kv1.3-in-2

KV1.3-IN-2 (Compound I) selectively inhibits the kv1.3 potassium channel without affecting the hERG channel. It is applicable in research related to immune-associated diseases such as psoriasis, rheumatoid arthritis, and systemic lupus erythematosus.

β-Defensin-1 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts.1It inhibits the growth ofB. adolescentis,L. acidophilus,B. breve,B. vulgatus,L. fermentum,B. longum, andS. thermophilusin an antimicrobial radial diffusion assay.2β-Defensin-1 also inhibits the growth of periodontopathogenic and cariogenic bacteria, includingP. gingivalisandS. salivarius, and of susceptibleM. tuberculosisH37Rv but not of resistantM. tuberculosisRM22 when used at a concentration of 128 μg/ml.3,4It blocks human and mouse Kv1.3 voltage-gated potassium channels (IC50s = 11.8 and 13.2 μM, respectively).5Overexpression of β-defensin-1 in the human oral squamous cell carcinoma (OSCC) cell lines HSC-3, UM-1, and SCC-9 increases migration and invasion but not proliferation.6 1.Lehrer, R.I.Primate defensinsNat. Rev. Microbiol.2(9)727-738(2004) 2.Schroeder, B.O., Ehmann, D., Precht, J.C., et al.Paneth cell α-defensin 6 (HD-6) is an antimicrobial peptideMucosal Immunol.8(3)661-671(2015) 3.Ouhara, K., Komatsuzawa, H., Yamada, S., et al.Susceptibilities of periodontopathogenic and cariogenic bacteria to antibacterial peptides, β-defensins and LL37, produced by human epithelial cellsJ. Antimicrob. Chemother.55(6)888-896(2005) 4.Fattorini, L., Gennaro, R., Zanetti, M., et al.In vitro activity of protegrin-1 and beta-defensin-1, alone and in combination with isoniazid, against Mycobacterium tuberculosisPeptides25(7)1075-1077(2004) 5.Feng, J., Xie, Z., Yang, W., et al.Human beta-defensin 1, a new animal toxin-like blocker of potassium channelToxicon113(2016) 6.Han, Q., Wang, R., Sun, C., et al.Human beta-defensin-1 suppresses tumor migration and invasion and is an independent predictor for survival of oral squamous cell carcinoma patientsPLoS One9(3)e91867(2014)

Dalazatide (ShK-186) is a specific inhibitor of the Kv1.3 potassium channel, used in research on autoimmune conditions such as multiple sclerosis (MS), lupus erythematosus, psoriasis, rheumatoid arthritis, type 1 diabetes, and inflammatory bowel disease [1] [2] [3].

Dalazatide (ShK-186) TFA, a precise Kv1.3 potassium channel peptide inhibitor, is employed in researching autoimmune conditions, including multiple sclerosis (MS), lupus erythematosus, psoriasis, rheumatoid arthritis, type 1 diabetes, and inflammatory bowel disease [1] [2] [3].

Noxiustoxin, a toxin extracted from the venom of the Mexican scorpion Centruroides noxius, inhibits both the voltage-dependent potassium channel (Kv1.3, IC50 = 360 nM) and the calcium-activated potassium channel. It is significant in the pathophysiology of neuroinflammatory diseases [1] [2].

ShK toxin, isolated from the Caribbean sea anemone (Stichodactyla helianthus), is an inhibitor of the voltage-dependent potassium channel (Kv1.3 channel). It competes with dendrotoxin I and α-dendrotoxin in binding to rat brain synaptosomal membranes and promotes acetylcholine release. Additionally, ShK toxin reduces K+ currents in cultured rat dorsal root ganglion neurons and inhibits T lymphocyte proliferation [1] [2].

BmP02, a compound isolated from Chinese scorpion (Buthus martensi Karsch) venom, acts as a selective Kv1.3 channel blocker and a highly-selective Kv4.2 modulator. It delays Kv4.2 inactivation in HEK293T cells, exhibiting an EC50 of approximately 850 nM, and inhibits the transient outward potassium currents (Ito) in ventricular muscle cells [1] [2].

HsTX1, a 34-residue, C-terminally amidated peptide isolated from the scorpion Heterometrus spinnifer, features four disulfide bridges and acts as a potassium channel inhibitor. It exhibits an IC50 of 12 pM for Kv1.3, impeding T EM cell activation and diminishing inflammation in autoimmune conditions [1] [2] [3].

Hemitoxin, a scorpion-venom peptide, acts as a K+ channel blocker, selectively inhibiting rat Kv1.1, Kv1.2, and Kv1.3 channels expressed in Xenopus oocytes, with IC50 values of 13 nM, 16 nM, and 2 nM, respectively [1].

KTX-Sp2, a potassium channel toxin, effectively blocks exogenous voltage-gated potassium channels Kv1.1, Kv1.2, and Kv1.3, as well inhibits the endogenous Kv1.3 channel and suppresses Ca2+ signaling in Jurkat T cells. Additionally, KTX-Sp2 inhibits IL-2 secretion from activated Jurkat T cells [1].

Ssm Spooky Toxin, derived from Scolopendra mutilans, exhibits potent lethality affecting both hematological and respiratory systems primarily through the inhibition of KCNQ (voltage-gated potassium channel family 7) channels. It demonstrates IC50 values of 2.8 μM for Kv7.4, 5.26 μM for Kv1.3, and 0.1-0.3 M for the Shal channel, respectively. Additionally, this toxin impedes cytokine production by selectively targeting the KV1.3 channel in T cells and is crucial for the centipede's circulatory system functions [1] [2] [3].

Nalanthalide, serving as a voltage-gated potassium channel Kv1.3 blocker (IC50 = 3.9 µM) with potential immunosuppressive properties, is applicable in the research of inflammatory immune diseases including neuroinflammation [1] [2].