xiIle-DL-Lys-DL-Cys(1)-DL-Ser-DL-Glu-DL-Ser-DL-Tyr-DL-Gln-DL-Cys(2)-DL-Phe-DL-Pro-DL-Val-DL-Cys(3)-DL-Lys-DL-Ser-DL-Arg-DL-Phe-Gly-DL-Lys-DL-xiThr-DL-Asn-Gly-DL-Arg-DL-Cys(1)-DL-Val-DL-Asn-Gly-DL-Phe-DL-Cys(2)-DL-Asp-DL-Cys(3)-DL-Phe-OH
Labeling Target	KV11.1 (hERG) channel
Activity	Blocker

InChI

InChI=1S/C174H261N51O52S6/c1-9-88(6)136(221-152(257)111(73-133(242)243)207-168(273)138(90(8)230)223-163(268)123-47-31-63-224(123)169(274)97(178)41-28-60-188-172(182)183)166(271)201-101(44-24-27-59-177)145(250)213-120-83-281-283-85-122-161(266)219-134(86(2)3)164(269)205-108(70-126(180)233)140(245)193-76-130(237)196-106(66-92-35-16-11-17-36-92)149(254)216-117-80-278-279-81-118(214-147(252)103(53-55-125(179)232)199-150(255)107(67-95-49-51-96(231)52-50-95)203-155(260)116(79-228)211-146(251)104(54-56-131(238)239)200-154(259)115(78-227)212-160(120)265)158(263)208-112(68-93-37-18-12-19-38-93)170(275)225-64-32-48-124(225)162(267)220-135(87(4)5)165(270)218-121(84-282-280-82-119(217-151(256)110(72-132(240)241)204-157(117)262)159(264)209-113(171(276)277)69-94-39-20-13-21-40-94)156(261)198-100(43-23-26-58-176)144(249)210-114(77-226)153(258)197-102(46-30-62-190-174(186)187)143(248)202-105(65-91-33-14-10-15-34-91)139(244)191-74-128(235)194-98(42-22-25-57-175)148(253)222-137(89(7)229)167(272)206-109(71-127(181)234)141(246)192-75-129(236)195-99(142(247)215-122)45-29-61-189-173(184)185/h10-21,33-40,49-52,86-90,97-124,134-138,226-231H,9,22-32,41-48,53-85,175-178H2,1-8H3,(H2,179,232)(H2,180,233)(H2,181,234)(H,191,244)(H,192,246)(H,193,245)(H,194,235)(H,195,236)(H,196,237)(H,197,258)(H,198,261)(H,199,255)(H,200,259)(H,201,271)(H,202,248)(H,203,260)(H,204,262)(H,205,269)(H,206,272)(H,207,273)(H,208,263)(H,209,264)(H,210,249)(H,211,251)(H,212,265)(H,213,250)(H,214,252)(H,215,247)(H,216,254)(H,217,256)(H,218,270)(H,219,266)(H,220,267)(H,221,257)(H,222,253)(H,223,268)(H,238,239)(H,240,241)(H,242,243)(H,276,277)(H4,182,183,188)(H4,184,185,189)(H4,186,187,190)

InChI Key

OQEMUGXECXBKDP-UHFFFAOYSA-N

References

The toxin BeKm-1 isolated from scorpion Buthus eupeus is singled out of other characterized α-KTxs by selectively inhibiting HERG channels, which are voltage-gated K+ channels, coded by the humanether-a-go-go-related gene. The interest in the HERG channels has increased due to the important role these channels play in different tissues, mainly in shaping the action potential in the heart). The HERG channels specify one component of the delayed rectifier that contributes to the repolarization phase of cardiac action potential. One form of inherited long QT syndrome, LQT2, results from genetic defects in herg1 gene and predisposes affected individuals to potentially lethal arrhythmias. However most often the same sickness is derived from the nonspecific blockade of cardiac HERG current by various commonly used medications, such as class III antiarrhythmics, antihistaminics, or antipsychotics. This undesirable side effect is a major hurdle in the development of new and safe drugs, which may be overcome by the resolution of HERG channel pore structure.

New Binding Site on Common Molecular Scaffold Provides HERG Channel Specificity of Scorpion Toxin BeKm-1*210

1. Effect of Short-Term Desiccation, Recovery Time, and CAPA-PVK Neuropeptide on the Immune System of the Burying Beetle Nicrophorus vespilloides

2. Genetic, cellular, and structural characterization of the membrane potential-dependent cell-penetrating peptide translocation pore

3. Application of human liver organoids as a patient-derived primary model for HBV infection and related hepatocellular carcinoma

4. Adipose tissue is a key organ for the beneficial effects of GLP-2 metabolic function

5. Immune-awakening Saccharomyces-inspired nanocarrier for oral target delivery to lymph and tumors

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