Delta-theraphotoxin-Hm1a Protein, Heteroscodra maculata, Recombinant (His & Myc & SUMO)

产品编号 TMPH-00818

别名: Kappa-TRTX-Hm1a, Delta-TRTX-Hm1a, Heteroscodratoxin-1, Kappa-theraphotoxin-Hm1a, HmTx1, Delta-theraphotoxin-Hm1a

Gating-modifier toxin that potently inhibits inactivation of the mammalian Nav1.1/SCN1A sodium channel (EC(50)=38 nM). Also moderately inhibits inactivation of Nav1.2/SCN2A (EC(50)=236 nM) and Nav1.3/SCN3A (EC(50)=220 nM) when the channels are expressed in oocytes without the beta-1 auxiliary subunit. Does not inhibit inactivation of Nav1.2/SCN2A when the channel is coexpressed with the beta-1 auxiliary subunit. When tested on Nav1.1/SCN1A channel, it enhances peak current amplitude and potently delays channel inactivation in a dose-dependent manner, leading to a large sustained current. It has no effect on the voltage-dependence of steady-state activation, and induces a depolarizing shift in the voltage dependence of inactivation. In addition, it does not modify the recovery from fast inactivation in Nav1.1/SCN1A. The binding affinity and subtype selectivity of the toxin towards Nav1.1/SCN1A channel is determined by residues within both the S1-S2 and S3-S4 loops of the domain IV voltage sensor of the channel. This toxin also weakly inhibits several subtypes of voltage-gated potassium channels. It moderately blocks Kv2.1/KCNB1 (23% inhibition at 100 nM), Kv2.2/KCNB2 (19.7% at 100 nM and 51% at 300 nM), Kv4.1/KCND1 (IC(50)=280 nM), Kv4.2/KCND2 (39% at 300 nM) and Kv4.3/KCND3 (43% at 300 nM). In vivo, intracerebroventricular injection into mice elicits convulsions, spasms, tremors and rapid death. When injected into mouse hindpaw, the toxin elicits an immediate and robust response to pain. However, intraplantar injection of toxin does not cause neurogenic inflammation or alter sensitivity to heat, indicative of a modality-specific effect on mechanosensitive neurons. In Dravet syndrome mice model, intracerebroventricular infusion of this peptide rescues mice from seizures and premature death.

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Delta-theraphotoxin-Hm1a Protein, Heteroscodra maculata, Recombinant (His & Myc & SUMO)

规格	价格/CNY	货期
20 μg	￥ 2,290	20日内发货
100 μg	￥ 4,320	20日内发货
1 mg	￥ 14,600	20日内发货

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种属	Heteroscodra maculata
表达系统	E. coli
标签	N-terminal 6xHis-SUMO-tagged and C-terminal Myc-tagged
蛋白编号	P60992
别名	Kappa-TRTX-Hm1a, Delta-TRTX-Hm1a, Heteroscodratoxin-1, Kappa-theraphotoxin-Hm1a, HmTx1, Delta-theraphotoxin-Hm1a
氨基酸序列	ECRYLFGGCSSTSDCCKHLSCRSDWKYCAWDGTFS Note: The complete sequence including tag sequence, target protein sequence and linker sequence could be provided upon request.
蛋白构建	1-35 aa
蛋白纯度	> 85% as determined by SDS-PAGE.
分子量	21.5 kDa (predicted)

缓冲液	Tris-based buffer,50% glycerol
复溶方法	A hardcopy of COA with reconstitution instructions is sent along with the products. Please refer to it for detailed information.
存储	Generally, the shelf life of liquid form is 6 months at -20°C/-80°C. The shelf life of lyophilized form is 12 months at -20°C/-80°C.
运输方式	In general, recombinant proteins are provided as lyophilized powder which are shipped at ambient temperature. Bulk packages of recombinant proteins are provided as frozen liquid. They are shipped out with blue ice unless customers require otherwise.
研究背景	Gating-modifier toxin that potently inhibits inactivation of the mammalian Nav1.1/SCN1A sodium channel (EC(50)=38 nM). Also moderately inhibits inactivation of Nav1.2/SCN2A (EC(50)=236 nM) and Nav1.3/SCN3A (EC(50)=220 nM) when the channels are expressed in oocytes without the beta-1 auxiliary subunit. Does not inhibit inactivation of Nav1.2/SCN2A when the channel is coexpressed with the beta-1 auxiliary subunit. When tested on Nav1.1/SCN1A channel, it enhances peak current amplitude and potently delays channel inactivation in a dose-dependent manner, leading to a large sustained current. It has no effect on the voltage-dependence of steady-state activation, and induces a depolarizing shift in the voltage dependence of inactivation. In addition, it does not modify the recovery from fast inactivation in Nav1.1/SCN1A. The binding affinity and subtype selectivity of the toxin towards Nav1.1/SCN1A channel is determined by residues within both the S1-S2 and S3-S4 loops of the domain IV voltage sensor of the channel. This toxin also weakly inhibits several subtypes of voltage-gated potassium channels. It moderately blocks Kv2.1/KCNB1 (23% inhibition at 100 nM), Kv2.2/KCNB2 (19.7% at 100 nM and 51% at 300 nM), Kv4.1/KCND1 (IC(50)=280 nM), Kv4.2/KCND2 (39% at 300 nM) and Kv4.3/KCND3 (43% at 300 nM). In vivo, intracerebroventricular injection into mice elicits convulsions, spasms, tremors and rapid death. When injected into mouse hindpaw, the toxin elicits an immediate and robust response to pain. However, intraplantar injection of toxin does not cause neurogenic inflammation or alter sensitivity to heat, indicative of a modality-specific effect on mechanosensitive neurons. In Dravet syndrome mice model, intracerebroventricular infusion of this peptide rescues mice from seizures and premature death.

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Keywords

Delta-theraphotoxin-Hm1a Protein, Heteroscodra maculata, Recombinant (His & Myc & SUMO) Kappa-TRTX-Hm1a Delta-TRTX-Hm1a Heteroscodratoxin-1 Kappa-theraphotoxin-Hm1a HmTx1 Delta-theraphotoxin-Hm1a recombinant recombinant-proteins proteins protein