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.

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.

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.

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.

Arsthinol is an antiprotozoal agent which may have anti-cancer activity. It was found that arsthinol, a trivalent organoarsenic compound (dithiarsolane), has been active in vitro on leukemia cell lines and offers a better therapeutic index than arsenic trioxide, as estimated by the ratio LD50/IC50. Arsthinol induced growth inhibition of NB4 cells at lower concentration (IC50 (concentration inhibiting growth by 50%) = 0.78 +/- 0.08 micromol/l after 24 h) than As(2)O(3) (IC50 = 1.60 +/- 0.23 micromol/l after 24 h) or melarsoprol (IC50 = 1.44 +/- 0.08 micromol/l after 24 h). Arsthinol-cyclodextrin complex demonstrated to have was more effective than arsenic trioxide (As2O3) and melarsoprol on the U87 MG cell line. Importantly, in the in vivo study, significant antitumor activity against heterotopic xenografts was observed after i.p. administration.

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-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].