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

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.

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.

CBL 0100 free base is an HIV-1 transcription inhibitor that blocks HIV-1 replication and reactivation in vitro and in ex vivo models. It targets the chromatin-associated transcription (FACT) complex, reducing the occupancy of RNA Polymerase II and FACT in the HIV-1 promoter region, and can be used as a latency-reversing agent (LRA) in cART therapy.

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-28 (Compound B2) is an orally active Cbl-b inhibitor. It enhances the function of immune cells by promoting the secretion of cytokines like IL-2 and modulating the phosphorylation levels of key proteins in the T cell receptor signaling pathway. Cbl-b-IN-28 is applicable in cancer immunology research.

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-20 (Example 50) is an inhibitor of casitas B-lineage lymphoma proto-oncogene-b (Cbl-b), with an IC50 value of less than 100 nM.

Cbl-b-IN-29 is an orally active inhibitor of CBL-B. It effectively binds to the active site of CBL-B, thereby inhibiting the function of the immune E3 ubiquitin ligase. Cbl-b-IN-29 can induce the release of IL-2 from Jurkat cells with an EC50 of 159 nM. This compound exhibits significant antitumor efficacy in vivo, showing good tolerance with no adverse effects observed. Cbl-b-IN-29 is applicable in cancer immunotherapy and related studies involving colon cancer and tumor immunotherapy combinations.

Cbl-b-IN-30 is an orally active inhibitor of Casitas B-lineage lymphoma-b (CBLB). It specifically binds to CBLB and inhibits its E3 ubiquitin ligase activity, with an IC50 value of 9.1 nM. Cbl-b-IN-30 promotes IL-2 secretion (EC50 value of 187.5 nM) and enhances T cell activation. This compound also exhibits antitumor activity and can induce immune memory. It is useful for colon cancer research.

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.

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].