BeKm 1

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Supplier	Creative Peptides
Product #	R1045
CAS #	524962-01-4
Pricing	Inquire
LabelingTarget	KV11.1 (hERG) channel
MolecularFormula	C174H261N51O52S6
MolecularWeight	4091.65
Sequence	RPTDIKCSESYQCFPVCKSRFGKTNGRCVNGFCDCF(Disulfide bridge: Cys7 and Cys28,Cys13 and Cys33,Cys17 and Cys35)
Storage	-20°C
Explanation	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.
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)
InChIKey	OQEMUGXECXBKDP-UHFFFAOYSA-N
Reference	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

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