Jingzhaotoxin III

• Supplier: Creative Peptides
• Product #: R0983
• CAS #: 925463-91-8
• LabelingTarget: NaV1.5 channels
• MolecularFormula: C174H241N47O46S6
• Source: Synthetic
• Sequence: DGECGGFWWKCGRGKPPCCKGYACSKTWGWCAVEAP(Disulfide bridge: Cys4 and Cys19,Cys11 and Cys24,Cys18 and Cys31)
• Storage: -20°C
• Explanation: Jingzhaotoxin-III selectively inhibits the activation of the voltage-dependent Nav1.5 channels (IC50 = 350 nM) in heart or cancer cells, but displays no effect on other isoforms,like NaV1.2, NaV1.4, NaV1.6 and NaV1.7. It also inhibits Kv2.1 channel (IC50 = 700 nM).
• Activity: Blocker
• InChI: InChI=1S/C174H241N47O46S6/c1-89(2)143(168(261)206-115(53-55-141(234)235)153(246)196-92(5)170(263)221-63-29-47-132(221)173(266)267)217-146(239)91(4)195-163(256)126-85-270-273-88-129-166(259)215-128-87-272-269-83-124(213-155(248)114(52-54-140(232)233)198-135(227)77-188-147(240)105(179)70-142(236)237)151(244)189-75-133(225)187-76-134(226)201-118(64-94-30-8-7-9-31-94)158(251)207-122(69-99-74-186-109-39-17-13-35-104(99)109)161(254)208-121(68-98-73-185-108-38-16-12-34-103(98)108)160(253)204-112(41-19-23-57-176)154(247)212-125(152(245)193-78-136(228)197-110(44-26-60-182-174(180)181)148(241)190-79-137(229)199-116(43-21-25-59-178)171(264)220-62-28-46-131(220)172(265)219-61-27-45-130(219)167(260)216-129)84-268-271-86-127(211-145(238)90(3)194-157(250)117(65-95-48-50-100(224)51-49-95)200-138(230)80-191-149(242)111(203-164(128)257)40-18-22-56-175)165(258)210-123(82-222)162(255)205-113(42-20-24-58-177)156(249)218-144(93(6)223)169(262)209-119(66-96-71-183-106-36-14-10-32-101(96)106)150(243)192-81-139(231)202-120(159(252)214-126)67-97-72-184-107-37-15-11-33-102(97)107/h7-17,30-39,48-51,71-74,89-93,105,110-132,143-144,183-186,222-224H,18-29,40-47,52-70,75-88,175-179H2,1-6H3,(H,187,225)(H,188,240)(H,189,244)(H,190,241)(H,191,242)(H,192,243)(H,193,245)(H,194,250)(H,195,256)(H,196,246)(H,197,228)(H,198,227)(H,199,229)(H,200,230)(H,201,226)(H,202,231)(H,203,257)(H,204,253)(H,205,255)(H,206,261)(H,207,251)(H,208,254)(H,209,262)(H,210,258)(H,211,238)(H,212,247)(H,213,248)(H,214,252)(H,215,259)(H,216,260)(H,217,239)(H,218,249)(H,232,233)(H,234,235)(H,236,237)(H,266,267)(H4,180,181,182)
• InChIKey: OKELXNUZHJLTAQ-UHFFFAOYSA-N
• Solubility: Soluble in aqueous buffer
• Appearance: White lyophilised solid
• Reference:
  • Jingzhaotoxin-III (JZTX-III) is a peptide toxin isolated from the venom of the Chinese spider Chilobrachys jingzhao that inhibits Nav channels of rat cardiac myocytes by modifying voltage-dependent gating and also binds to Kv2.1 channel (Kd=0.43 μM) with an action model similar to that of hanatoxin1 and SGTx1. The solution structure of JZTX-III was determined by 1H 2D NMR method. The toxin adopts an ICK motif composed of three β-strands connected by four turns. Structural comparison of JZTX-III with those of other ICK motif peptides shows that they all adopt a conserved surface profile, a hydrophobic patch surrounded by charged residues, which might be the crucial site for voltage-gating ion channel inhibition. Furthermore, the similar action model of JZTX-III affecting both Kv and Nav channels implies that JZTX-III recognized a conserved receptor within the voltage sensing domains, which is similar to that of hanatoxin1 binding to both Kv and Cav channels.
  • Solution structure of Jingzhaotoxin-III, a peptide toxin inhibiting both Nav1.5 and Kv2.1 channels
• Purity: >98%