proto-oncogene

Arglabin ((+)-Arglabin) is a natural product isolated from Artemisia glabella, is a NLRP3 inflammasome inhibitor, has anti-atherogenic and anticancer effects.

Amivantamab (Anti-c-Met) is a human antibody that recognizes the MET proto-oncogene (MET) and can be used in cancer-related research.

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

Capmatinib 2HCl.H2O (NVP-INC280 2HCl.H2O) is an orally bioavailable inhibitor of the proto-oncogene c-Met (HGFR)with potential antineoplastic activity.

C-MYC PEPTIDE EPITOPE TFA, the product of the c-myc proto-oncogene, is a helix-loop-helix leucine zipper phosphoprotein that regulates gene transcription in cell proliferation, cell differentiation and apoptosis. This peptide is a human c-myc epitope.

ASP3026 has been used in trials studying the treatment of Solid Tumor, B-Cell Lymphoma, Advanced Malignancies, Positive for Anaplastic Lymphoma Kinase, and Positive for Proto-Oncogene Tyrosine-Protein Kinase ROS.

Capmatinib (INCB28060) is an orally active, highly selective, ATP-competitive c-Met tyrosine kinase inhibitor with an IC50 value of 0.13 nM. Capmatinib effectively inhibits the proliferation and migration of c-Met-dependent tumor cells, induces apoptosis, and exhibits antitumor activity.

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-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.

Merestinib (LY2801653) is an orally available, small molecule inhibitor of the proto-oncogene c-Met (Ki: 2 nM) with potential antineoplastic activity. Merestinib electively binds to c-Met, thereby inhibiting c-Met phosphorylation and disrupting c-Met signal transduction pathways. This may induce cell death in tumor cells overexpressing c-Met protein or expressing the constitutively activated c-Met protein.

c-Myc inhibitor 4 is a potent, orally active compound that reduces c-Myc, an important proto-oncogene closely associated with the development of many tumors.

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.

Foretinib phosphate is an orally bioavailable small molecule with potential antineoplastic activity. MET/VEGFR2 inhibitor GSK1363089 binds to and selectively inhibits hepatocyte growth factor (HGF) receptor c-MET and vascular endothelial growth factor receptor 2 (VEGFR2), which may result in the inhibition of tumor angiogenesis, tumor cell proliferation and metastasis. The proto-oncogene c-MET has been found to be over-expressed in a variety of cancers.

Pyridostatin (RR82) hydrochloride, a G-quadruplex DNA stabilizing agent (Kd = 490 nM), induces replication- and transcription-dependent DNA damage, promoting growth arrest in human cancer cells. It specifically targets the proto-oncogene Src, leading to reduced SRC protein levels and decreased SRC-dependent cellular motility in human breast cancer cells.

RGB-1, a small molecule that selectively stabilizes the RNA G-quadruplex structure, enhances G-quadruplex-mediated inhibition of RNA translation in mammalian cells and reduces NRAS proto-oncogene expression in breast cancer cells.

Sutetinib is an orally effective tyrosine kinase inhibitor that targets enzymes linked to tumor growth and angiogenesis, such as VEGFR (VEGFR-1/2/3 with Ki= 0.009 µM), PDGFR (PDGFR-α/β with Ki= 0.008 µM), and the proto-oncogene cKIT. It inhibits the proliferation, migration, and tubular structure formation of endothelial and fibroblast cells, demonstrating antitumor activity across various cancer cell lines.

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.

Amivantamab (JNJ-61186372) is a humanized antibody that recognizes epidermal growth factor receptor (EGFR) and MET proto-oncogene (MET), with anticancer and anti-tumor activities, preventing ligand binding to EGFR and MET and receptor dimerization that inhibits downstream signal transduction. Amivantamab can induce Fc-dependent endocytosis of macrophages and antibody-dependent cytotoxicity of natural killer cells, and can be used to study metastatic non-small cell lung cancer.