220 1045 


Selective blocker of Nav1.5 channel

Jingzhaotoxin-III (ß-TRTX-Cj1α) has been isolated initially from the Chinese Tarantula spider Chilobrachys Jingzhaovenom. Jingzhaotoxin-III selectively inhibits the activation of the voltage-dependent sodium channel Nav1.5 in heart or cancer cells with an IC50value close to 350 nM. It is inactive on Nav1.2, Nav1.4, Nav1.6 and Nav1.7 and should therefore be considered as an interesting research tool to discriminate between sodium channel subtypes. Jingzhaotoxin-III binds onto receptor site 4 presumably located on DIIS3-S4 linker of Nav1.5 and supposedly blocks Nav1.5 through a different mechanism than ProTx-II and Huwentoxin IV. ß-TRTX-Cj1α is composed of 36 amino acid residues including 6 cysteines cross-linked according to a C1-C4, C2-C5 and C3-C6 pattern. Jingzhaotoxin-III also inhibits Kv2.1 channel with an IC50 of around 700 nM.

Jingzhaotoxin III #12JGZ003 Nav1.5 sodium channel blocker

Fig 1: Representative effects of different Jinghzaotoxin III concentrations on the amplitude of INa. Jinghzaotoxin III was applied externally to the cell at the time and concentrations indicated on top. Inward sodium currents were triggered in human MDA-MB-231 breast cancer cells by 30 ms-long voltage steps from -100 to -5 mV, from a holding potential of -100 mV. 1 step every 2 sec.

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AA sequence: Asp-Gly-Glu-Cys4-Gly-Gly-Phe-Trp-Trp-Lys-Cys11-Gly-Arg-Gly-Lys-Pro-Pro-Cys18-Cys19-Lys-Gly-Tyr-Ala-Cys24-Ser-Lys-Thr-Trp-Gly-Trp-Cys31-Ala-Val-Glu-Ala-Pro-OH
Disulfide bonds: Cys4-Cys19, Cys11-Cys24, and Cys18-Cys31
Length (aa): 36
Formula: C174H241N47O46S6
Molecular Weight:  3919.53 Da
Appearance: White lyophilized solid
Solubility: aqueous buffer
CAS number: not available
Source: Synthetic
Purity rate:> 98%




Analysis of the interaction of tarantula toxin jingzhaotoxin-III (β-TRTX-Cj1α) with the voltage sensor of Kv2.1 uncovers the molecular basis for cross-activities on Kv2.1 and Nav1.5 channels

Molecular basis of the tarantula toxin jingzhaotoxin-III (Beta-TRTX-Cj1 alpha) interacting with voltage sensors in sodium channel subtype Nav1.5

Jingzhaotoxin-III, a Novel Spider Toxin Inhibiting Activation of Voltage-gated Sodium Channel in Rat Cardiac Myocytes

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