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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.
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.
M21158 Vepdegestrant (ARV-471) Vepdegestrant (ARV-471) is an oral estrogen receptor PROTAC protein degrader for breast cancer.ARV-471 is a heterobifunctional molecule that promotes the interaction between estrogen receptor alpha and intracellular E3 ligase complexes.ARV-471 causes ubiquitination and subsequent degradation of the estrogen receptor via the proteasome.ARV-471 potently degrades ER-positive The ER in breast cancer cell lines is potently degraded by ARV-471 with a DC50 value of approximately 2 nM.
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).
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.
M14870 dTRIM24 dTRIM24 is a selective bifunctional degrader of TRIM24 based on PROTAC, consists of ligands for von Hippel-Lindau and TRIM24.
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.
M13389 ACBI1 ACBI1 is an effective and synergistic PROTAC inhibitor of SMARCA2, SMARCA4 and PBRM1, with DC50 of 6 nM, 11 nM and 32 nM in MV-4-11 cells, respectively. ACBI1 can induce antiproliferative effect and apoptosis.
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.
M10386 MT-802 MT-802 is a potent BTK degrader based on PROTAC technology, it induces Bruton's tyrosine kinase (BTK) knockdown.
M10385 LC-2 LC-2 is a potent first-in-class PROTAC capable of degrading endogenous KRAS G12C, with DC50s between 0.25 and 0.76 μM.
M10384 Homo-PROTAC pVHL30 degrader 1 Homo-PROTAC pVHL30 degrader 1 is a pVHL30 degrader based on PROTAC and a potent VHL inhibitor.
M10383 Homo-PROTAC cereblon degrader 1 (OUN20985) Homo-PROTAC cereblon degrader 1 (OUN20985) is a potent and efficient cereblon (CRBN) degrader with minimal effects on IKZF1 and IKZF3.
M10382 PROTAC SGK3 degrader-1 PROTAC SGK3 degrader-1 (SGK3-PROTAC1) is a potent SGK3 degrader, it is a PROTAC conjugate of the 308-R SGK inhibitor with the VH032 VHL binding ligand, targeting SGK3.
M10381 TD-165 TD-165 is a PROTAC-based cereblon (CRBN) degrader.
M10380 dBET57 dBET57 is a novel BRD4 heterobifunctional small-molecule ligand (PROTAC) which exhibits significant and selective degradation of BRD4 BD1 but is inactive on BRD4 BD2.
M10379 BSJ-03-123 BSJ-03-123 is a novel, potent CDK6-selective small-molecule degrader (PROTAC).
M10067 Ac4GalNAz Ac4GalNAz is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.
M9838 VH032-PEG6-C4-Cl (S,R,S)-AHPC-PEG6-C4-Cl is a small molecule HaloPROTAC that incorporates the (S,R,S)-AHPC based VHL ligand and 6-unit PEG linker.
M9824 MZ 1 MZ 1 is a PROTAC BRD4 degrader, with Kd values of 382/120, 119/115, and 307/228 nM for BRD4 BD1/2, BRD3 BD1/2, and BRD2 BD1/2, respectively.




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