CRBN 选择性抑制剂 | 化学产品 | 调节剂
| 目录号 | 产品名 | 产品描述 | Selective / Pan | IC50 / Ki |
|---|---|---|---|---|
| S1015 | Thalidomide-OH | Thalidomide-OH (Cereblon ligand 2, E3 ligase Ligand 2) is a presumed hydroxylated thalidomide metabolite, with weak antiangiogenic activity (the average inhibition rate of vessel density was 14% in 100 μg), also can be applicable to the recruitment of CRBN protein. | Selective | |
| S8975 | Mezigdomide (CC-92480) | Mezigdomide (CC-92480) is a novel protein degrader and a cereblon E3 ligase modulator (CELMoD) that has anti-myeloma activity. | Selective | |
| S6794 | Thalidomide-O-COOH (Cereblon ligand 3) | Thalidomide-O-COOH (Cereblon ligand 3, E3 ligase Ligand 3), a Thalidomide-based Cereblon (CRBN) ligand, is used in the recruitment of CRBN protein. Thalidomide-O-COOH (Cereblon ligand 3) can be connected to the ligand for protein by a linker to form PROTACs (Proteolysis Targeting Chimera). | Selective | |
| S2881 | Homo-PROTAC cereblon degrader 1 | Homo-PROTAC cereblon degrader 1 (OUN20985) is a potent and efficient cereblon (CRBN) degrader with minimal effects on IKZF1 and IKZF3. | Selective | |
| S9832 | CC-90009 | CC-90009 is a novel cereblon (CRBN) E3 ligase modulator and specifically targets GSPT1 (G1 to S phase transition 1) for proteasomal degradation. | Selective | |
| S8300 | CC-885 | CC-885 is a novel cereblon (CRBN) modulator. CC-885 selectively promotes CRBN- and p97-dependent PLK1 ubiquitination and degradation. |
Selective | |
| S9889 | dCBP-1 | dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP by hijacking the E3 ubiquitin ligase CRBN, also is exceptionally potent at killing multiple myeloma cells and can abolish the enhancer that drives MYC oncogene expression. | Selective | |
| S8760 | Iberdomide (CC220) | Iberdomide (CC-220) is a novel oral immunomodulatory compound that targets cereblon, part of the CRL4CRBN E3 ubiquitin ligase complex, with an IC50 of 60 nM in a competitive TR-FRET assay. Iberdomide (CC-220) induces apoptosis with antitumor and immunostimulatory activities. | Selective | cereblon, IC50: 60 nM |
| S1567 | Pomalidomide | Pomalidomide inhibits LPS-induced TNF-α release with IC50 of 13 nM in PBMCs. Pomalidomide can be utilized in PROTAC as a ligand for targeting E3 ligase and inhibiting the E3 ligase protein cereblon (CRBN). Pomalidomide promotes apoptosis and cell cycle arrest. | Selective | |
| S7892 | Avadomide (CC-122) | Avadomide (CC-122), a new chemical entity termed pleiotropic pathway modifier, is a novel agent for Diffuse large B-cell lymphoma(DLBCL) with antitumor and immunomodulatory activity. Its molecular target is the protein cereblon (CRBN), a substrate receptor of the cullin ring E3 ubiquitin ligase complex CRL4CRBN. | Selective | |
| S1193 | Thalidomide | Thalidomide was introduced as a sedative drug, immunomodulatory agent and also is investigated for treating symptoms of many cancers. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1. | Selective | |
| S8979 | THAL-SNS-032 | THAL-SNS-032 is a selective Cyclin-dependent kinase 9 (CDK9) degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN). | Selective | |
| S1029 | Lenalidomide | Lenalidomide is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide promotes cleaved caspase-3 expression and inhibit VEGF expression and induces apoptosis. | Selective | |
| S8888 | GMB-475 | GMB-475 is a proteolysis-targeting chimera (PROTAC) that allosterically targets BCR-ABL1 protein and recruit the E3 ligase Von Hippel-Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein. | Selective |
