cbl

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

Cbl-b-IN-5 is a potent CPL-B inhibitor with IC50 values between 3 and 10 µM. Cbl-b-IN-5 has been used to study cancer and diseases related to the immune system.

Cystathionine β-lyase is a pyridoxal 5′-phosphate (PLP)-dependent enzyme that cleaves the Cβ-Sγ bond of cystathionine to convert L-cysteine into L-homocysteine. Cystathionine β-lyase is involved in the de novo synthesis of methionine in microorganisms and plants and plays an important role in bacterial virulence.

hydrocotarnine is an inhibitor of Cbl.

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-26 (Example A1) is an inhibitor of Cbl-b with a dissociation constant (Kd) of 34.6 nM. It is used in the research of chronic viral infections and cancer.

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

Cbl-b-IN-2 is an orally active biological compound that inhibits the E3 enzyme Casitas b lineage lymphoma proto-oncogene b (Cbl-b) in the ubiquitin proteasome pathway and can be used in the study of diseases that modulate the immune system and are susceptible to regulation by the immune system. Cbl-b-IN-2 can also be used in cancer research alone or in combination with one or more immune checkpoint inhibitors, antitumour agents and radiopharmaceuticals.

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].

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-27 is an inhibitor of the B lymphoma proto-oncogene b (Cbl-b), with an IC50 value of 7 nM. This compound is promising for research into the regulation of effector T cell function, T cells, natural killer (NK) cells, and B cell activation.

Cbl-b-IN-21, a PROTAC target protein ligand (Ligands for Target Protein for PROTACs), serves as a key component in the synthesis process.

CBL0137 hydrochloride (Curaxin-137 hydrochloride) is an inhibitor of the histone chaperone FACT, which also activates p53 and inhibits NF-κB with EC50 values ​​of 0.37 and 0.47 μM, respectively. CBL0137 hydrochloride functionally inactivates the complex that promotes chromatin transcription (FACT), thereby driving effects on p53 and NF-κB and promoting cancer cell death, and when used in combination with cisplatin, CBL0137 hydrochloride has potent anticancer activity against SCLC.

CBL0137 (Curaxin 137), a metabolically stable curaxin, activates p53 (EC50: 0.37 μM) and inhibits NF-κB (EC50: 0.47 μM). It functionally inactivates the facilitates chromatin transcription complex (FACT), driving the effects on p53 and NF-κB and promoting cancer cell death. CBL0137 has broad anticancer activity in mice when administered orally, eradicates drug-resistant cancer stem cells, and potentiates the efficacy of gemcitabine in preClinicalal models of pancreatic cancer.

CBL0100 is an inhibitor of viral transcriptional elongation, blocking both HIV-1 replication and reactivation.

CBLB 612 is both an auxiliary anti-radiation and an anti-tumor agent [1].

(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).