cbl-b-in-1

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-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].

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-3 is a potent inhibitor of casitas b lineage lymphoma proto-oncogene-b (Cbl-b) (ic50 < 1 nM).

(3S)Lenalidomide-5-Pip-C-Pip-2C-Pip serves as an E3 Ligase Ligand-Linker Conjugate and is utilized in the synthesis of PROTAC Cbl-b-IN-1.

Siamycin I is a tricyclic peptide originally isolated from Streptomyces and has antiviral and antibacterial activities. It is active against laboratory strains and clinical isolates of HIV-1 (ED50s = 0.05-0.45 and 0.89-5.7 μM, respectively), as well as the CBL-20 strain of HIV-2 (ED50 = 0.45 μM), in vitro. Siamycin I inhibits HIV-induced fusion of C8166 T cells with HIV-1-infected CEM-SS cells with an ED50 value of 0.08 μM. It is also active against B. subtilis, M. luteus, and S. aureus (MICs = 1.6-6.3 μg/ml). Siamycin I inhibits autophosphorylation of the E. faecalis quorum sensing kinase FsrC induced by gelatinase biosynthesis-activating pheromone (GBAP).

Cbl-b-IN-6 (Compound 246) is an inhibitor of casitas B-lineage lymphoma-b (Cbl-b) and c-Cbl, with half-maximal inhibitory concentrations (IC50s) of 6.7 nM for Cbl-b and 5.2 nM for c-Cbl, respectively [1].

Cbl-b-IN-7 (Compound 248) is an inhibitor of casitas B-lineage lymphoma-b (Cbl-b) and c-Cbl, with half-maximal inhibitory concentrations (IC50s) of 6.7 nM and 5.2 nM, respectively [1].

Cbl-b-IN-8 (Compound 293) is an inhibitor of casitas B-lineage lymphoma-b (Cbl-b) and c-Cbl, with half maximal inhibitory concentrations (IC50s) of 5.5 nM and 7.8 nM, respectively [1].

Cbl-b-IN-9 (Compound 300) is a potent inhibitor targeting casitas B-lineage lymphoma-b (Cbl-b) and c-Cbl, with half-maximal inhibitory concentrations (IC50s) of 5.6 nM and 4.7 nM, respectively [1].