Chemicals & Small Molecules

Mambalgin 1 (Legacy Tebubio ref. 282TP2003). Selective ASIC1a inhibitor (IC50 values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively). Binds to closed/inactive channel. Selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Increases latency of withdrawal response in mouse tail-flick and paw-flick tests. Analgesic.

Margatoxin (Legacy Tebubio ref. 282TP2004). 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.

Kisspeptin-54(human) (Legacy Tebubio ref. 282TP2005). Potent endogenous ligand of the kisspeptin receptor (KISS1, GPR54). Binds with high affinity to rat and human KISS1 receptors with Ki values of 1.80 and 1.45 nM respectively. Inhibits chemotaxis, invasion and metastasis of human melanomas and breast carcinomas. Stimulates gonadotropin secretion following i.c.v. administration.

LDV (Legacy Tebubio ref. 282TP2006). α4β1 integrin (VLA-4) ligand (Kd ~ 12 nM). Non-fluorescent derivative of LDV FITC.

Lei-Dab7 (Legacy Tebubio ref. 282TP2007). High affinity, selective KCa2.2 (SK2) channel blocker (Kd = 3.8 nM). Exhibits >200-fold selectivity for KCa2.2 over KCa2.1, KCa2.3, KCa3.1, IK, Kv and Kir2.1. Increases theta-burst responses and increases LTP in rat hippocampal slices in vitro. Convulsive in vivo.

Lyn peptide inhibitor (Legacy Tebubio ref. 282TP2008). Cell-permeable inhibitor of Lyn-dependent effects of the IL-5 receptor. Blocks binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors, blocking Lyn activation. Inhibits IL-5 receptor-mediated eosinophil differentiation and survival in vitro. Inhibits airway eosinophilic inflammation in mouse model of asthma.

Lyn peptide inhibitor acetate (Legacy Tebubio ref. 282TP2008L). Lyn peptide inhibitor acetate is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor can be used for study of asthma, allergic, and other eosinophilic disorders.

K41498 (Legacy Tebubio ref. 282TP2009). Potent and highly selective CRF2 receptor antagonist (Ki values are 0.66, 0.62 and 425 nM for human CRF2α, CRF2β and CRF1 receptors respectively). Inhibits sauvagine-stimulated cAMP accumulation in hCRF2α- and hCRF2β-expressing cells. In rats in vivo, blocks urocortin-induced hypotension following systemic administration.

K 41498 aceate (Legacy Tebubio ref. 282TP2009L). K41498 acetate, an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF2α- and hCRF2β-expressing cells. K41498 acetate is a potent and highly selective antagonist CRF2 receptor with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF2α, CRF2β and CRF1 receptors respectively.