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ADWX 1

* Please kindly note that our products are not to be used for therapeutic purposes and cannot be sold to patients.

ADWX 1 has been found to be a Kv1.3 channel blocker and could probably ameliorate autoimmune encephalomyelitis at some extent.

Category

Peptide Inhibitors

Catalog number

BAT-010222

Molecular Formula

C169H281N57O46S7

Molecular Weight

4071.86

Specification
Reference Reading

IUPAC Name

6-amino-2-[[1-[2-[[47-[[6-amino-2-[[2-[[4-amino-2-[[2-[[2-[(2-amino-3-methylbutanoyl)amino]acetyl]amino]-3-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-methylbutanoyl]amino]hexanoyl]amino]-15,39,50,72,89-pentakis(4-aminobutyl)-78-(2-amino-2-oxoethyl)-62-(3-amino-3-oxopropyl)-33-benzyl-30,59-bis(3-carbamimidamidopropyl)-18-(carboxymethyl)-81-(1-hydroxyethyl)-56-(hydroxymethyl)-4,53-bis(1H-imidazol-4-ylmethyl)-21-methyl-86-(2-methylpropyl)-27-(2-methylsulfanylethyl)-2,5,13,16,19,22,25,28,31,34,37,40,48,51,54,57,60,63,71,74,77,80,83,84,87,90,96-heptacosaoxo-9,10,44,45,67,68-hexathia-3,6,14,17,20,23,26,29,32,35,38,41,49,52,55,58,61,64,70,73,76,79,82,85,88,91,97-heptacosazatetracyclo[40.27.14.1412,65.091,95]heptanonacontane-7-carbonyl]amino]-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]amino]hexanoic acid

Synonyms

ADWX1

Appearance

White Lyophilized Solid

Purity

>98%

Sequence

VGXNVKC(1)KHSRQC(2)LKPC(3)KDAGMRFGKC(1)XNGKC(2)HC(3)XPK

Storage

Store at -20°C

InChI

InChI=1S/C169H281N57O46S7/c1-13-88(8)132(221-128(236)75-192-161(265)130(180)86(4)5)163(267)213-111(68-124(179)232)151(255)222-131(87(6)7)162(266)204-99(41-21-28-55-174)144(248)216-114-77-274-278-81-118-157(261)223-133(90(10)228)164(268)212-110(67-123(178)231)137(241)191-74-127(235)196-95(37-17-24-51-170)138(242)215-116-79-276-275-78-115(217-145(249)102(48-49-122(177)230)203-140(244)100(44-31-58-187-168(181)182)200-152(256)113(76-227)214-149(253)108(65-93-70-185-83-193-93)209-141(245)97(201-153(114)257)39-19-26-53-172)155(259)207-106(63-85(2)3)148(252)205-104(42-22-29-56-175)165(269)225-60-33-46-120(225)160(264)220-117(80-277-279-82-119(219-150(254)109(210-156(116)260)66-94-71-186-84-194-94)158(262)224-134(91(11)229)166(270)226-61-34-47-121(226)159(263)206-105(167(271)272)43-23-30-57-176)154(258)202-98(40-20-27-54-173)142(246)211-112(69-129(237)238)147(251)195-89(9)135(239)189-72-125(233)198-103(50-62-273-12)146(250)199-101(45-32-59-188-169(183)184)143(247)208-107(64-92-35-15-14-16-36-92)136(240)190-73-126(234)197-96(139(243)218-118)38-18-25-52-171/h14-16,35-36,70-71,83-91,95-121,130-134,227-229H,13,17-34,37-69,72-82,170-176,180H2,1-12H3,(H2,177,230)(H2,178,231)(H2,179,232)(H,185,193)(H,186,194)(H,189,239)(H,190,240)(H,191,241)(H,192,265)(H,195,251)(H,196,235)(H,197,234)(H,198,233)(H,199,250)(H,200,256)(H,201,257)(H,202,258)(H,203,244)(H,204,266)(H,205,252)(H,206,263)(H,207,259)(H,208,247)(H,209,245)(H,210,260)(H,211,246)(H,212,268)(H,213,267)(H,214,253)(H,215,242)(H,216,248)(H,217,249)(H,218,243)(H,219,254)(H,220,264)(H,221,236)(H,222,255)(H,223,261)(H,224,262)(H,237,238)(H,271,272)(H4,181,182,187)(H4,183,184,188)

