cblbin1

Cbl-b-IN-1 is a potent Cbl-b inhibitor (IC50 <100 nM) with potential anticancer activity for the study of intestinal inflammation.

PROTAC Cbl-b-IN-1 is a PROTAC that targets Cbl-b. It is composed of the PROTAC targeting protein ligand Cbl-b-IN-21, PROTAC Linker Cbz-Pip-2C-Pip-C-Pip, and the E3 ubiquitin ligase ligand (3S)Lenalidomide-5-Br. The conjugate of the E3 ubiquitin ligase ligand and Linker is (3S)Lenalidomide-5-Pip-C-Pip-2C-Pip.

Cbl-b-IN-15 (compound 25) is an inhibitor of the RING finger E3 ubiquitin ligase Cbl, demonstrating an IC50 of 15 nM. Cbl-b refers to Casitas B-lineage Lymphoma proto-oncogene-b, which can inhibit the activation of T cells, natural killer (NK) cells, and B cells. Cbl-b-IN-15 can activate T cell function with an EC50 of 0.41 μM.

Cbl-b-IN-16 (compound 31) is an orally active inhibitor of the RING E3 ligase Cbl-b, with an IC50 of 30 nM. It enhances IL-2 production in human T cells with an EC50 of 230 nM and exhibits antitumor activity.

Cbl-b-IN-18 (compound 51) is an inhibitor of the E3 ubiquitin ligase Cbl-b, effectively blocking Cbl-b phosphorylation with an IC50 of less than 100 nM.

Cbl-b-IN-17 (Example-40) is an inhibitor of Cbl-b, with an IC50 value of less than 100 nM.

Cbl-b-IN-19 (Compound 49) is an inhibitor of the E3 ligase Cbl-b, effectively suppressing its phosphorylation with an IC50 of less than 100 nM.

Cbl-b-IN-10 (Compound 463) is a potent inhibitor of both casitas B-lineage lymphoma-b (Cbl-b) and c-Cbl, with half-maximal inhibitory concentrations (IC50s) of 6.0 nM and 3.5 nM, respectively [1].

Cbl-b-IN-11 (Compound 466) is an inhibitor of casitas B-lineage lymphoma-b (Cbl-b) and c-Cbl, with half-maximal inhibitory concentrations (IC50s) of 6.4 nM and 6.1 nM, respectively [1].

Cbl-b-IN-12 (Example 10) is a CBL-B inhibitor with an IC50 of less than 100 nM [1].

Cbl-b-IN-13 (Example 520) is a potent Cbl-b inhibitor with an IC50 of less than 100 nM, capable of activating T-cells [1].