Angiogenesis

NX-2127 is an orally effective BTK inhibitor that can induce the degradation of mutated BTKC481S in cells. NX-2127 inhibits the proliferation of TMD8 cells with the BTKC481S mutation more effectively than Ibrutinib. NX-2127 catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3), corresponding to concentrations of 25 nM and 54 nM, respectively. NX-2127 stimulates T cell activation and increases IL-2 production in primary human T cells.

Orbofiban acetate is an orally active platelet membrane glycoprotein IIb/IIIa antagonist that inhibits platelet aggregation.

Parstatin (mouse) TFA is a peptide agonist of the PAR-1 thrombin receptor with cell-penetrating properties and an effective inhibitor of angiogenesis.

Protease-Activated Receptor-1, PAR-1 Agonist is a selective peptide that activates Protease-Activated Receptor-1 (PAR-1), which corresponds to the PAR1 ligand and selectively mimics the action of thrombin through this receptor.

(R/S)-Alicaforsen is the racemic form of Alicaforsen, which consists of both R and S configurations. Alicaforsen is a 20-base length antisense oligonucleotide that inhibits the production of ICAM-1, an important adhesion molecule involved in the migration and transport process of white blood cells to inflammatory sites.

Fradafiban (BIBU-52) hydrochloride is a nonpeptide platelet glycoprotein IIb/IIIa antagonist, which binds to the human platelet GP IIb/IIIa complex with a Kd value of 148 nM.

Atuzabrutinib (SAR 444727) is a potent, selective reversible inhibitor of Btk (Bruton's tyrosine kinase) inhibitor.

Egaptivon pegol sodium is an aptamer, which blocks binding of the von Willebrand Factor (VWF) to platelet GPIb receptors.

Volociximab (M200) is a chimeric human/murine IgG4 antibody IIA1 targeting integrin α5β1 (EC50=0.2 nM).

Rovelizumab is a humanized monoclonal leukointegrin antibody.

JS25 is a selective and covalent inhibitor of BTK that inactivates BTK with an IC50 value of 5.8 nM by chelating Tyr551.

RSH-7 is a potent BTK and FLT3 inhibitor with IC50s of 47, 12 nM, respectively.

Larotinib is a potent broad-spectrum and orally active tyrosine kinase inhibitor (TKI) with EGFR as the main target with an IC50 of 0.6 nM.

JNJ-64264681 is a potent, orally active, selective and irreversible covalent BTK inhibitor.

NRX-0492 is an orally active and potent degrader of BTK.

GBD-9 is a double-mechanism degrader that efficiently degrades BTK and GSPT1 by recruiting the E3 ligase cereblon (CRBN).

BT200 sodium, a pegylated form of the aptamer BT100, inhibits binding of von Willebrand factor (VWF) to platelet glycoprotein GPIb, preventing arterial thrombosis.

KIN-8194 is an orally active dual inhibitor of HCK and BTK, with IC50 values of 0.915 and <0.495 nM, respectively.

BTK-IN-29 (compound 14) is an inhibitor of Btk.

UBX-382 is an orally available proteolysis-targeting chimeras (PROTACs) that target BTK to inactivate B-cell receptor signaling.

BIIB129 is a covalent, selective, small molecule inhibitor of Bruton's tyrosine kinase (BTK) capable of penetrating the blood-brain barrier.

Obtustatin triacetate is a 41-residue non-RGD disintegrin.

A20FMDV2 is a selective αvβ6 integrin inhibitor (IC50: 3 nM), with an activity 1,000-fold more selective for αvβ6 than for other RGD-directed integrins (αvβ3, αvβ5, and α5β1).

Synstatin (92-119) is an anti-tumor agent that inhibits angiogenesis and cancer cell invasion.