InChI Key

KOXLLJFKLFSCAF-UHFFFAOYSA-N

Canonical SMILES

CCC(C)C(C(=O)NC(CC(=O)N)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NC1CSSCC2C(=O)NC(C(=O)NC(C(=O)NCC(=O)NC(C(=O)NC3CSSCC(C(=O)NC(C(=O)NC(C(=O)N4CCCC4C(=O)NC(CSSCC(NC(=O)C(NC3=O)CC5=CNC=N5)C(=O)NC(C(C)O)C(=O)N6CCCC6C(=O)NC(CCCCN)C(=O)O)C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NCC(=O)NC(C(=O)NC(C(=O)NC(C(=O)NCC(=O)NC(C(=O)N2)CCCCN)CC7=CC=CC=C7)CCCNC(=N)N)CCSC)C)CC(=O)O)CCCCN)CCCCN)CC(C)C)NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)CCCCN)CC8=CNC=N8)CO)CCCNC(=N)N)CCC(=O)N)CCCCN)CC(=O)N)C(C)O)NC(=O)CNC(=O)C(C(C)C)N

1. Peptides with therapeutic potential in the venom of the scorpion Buthus martensii Karsch

Yong Wang, Ping Hu, Wenlan Wu, Zhongjie Li Peptides . 2019 May;115:43-50. doi: 10.1016/j.peptides.2019.02.009.

The scorpion Buthus martensii Karsch (BmK) has generated significant interest due to the presence of biologically active peptides in its venom. In the past decade, dozens of different peptides from BmK have been identified. Most of the peptides are neurotoxins and are responsible for the toxicity of BmK venom. Other peptides, including neurotoxins and non-disulfide-bridged peptides, show potential anticancer, antimicrobial, analgesic, and anti-epileptic therapeutic effects. These peptides are attractive candidates for drug development, and peptide derivatives have also been designed to enhance their therapeutic potential, such as ADWX-1 and Kn2-7. In this review, we provide an overview of the most promising peptides found in BmK venom and of modified peptide derivatives showing therapeutic potential.

2. Different residues in channel turret determining the selectivity of ADWX-1 inhibitor peptide between Kv1.1 and Kv1.3 channels

Mai-Li Liu, Ying-Liang Wu, Hong Yi, Ling Jiang, Shi-Jin Yin, Zhi-Jian Cao, Wen-Xin Li, Song Han, Dai-Wen Yang, Hui Liu J Proteome Res . 2008 Nov;7(11):4890-7. doi: 10.1021/pr800494a.

The low selectivity of Kv1 peptide inhibitors for specific isoforms makes them poor candidates for the development of theraputics. Using combined approaches, we showed that the Kv1 turret is the critical determinant for ADWX-1 peptide inhibitor selectivity of Kv1.3 over Kv1.1. Mutation of Kv1.1 turret residues to match the sequence of Kv1.3 lead to increased inhibition of Kv1.1 activity. These studies may lead to improvements in peptide inhibitor drug development.

3. Structural basis of a potent peptide inhibitor designed for Kv1.3 channel, a therapeutic target of autoimmune disease

Ying-Liang Wu, Hong Yi, Zong-Yun Chen, Zhi-Jian Cao, Wen-Xin Li, Song Han, Shi-Jin Yin, Hui Liu J Biol Chem . 2008 Jul 4;283(27):19058-65. doi: 10.1074/jbc.M802054200.

The potassium channel Kv1.3 is an attractive pharmacological target for immunomodulation of T cell-mediated autoimmune diseases. Potent and selective blockers of Kv1.3 are potential therapeutics for treating these diseases. Here we describe the design of a new peptide inhibitor that is potent and selective for Kv1.3. Three residues (Gly(11), Ile(28), and Asp(33)) of a scorpion toxin BmKTX were substituted by Arg(11), Thr(28), and His(33), resulting in a new peptide, named ADWX-1. The ADWX-1 peptide blocked Kv1.3 with picomolar affinity (IC(50), 1.89 pM), showing a 100-fold increase in activity compared with the native BmKTX toxin. The ADWX-1 also displayed good selectivity on Kv1.3 over related Kv1.1 and Kv1.2 channels. Furthermore, alanine-scanning mutagenesis was carried out to map the functional residues of ADWX-1 in blocking Kv1.3. Moreover, computational simulation was used to build a structural model of the ADWX-1-Kv1.3 complex. This model suggests that all mutated residues are favorable for both the high potency and selectivity of ADWX-1 toward Kv1.3. While Arg(11) of ADWX-1 interacts with Asp(386) in Kv1.3, Thr(28) and His(33) of ADWX-1 locate right above the selectivity filter-S6 linker of Kv1.3. Together, our data indicate that the specific ADWX-1 peptide would be a viable lead in the therapy of T cell-mediated autoimmune diseases, and the successful design of ADWX-1 suggests that rational design based on the structural model of the peptide-channel complex should accelerate the development of diagnostic and therapeutic agents for human channelopathies.