Cbl-b-IN-2

Cbl-b-IN-2 (Example 8) is an orally bioavailable compound, can inhibit the E3 enzyme Casitas B-lineage lymphoma proto-oncogene-b (Cbl-b) in the ubiquitin proteasome pathway. Cbl-b-IN-2 can be used to modulate the immune system and diseases amenable to immune system modulation. Cbl-b-IN-2 (Example 8) also may be administered to an individual with cancer, either alone or as part of a combination, with one or more of an immune checkpoint inhibitor, an anti-neoplastic agent, and radiation agent[1].

Research Areas >> Cancer

Research Areas >> Inflammation/Immunology

Signaling Pathways >> PROTAC >> E3 Ligase Ligand-Linker Conjugate

Cbl-b-IN-2 (Example 8) is a Cbl-b inhibitor with IC50 values range of 5.1-100 nM and ﹤1 nM in high and low concentration of Cbl-b, respectively[1]. Cell Viability Assay[1] Cell Line: Immune cell Concentration: 0.125 nM, 0.15 nM Incubation Time: 1 h Result: Showed Cbl-b activity with an with IC50 values range of 5.1-100 nM and ﹤1 nM in high and low concentration of Cbl-b, respectively.

[1]. Arthur T. Sands, et al. 3-substituted piperidine compounds for cbl-b inhibition, and use of a cbl-b inhibitor in combination with a cancer vaccine and/or oncolytic virus. Patent WO 2020210508A1.