Selective, high affinity α4β1 (Very Late Antigen 4; VLA-4) inhibitor; Displays 200-fold selectivity for the activated form of α4β1 (KD = 70 pM; IC50 = 0.004 μM).
CAT No: R1096
CAS No:187735-94-0
Synonyms/Alias:BIO-1211;187735-94-0;BIO 1211;UNII-61G4E2353I;BIO1211;L-Proline, N-((4-((((2-methylphenyl)amino)carbonyl)amino)phenyl)acetyl)-L-leucyl-L-alpha-aspartyl-L-valyl-;61G4E2353I;CHEMBL88478;(2S)-1-[(2S)-2-[[(2S)-3-carboxy-2-[[(2S)-4-methyl-2-[[2-[4-[(2-methylphenyl)carbamoylamino]phenyl]acetyl]amino]pentanoyl]amino]propanoyl]amino]-3-methylbutanoyl]pyrrolidine-2-carboxylic acid;L-Proline, N-(2-(4-((((2-methylphenyl)amino)carbonyl)amino)phenyl)acetyl)-L-leucyl-L-alpha-aspartyl-L-valyl-;(2-(4-(3-(o-tolyl)ureido)phenyl)acetyl)-L-leucyl-L-aspartyl-L-valyl-L-proline;N-((4-((((2-methylphenyl)amino)carbonyl)amino)phenyl)acetyl)-leucyl-aspartyl-valyl-proline;L-PROLINE, N-((4-((((2-METHYLPHENYL)AMINO)CARBONYL)AMINO)PHENYL)ACETYL)-L-LEUCYL-L-.ALPHA.-ASPARTYL-L-VALYL-;MFCD02259692;MPUPA-LDVP;;GTPL6589;SCHEMBL1223367;GLXC-01821;BDBM50074661;AKOS024457866;DA-71489;FM111090;HY-14126;MS-31193;CS-0003215;G13126;BRD-K03399463-001-01-6;Q27075284;(S)-1-{(S)-2-[(S)-3-Carboxy-2-((S)-4-methyl-2-{2-[4-(3-o-tolyl-ureido)-phenyl]-acetylamino}-pentanoylamino)-propionylamino]-3-methyl-butyryl}-pyrrolidine-2-carboxylic acid;(S)-1-{(S)-2-[3-Carboxy-2-((1S,5S)-4-methyl-2-{2-[4-(3-o-tolyl-ureido)-phenyl]-acetylamino}-pentanoylamino)-propionylamino]-3-methyl-butyryl}-pyrrolidine-2-carboxylic acid;192390-59-3;L-PROLINE, N-(2-(4-((((2-METHYLPHENYL)AMINO)CARBONYL)AMINO)PHENYL)ACETYL)-L-LEUCYL-L-.ALPHA.-ASPARTYL-L-VALYL-;
BIO 1211 is a highly selective small-molecule antagonist of the α4β1 integrin (also known as very late antigen-4, VLA-4), a cell surface receptor critically involved in cell adhesion, migration, and immune cell trafficking. As a member of the integrin inhibitor compound class, BIO 1211 is widely recognized for its ability to modulate integrin-mediated signaling pathways, providing researchers with a valuable tool to dissect the functional roles of α4β1 integrins in various cellular and molecular contexts. Its strong binding affinity and selectivity profile make it particularly useful for studies aiming to elucidate the mechanistic basis of cell-extracellular matrix interactions, immune cell dynamics, and related physiological or pathological processes.
Cell Adhesion Research: In the study of cell adhesion mechanisms, BIO 1211 serves as a robust probe for selectively inhibiting α4β1 integrin-mediated binding events. By blocking the interaction between VLA-4 and its natural ligands such as vascular cell adhesion molecule-1 (VCAM-1) or fibronectin, the compound enables detailed investigation of integrin-dependent adhesion processes. This is especially valuable in experimental systems where precise modulation of cell attachment to the extracellular matrix is required to understand the molecular determinants of tissue organization, cell migration, or immune cell localization.
Leukocyte Trafficking Studies: The compound is extensively utilized in research focused on leukocyte trafficking and immune cell migration. By specifically antagonizing α4β1 integrin function, it allows for controlled disruption of leukocyte adhesion and transmigration across endothelial barriers. This capability is instrumental in dissecting the stepwise mechanisms governing immune surveillance and inflammatory responses, as well as in modeling disease-relevant scenarios involving aberrant leukocyte infiltration.
Signal Transduction Analysis: BIO 1211 is a valuable tool for exploring integrin-dependent intracellular signaling cascades. Inhibition of α4β1 integrin with this molecule can help delineate the downstream signaling pathways triggered by cell-matrix interactions, including those involving focal adhesion kinase (FAK), phosphoinositide 3-kinase (PI3K), and mitogen-activated protein kinase (MAPK) pathways. Such studies are essential for clarifying the role of integrin signaling in cell survival, proliferation, and differentiation across diverse cell types.
Tumor Microenvironment Modeling: Within cancer research, the selective inhibition of α4β1 integrin by this antagonist is leveraged to investigate the contribution of integrin-mediated adhesion to tumor cell behavior and microenvironmental dynamics. The compound facilitates studies into how malignant and stromal cells interact with the extracellular matrix, migrate, and respond to microenvironmental cues. These insights are crucial for understanding processes such as tumor invasion, metastasis, and the formation of pre-metastatic niches.
Drug Discovery and Screening: In the context of early-stage drug development, BIO 1211 is frequently employed as a reference compound or positive control in high-throughput screening assays targeting integrin pathways. Its well-characterized mechanism of action and specificity for α4β1 integrin make it an indispensable standard for validating assay performance and benchmarking the activity of novel integrin-targeting molecules. This application supports the identification and optimization of new candidates with potential to modulate integrin-related biological processes for research purposes.
3. Autoinhibition and phosphorylation-induced activation of phospholipase C-γ isozymes
4. TMEM16F and dynamins control expansive plasma membrane reservoirs
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