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PROTAC Proteolysis Targeting Chimeric Molecules

Inhibitors

Cat.No.  Name Information
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.
M21359 DSPE-PEG-Biotin (MW 2000) DSPE-PEG-Biotin (MW 2000) is a PROTAC linker, which belongs to the PEG class. It can be used to synthesize PROTAC molecules.
M21318 Biotin-PEG4-amino-t-Bu-DADPS-C6-azide Biotin-PEG4-amino-t-Bu-DADPS-C6-azide is a PROTAC linker, which belongs to the PEG class. It can be used for the synthesis of PROTAC molecules.*The compound is unstable in solutions, freshly prepared is recommended
M21231 PROTAC CDK9 Degrader-1 PROTAC CDK9 Degrader-1 is a PROTAC linked by Cereblon ligand and CDK ligand and is a selective CDK9 degrader.
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.
M21032 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.
M14876 THAL-SNS-032 THAL-SNS-032 is a selective CDK9 degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN).
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.
M14872 MD-224 MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept.
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.
M14870 dTRIM24 dTRIM24 is a selective bifunctional degrader of TRIM24 based on PROTAC, consists of ligands for von Hippel-Lindau and TRIM24.
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).



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