kv1.3 channels

PAP-1 (5-(4-Phenoxybutoxy)psoralen) 是口服活性的Kv1.3选择性阻滞剂 (EC50=2 nM)。它依赖性阻止 Kv1.3，并优先与通道的 C 型失活状态结合来发挥作用。

UK 78282 hydrochloride，一种新型有效且具有选择性的 Kv1.3 阻滞剂。UK 78282 hydrochloride 抑制 Kv1.3 电压门控钾通道，抑制人 T 细胞活化。

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)

OSK-1 is a potent potassium channel blocker belonging to the α-KTx3 toxins. It exhibits IC50 values of 0.6 nM, 5.4 nM, and 0.014 nM for Kv1.1, Kv1.2, and Kv1.3 channels, respectively. Additionally, OSK-1 acts as a moderate blocker of the calcium-activated KCa3.1 channel, with an IC50 of 225 nM. Consequently, OSK-1 finds application as an immunosuppressive drug.

Jingzhaotoxin-IX是由35个氨基酸残基组成的C端酰胺化神经毒素。该化合物既抑制电压门控钠通道（包括河豚毒素抗性和河豚毒素敏感亚型）又抑制Kv2.1通道，但对延迟整流钾通道Kv1.1、1.2和1.3无效。

Hemitoxin为一种蝎毒肽，作用于K+通道阻滞剂。其能够阻断表达于非洲爪蟾卵母细胞的大鼠Kv1.1、Kv1.2和Kv1.3通道，对应IC50值为13 nM、16 nM及2 nM。

Aam-KTX，一种从蝎子Mesobuthus eupeus毒液中提取的毒性肽类Kv通道抑制剂，对Kv1.3和Kv1.1的IC50值分别为1.1 nM和＞750 nM。Aam-KTX在研究自身免疫性疾病方面显示出潜在应用价值。

KTX-Sp2为钾通道毒素，能高效阻断三种外源电压门控钾通道Kv1.1、Kv1.2和Kv1.3。该化合物还能抑制内源性Kv1.3通道，降低Jurkat T细胞内Ca2+信号并抑制其活化后的IL-2分泌。

Ssm Spooky Toxin是从Scolopendra mutilans中分离出的化合物，其特点是有效抑制KCNQ（电压门控钾通道家族7）通道，表现出对血液和呼吸系统的致命毒性。Ssm Spooky Toxin对Kv7.4、Kv1.3和Shal通道的IC50值分别为2.8 μM、5.26 μM和0.1-0.3 M，且能够通过针对T细胞中的KV1.3通道抑制细胞因子的产生，在蜈蚣的循环系统中起着关键作用。

Potent KV1.3 channel blocker (IC50 = 36 pM). Displays no effect at calcium-activated channels. Reduces VEGF-induced transmembrane calcium influxes and nitric oxide production in human endothelial cells.

Potent Shaker K+ channel blocker (Ki = 0.64 nM). Also inhibits Kv1.3, Kv1.6 and Kv1.1 K+ channels (Ki values are 4, 37 and 44 pM respectively).

Extremely potent KV1.3 channel blocker (Kd = 23 pM for mKV1.3 currents). Selective for KV1.3 over other mammalian potassium channels (IC50 values are 23, 1800, 10500, 37000 and 39000 pM for mKV1.3, mKV1.1, hKV1.6, mKV1.4 and rKV1.2 respectively, and >1000