Recombinant Heteroscodra maculata Kappa-theraphotoxin-Hm1a
| Product Name | Recombinant Heteroscodra maculata Kappa-theraphotoxin-Hm1a |
|---|---|
| Description | Gating modifier toxin that principally inhibits inactivation of the mammalian voltage-gated sodium channel Nav1.1/SCN1A. When tested against human Nav1.1/SCN1A-Nav1.8/SCN10A alpha subunits heterologously expressed in Xenopus oocytes, the toxin inhibits inactivation of Nav1.1 (EC(50)=38 nM), with substantially weaker effects on Nav1.2/SCN2A (EC(50)=236 nM) and Nav1.3/SCN3A (EC(50)=220 nM). The toxin inhibits several subtypes of voltage-gated potassium channels with significantly lower potency than its effects on Nav1.1/SCN1A. It is a moderately potent blocker of Kv2.1/KCNB1, Kv2.2/KCNB2, Kv4.1/KCND1, Kv4.2/KCND2 and Kv4.3/KCND3 and has little effect on Kv1.1/KCNA1, Kv1.2/KCNA2, Kv1.3/KCNA3, Kv1.4/KCNA4, Kv1.5/KCNA5, Kv1.6/KCNA6 and Kv3.4/KCNC4. The binding affinity and subtype selectivity of the toxin is determined by residues within both the S1-S2 and S3-S4 loops of the domain IV voltage sensor. 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. Intraplantar injection of toxin does not cause neurogenic inflammation or alter sensitivity to heat, indicative of a modality-specific effect on mechanosensitive neurons |
| Synonyms | Heteroscodratoxin-1 |
| Host | Yeast |
| Molecular Weight | 4.0 kDa |
| Amino Acid Sequence | ECRYLFGGCSSTSDCCKHLSCRSDWKYCAWDGTFS |
| Protein Length | Full Length, 1-35aa |
| Tag | NO-tagged |
| Reactivity | Spider |
| Applications | SDS-PAGE |
| Form | Liquid, in Tris-based buffer, 50% glycerol |
| Purity | Greater than 90% as determined by SDS-PAGE. |
| References |
"Novel tarantula toxins for subtypes of voltage-dependent potassium channels in the Kv2 and Kv4 subfamilies." Escoubas P., Diochot S., Celerier M.-L., Nakajima T., Lazdunski M. Mol. Pharmacol. 62:48-57(2002) |
| Background | Gating modifier toxin that principally inhibits inactivation of the mammalian voltage-gated sodium channel Nav1.1/SCN1A. When tested against human Nav1.1/SCN1A-Nav1.8/SCN10A alpha subunits heterologously expressed in Xenopus oocytes, the toxin inhibits inactivation of Nav1.1 (EC(50)=38 nM), with substantially weaker effects on Nav1.2/SCN2A (EC(50)=236 nM) and Nav1.3/SCN3A (EC(50)=220 nM). The toxin inhibits several subtypes of voltage-gated potassium channels with significantly lower potency than its effects on Nav1.1/SCN1A. It is a moderately potent blocker of Kv2.1/KCNB1, Kv2.2/KCNB2, Kv4.1/KCND1, Kv4.2/KCND2 and Kv4.3/KCND3 and has little effect on Kv1.1/KCNA1, Kv1.2/KCNA2, Kv1.3/KCNA3, Kv1.4/KCNA4, Kv1.5/KCNA5, Kv1.6/KCNA6 and Kv3.4/KCNC4. The binding affinity and subtype selectivity of the toxin is determined by residues within both the S1-S2 and S3-S4 loops of the domain IV voltage sensor. 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. Intraplantar injection of toxin does not cause neurogenic inflammation or alter sensitivity to heat, indicative of a modality-specific effect on mechanosensitive neurons |
| Supplier | Cusabio |
All Research Products are sold for laboratory RESEARCH USE ONLY and ARE NOT TO BE USED FOR HUMAN OR ANIMAL THERAPEUTIC OR DIAGNOSTIC APPLICATIONS. The information presented is believed to be accurate; however, said information and products are offered without warranty or guarantee since the ultimate conditions of use and the variability of the materials treated are beyond our control. Nothing disclosed herein is to be construed as a recommendation to use our products in violation of any patents. ARP American Research Products, Inc. does not submit its products for regulatory review by any government body or other organization, and we do not validate them for clinical, therapeutic or diagnostic use, or for safety and effectiveness. You are solely responsible for making sure that the way you use the products complies with applicable laws, regulations and governmental policies and for obtaining all necessary approvals, intellectual property rights, licenses and permissions that you may need related to your use. Under no circumstances shall ARP American Research Products, Inc. be liable for damages, whether consequential, compensatory, incidental or special, strict liability or negligence, breach of warranty or any other theory arising out of the use of the products available from ARP American Research Products, Inc. Nothing contained herein warrants that the use of the products will not infringe on the claims of any patents covering the product itself or the use thereof in combination with other products or in the operation of any process. ARP American Research Products, Inc. disclaims any and all representations or warranties of any kind whatsoever, express or implied, including without limitation any implied warranties of merchantability or fitness for a particular purpose, of non-infringement, or regarding results obtained through the use of any product, whether arising from a statute or otherwise in law or from a course of performance, dealing or usage of trade.
