Ion & Other Channels
Biological systems function through the complex interplay of a multitude of enzymes, transporters, ion channels, receptors, and other reactive molecules. The actions of these effectors can be modified by endogenous ligands, externally applied chemical reagents, or genetic or epigenetic changes to relevant genes. Pathological states can result when the actions of any of these biological effectors are perturbed.
Herboxidiene (142861-00-5) is a novel polyketide fermentation product produced by Streptomyces chromofuscus, originally discovered by screening for herbicidal activity. Potent and selective inhibitor of spliceosome subunit SF3b.2 Specifically targets SAP155, a subunit of SF3b responsible for pre-mRNA splicing.3 Displays anti-angiogenic activity via down-regulation of VEGFR-2 and HIF-1α.4 Spliceosome inhibitors have attracted enormous attention due to their potential use in cancer treatment.5
YM-254890 (568580-02-9) is a novel Gαq/11 inhibitor.1 U46619-induced platelet aggregation is inhibited but phorbol ester- or ionophore-induced aggregation is not2 (IC50 = 0.1-0.2 μM)1. It blocks Pasteurella multocida toxin-mediated activation of Gαq.3 A highly useful new tool for studying Gαq/11-coupled receptor signaling and resulting cellular events.4
7-Cl-O-Nec1 (852391-15-2) is a necrostatin-1 (Cat.# 10-1162) analogue with superior potency (IC50 = 206nM vs 494nM), selectivity and metabolic stability in blocking RIP1.1,2 7-Cl-O-Nec1 shows no off-target inhibition of indolamine-2,3-deoxygenase (IDO) in contrast to Necrostatin-1 (Nec-1).3,4 7-Cl-O-Nec1 showed higher activity in inhibiting necroptosis in Jurkat cells than Necrostatin-1 (EC50 = 210 nM vs. EC50 = 490 nM), no non-specific cytotoxicity at high concentrations (100 μM) and reasonable pharmacokinetic characteristics when used in mice.2 7-Cl-O-Nec1 is recommended for cellular and in vivo use over Necrostatin-1.5