Cat.No. | Name | Information |
---|---|---|
M21192 | ARD-2585 | ARD-2585 is a potent, orally active PROTAC reducer of the androgen receptor. |
M21160 | ARD-61 | ARD-61 is a potent and specific PROTAC androgen receptor (AR) depressant. ARD-61 effectively and efficiently induces AR and progesterone receptor (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and also effectively inhibits tumor growth in a mouse MDA-MB-453 xenograft model. |
M21159 | SD-36 | SD-36 is a potent STAT3 PROTAC degradation agent (Kd=~50 nM) with a high selectivity compared to other STAT members. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of Cereblon ligand Lenalidomide for E3 ubiquitin ligase. |
M21153 | MG-277 | MG-277 is a molecular gel degrader that efficiently induces degradation of the translation termination factor GSPT1 based on Cereblon E3 ligands with a DC50 of 1.3 nM. MG-277 inhibits tumor cell growth in a non-p53 manner with an IC50 of 3.5 nM and 3.4 nM for RS4;11 cells and p53 mutant RS4;11/IRMI-2 cells, respectively. MG-277 exhibited potent anticancer activity. |
M21137 | Folate-MS432 | The FOLR1-targeted folate receptor-dependent PROTAC conjugate, folate-MS432, is a MEK1/2 degrader that targets FOLR1, a receptor highly expressed in many cancer cell types, but less expressed in most cases. |
M14875 | PROTAC FAK degrader 1 | PROTAC FAK degrader 1 is a selective and potent von Hippel-Lindau-based focal adhesion kinase (FAK) degrader with an IC50 of 6.5 nM, DC50 of 3 nM. |
M14874 | PROTAC BET degrader-2 | PROTAC BET degrader-2 is a PROTAC connected by ligands for Cereblon and BET with an IC50 value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression. |
M14873 | PROTAC BET Degrader-1 | PROTAC BET Degrader-1 is a PROTAC connected by ligands for Cereblon and BET, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration. |
M14871 | Gefitinib-based PROTAC 3 | Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a von Hippel-Lindau ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively. |
M14869 | CP-10 | CP-10 is a PROTAC connected by ligands for Cereblon and CDK, with highly selective, specific, and remarkable CDK6 degradation (DC50=2.1 nM). |
M14862 | (S,R,S)-AHPC-PEG4-NH2 hydrochloride | (S,R,S)-AHPC-PEG4-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology. |
M14861 | Thalidomide-O-amido-C8-NH2 TFA | Thalidomide-O-amido-C8-NH2 TFA (Cereblon Ligand -Linker Conjugates 2 TFA) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology. |
M13398 | BSJ-03-204 | BSJ-03-204 is a Cereblon ligand linked to THE CDK ligand PROTAC, which is an effective, selective cdK4/6 dual inhibitor based on Palbociclib. The IC50 of CDK4/D1 and CDK6/D1 were 26.9 nM and 10.4 nM, respectively. |
M10793 | BETd-260 | BETd-260 (ZBC 260) is a PROTAC connected by the Cereblon ligand and bet ligands in leukemia cells RS4; 11 At low concentrations of 30 pM, BRD4 protein activity is reduced. BETd-260 significantly inhibits the activity of HCC cells in hepatocellular carcinoma and induces apoptosis. |
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