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Inhibitors
| Cat.No. | Name | Information |
|---|---|---|
| M21353 | Golcadomide | Golcadomide (CC-99282) is a potent and orally active CRBN E3 ligase modulator (CELMoD).CC-99282 co-induces effective and targeted degradation of Ikaros and Aiolos with CRBN.CC-99282 can be used in studies of non-Hodgkin's lymphoma. |
| M21151 | ZXH-1-161 | ZXH-1-161 is a potent cereblon (CRBN) regulator with an IC50 of 39 μM in wild-type MM1.S cells. ZXH-1-161 has selective degradation activity against GSPT1. ZXH-1-161 can be used in the study of multiple myeloma. |
| M21003 | 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. |
| M14867 | VH032 | VH032 is a VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. VH032 is a VHL/HIF-1α interaction inhibitor with a Kd[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. |
| M14865 | VH032-cyclopropane-F | VH032-cyclopropane-F is the VH032-based VHL ligand. VH032-cyclopropane-F can be connected to the ligand for protein (e.g., SMARCA BD ligand) by a linker to form PROTACs (e.g., PROTAC 1). PROTAC 1 is a partial degrader of SMARCA2 and SMARCA4. |
| M14864 | (S,R,S)-AHPC | (S,R,S)-AHPC (VH032-NH2) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. |
| 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. |
| M13434 | CFT7455 | CFT7455 is an orally active inhibitor of zinc finger transcription factors Ikaros (IKZF1) and Aiolos (IKZF3). It is also an anticancer agent that binds cereblon E3 ligase with high affinity (Kd 0.9 nM). |
| 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. |
| M9837 | Thalidomide-O-amido-C4-NH2 (TFA) | Thalidomide-O-amido-C4-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker. |
| M9836 | Pomalidomide-PEG4-C-COOH | Pomalidomide-PEG4-C-COOH (E3 Ligase Ligand-Linker Conjugates 1) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 4-unit PEG linker. |
| 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. |
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