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PROTAC Proteolysis Targeting Chimeric Molecules

Cat.No.  Name Information
M40697 NX-5948 NX-5948 (BTK-IN-24) is an orally active, blood-brain barrier-penetrating, BTK-targeting degradation agent for the study of B-cell malignancies and autoimmune diseases. NX-5948 induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. NX-5948 mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation.
M10423 DT2216 DT2216 is a BCL-XL protein hydrolysis targeting chimera (PROTAC) that ligates and degrades BCL-XL with E3 ubiquitin (E3) ligase. DT2216 is effective against a variety of BCL-XL-dependent leukemias and cancer cells.
M25609 CFT1946 CFT1946 is an orally active, selective, CRBN-based protein degrader targeting BRAFV600X and BTK for tumor-related studies.
M25608 FHD-609 FHD-609 is an inhibitor and a degrader of BRD9 (bromodomain-containing protein 9). FHD-609 targets to ncBAF, can be used for research of wide range of cancers that contain a mutation in a BAF complex subunit.
M21519 U7D-1 U7D-1 is a first-in-class, potent and selective ubiquitin-specific protease 7 USP7 PROTAC depressant in RS4; The DC50 in 11 cells was 33 nM. U7D-1 has anti-cancer activity.
M21512 SR-1114 SR-1114 is a first-in-class PROTAC ENL depressant. SR-1114 in MV4; ENL degradation was observed in 11, MOLM-13 and OCI/AML-2 cells with DC50 values of 150 nM, 311 nM and 1.65 μM, respectively.
M21435 MS170 MS170 is a potent selective PROTAC AKT depressant. MS170 consumes total AKT (T-AKT) and has a DC50 value of 32 nM. MS170 binds to AKT1, AKT2 and AKT3 with Kd of 1.3 nM, 77 nM and 6.5 nM, respectively.
M21434 INY-03-041 INY-03-041 is an effective and highly selective Protac-based pan-Akt degradation consisting of GDC-0068, an ATP-competitive AKT inhibitor conjugated to lenalidomide (Cereblon ligand). INY-03-041 inhibited AKT1, AKT2 and AKT3 with IC50 values of 2.0 nM, 6.8 nM and 3.5 nM, respectively.
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.
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.
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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