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  • 产品名称：BeKm-1

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  • 产品厂商：Smartox-Biotech
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简单介绍：
BeKm-1
详情介绍：
Sequence AA sequence: Arg-Pro-Thr-Asp-Ile-Lys-Cys7-Ser-Glu-Ser -Tyr-Gln-Cys13-Phe-Pro-Val-Cys17-Lys-Ser-Arg -Phe-Gly-Lys-Thr-Asn-Gly-Arg-Cys28-Val-Asn- Gly-Phe-Cys33-Asp-Cys35-Phe-OH Disulfide bonds: Cys7-Cys28, Cys13-Cys33, and Cys17-Cys35
Characteristics BeKm-1 is a selective blocker of hERG1 channel
Background BeKm-1 toxin is a peptide toxin that has been isolated from the venom of the Central Asian scorpion Buthus eupeus. BeKm-1 toxin has been reported to be a highly selective inhibitor of the human ether-a-go-go ERG1 channel (hERG1). BeKm-1 inhibits hERG1 channels expressed in HEK-293 cells with an IC50 of 3.3 nM, but has no effect at 100 nM on human EAG, human SK1, rat SK2, human IK, human BK, KCNQ1/KCNE1, KCNQ2/KCNQ3, and KCNQ4 channels. It has also minimal effects on rat ELK1 channel. BeKm-1 inhibits the human ERG1 + KCNE1 combination transiently expressed in HEK-293 cells with an IC50 value in the range of 10 to 30 nM. BeKm-1 toxin preferentially blocks human ERG channel through the closed (resting) state, although some open channel blockade is also reported to occur.
Molecular Weight 4091.70 kDa
Restrictions For Research Use only
Storage -20 °C
Background publications Milnes, Dempsey, Ridley, Crociani, Arcangeli, Hancox, Witchel: "Preferential closed channel blockade of HERG potassium currents by chemically synthesised BeKm-1 scorpion toxin." in: FEBS letters, Vol. 547, Issue 1-3, pp. 20-6, 2003 (PubMed).

Korolkova, Bocharov, Angelo, Maslennikov, Grinenko, Lipkin, Nosyreva, Pluzhnikov, Olesen, Arseniev, Grishin: "New on common molecular scaffold provides HERG channel specificity of scorpion toxin BeKm-1." in: The Journal of biological chemistry, Vol. 277, Issue 45, pp. 43104-9, 2002 (PubMed).