btk-in-8

BTK-IN-8 is a potent, selective, peripheral covalent BTK inhibitor with an IC50 value of 0.22 nM and a Kd value of 0.91 nM. BTK-IN-8 exhibits good potency in whole blood CD69 cells with an IC50 value of 0.029 μM.

BTK-IN-41 (Compound 47) is a BTK inhibitor with an IC50 of 5.4 nM. It inhibits diffuse large B-cell lymphoma cells TDM-8 with an IC50 of 13.8 nM.

KIN-8194 is a dual inhibitor of HCK and BTK, effective when administered orally, displaying IC 50 values of 0.915 nM for HCK and <0.495 nM for BTK. It inhibits growth and disrupts integrin-mediated adhesion in BTKi-resistant mantle cell lymphoma (MCL). Additionally, KIN-8194 has shown efficacy in overcoming ibrutinib resistance, enhancing survival in TMD-8 ABC DLBCL xenografted mice [1] [2].

BMX-IN-1 (BMX kinase inhibitor) is a selective inhibitor of bone marrow tyrosine kinase on chromosome X (BMX, IC50 = 8 nM) and the related Bruton's tyrosine kinase (BTK, IC50 = 10.4 nM), but BMX-IN-1 is more than 47-656 fold less potent against Blk, JAK3, EGFR, Itk, or Tec activity.

UBX-382 is an orally administered proteolysis-targeting chimera (PROTAC) designed to target BTK and disrupt B-cell receptor signaling. It demonstrates enhanced degradation of both wild-type and mutant BTK proteins, exhibiting anti-cancer effects in murine xenograft models using TMD-8 cells [1].

BTK-IN-27 (example 8), a potent BTK inhibitor with an IC50 of 0.2 nM, demonstrates anti-proliferative effects in TMD8 cells with an IC50 of less than 5 nM. It is suitable for the research of various conditions including cancer, lymphoma, leukemia, and immunological diseases [1].