6 October 2025
Vanin 1 and vanin 2 are members of the vascular non-inflammatory molecule (vanin) family. These ectoenzymes catalyze the conversion of pantetheine into pantothenic acid and cysteamine, playing a pivotal role in cellular redox homeostasis. Their reaction products can interfere with glutathione biosynthesis, a critical pathway for maintaining oxidative balance. Vanin 1 is predominantly expressed in immune-competent tissues, intestine, liver, and kidney, while vanin 2 is broadly expressed, with the highest levels in spleen, kidney, and blood. Vanin 1 knockout mice exhibit enhanced resistance to oxidative stress and inflammation, suggesting a potential role of vanin signaling in inflammatory and oxidative stress-related disorders.
To advance research into vanin biology, we offer BI-4122, a highly potent and selective dual inhibitor of vanin 1 and vanin 2. BI-4122 is well-suited for both intravenous (i.v.) and oral (p.o.) administration, due to its favorable pharmacokinetic properties. To support robust experimental design, we also provide BI-9534, a structurally similar but inactive analogue, as a negative control.
Interested researchers will receive both BI-4122 and BI-9534 free of charge and retain full ownership of their results. We encourage you to publish your findings to advance the field of vanin biology.
No registration required
Subscribe to our newsletter to stay updated as we add new molecules to opnMe.com.
About BI-4122:
BI-4122 is an orally bioavailable small molecule that reversibly and competitively inhibits vanin enzymatic activity. It demonstrates high potency, with IC50 values of 0.3 nM for vanin 1 and 1.5 nM for vanin 2. In a human whole blood assay, BI-4122 exhibits single-digit nanomolar potency (IC50 = 2 nM).
The compound shows excellent solubility across all pH values and high permeability in Caco-2 assays. It also has a favorable selectivity profile, with no significant activity observed across a panel of 268 kinases and 68 enzymes/receptors.
BI-4122 is suitable for once- or twice-daily oral dosing in acute or sub-chronic in vivo experiments.
About opnMe:
opnMe.com, the open innovation portal of Boehringer Ingelheim, fosters science and collaboration initiatives in areas of high unmet medical need. As part of our first pillar, the “Molecules to Order”, we share well-characterized tool compounds free of charge with no IP strings attached. With our “opn2EXPERTS” and “techMATCH” programs, we enlist scientific advice on key biologic issues to fuel further drug discovery and deliver novel solutions that benefit unmet patient needs. Our opn2TALENTS PostDoc grants, provide an opportunity for high-caliber talents to pitch their scientific approaches for well-defined research questions to conduct their research at one of our discovery research sites.