Cat.No. | Name | Information |
---|---|---|
M2225 | Thalidomide | Thalidomide is a sedative and immunomodulator used to study the symptoms of many cancers, it has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ∼250 nM. |
M57279 | BC-1215 | BC-1215 is a novel inhibitor of F-box protein 3 (Fbxo3) activity. BC-1215 works by antagonizing of Fbxo3 on TRAF cytokine signaling and exhibits a low IC50 in vitro. BC-1215 relieves allodynia by preventing ubiquitination-dependent Fbxl2/TRAF2/TNIK/pGluR1 signaling. BC-1215 exerted robust therapeutic effects in cytokine-driven inflammation, including pseudomona-induced lung injury and cecum ligation/punctured-induced sepsis, by targeting Fbxo3/Fbxl2/TRAF-mediated cytokine release. BC-1215 can be used for the research of inflammation. |
M55581 | PT-179 | PT-179 is an orthogonal Thalidomide (M2225) derivative that targets cereblon without causing off-target degradation effects. PT-179 is able to specifically bind CRBN, form a ternary complex with a target protein fused to a zinc finger (ZF) degron, and mediate the degradation of the tagged protein. |
M43913 | 2,6-Bis(benzyloxy)-3-bromopyridine | 2,6-Bis(benzyloxy)-3-bromopyridine |
M25473 | HaloPROTAC3 | HaloPROTAC3 is a conjugate of ligands for E3 and 16-atom-length linker, and it is also a highly potent and efficacious degrader of GFP-HaloTag7 fusion proteins with a DC50 of 19 nM. |
M21003 | CC-90009 | CC-90009 is a first-in-class, novel Cereblon (CRBN) E3 ligase modulator that specializes in proteasomal degradation of GSPT1 (G1 to S phase transition 1). |
M14866 | E3 ligase Ligand 8 | E3 ligase Ligand 8 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 8 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins. |
M14863 | CC-885 | CC-885 is a regulator of CRBN protein with a wide range of strong CRBN-dependent anti-proliferative activity in various tumor cell lines, with enhanced anti-proliferative activity compared to lenalidomide and pomalidomide.CC-885 promotes the binding of CRBN to the novel substrate GSPT1, targeting its degradation. |
M11441 | CFT7455 | CFT7455 is an orally active inhibitor of zinc finger transcription factors Ikaros (IKZF1) and Aiolos (IKZF3). CFT7455 is an anticancer agent that binds cereblon E3 ligase with high affinity (Kd 0.9 nM) (WO2022032132A1; Compound 1). |
M10387 | Thalidomide-NH-CH2-COOH | Thalidomide-NH-CH2-COOH is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. |
M9834 | E3 ligase Ligand 4 | E3 ligase Ligand 4 (Thalidomide 4-fluoride) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein, it can connect to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1. |
M9833 | E3 ligase Ligand 3 | E3 ligase Ligand 3 (Thalidomide-O-COOH) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein, it connected to the ligand for protein by a linker to form PROTACs. |
M9832 | E3 ligase Ligand 2 | E3 ligase Ligand 2 (Thalidomide-4-OH) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein, it can be connected to the ligand for protein by a linker to form PROTACs. |
M9826 | E3 ligase Ligand 1 | E3 ligase Ligand 1 (VHL ligand 2 hydrochloride; (S,R,S)-AHPC-Me hydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. |
M9736 | VHL Ligand 1 hydrochloride | VHL Ligand 1 hydrochloride is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. |
M9033 | VH-298 | VH-298 is a potent VHL inhibitor that stabilizes HIF-α and elicits a hypoxic response via a different mechanism, with a Kd value of 80 to 90 nM. |
M1976 | Pomalidomide | Pomalidomide is the third-generation immunomodulatory agent, functions through interacting with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors. Pomalidomide is a second generation immunomodulator, TNF-α inhibitor with IC50 of 13 nM. |
M58123 | OICR-8268 | OICR-8268 is a reversible DCAF1 ligand that binds to the DCAF1 WDR domain with a Kd of 38 nM. OICR-8268 can be used in the development of DCAF1-based PROTACs. |
M57120 | VH 101, acid | VH 101, acid is a functionalized von-Hippel-Lindau (VHL) protein ligand for PROTAC research and development. |
M57119 | (S,R,S)-AHPC-Boc | (S,R,S)-AHPC-Boc (VH032-Boc) is a ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. |
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