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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.
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.
M57181 CMP98  CMP98, a PROTAC, is unable to induce degradation of VHL.
M57180 MS8815  MS8815 is a selective enhancer of zeste homolog 2 (EZH2) PROTAC degrader.
M57179 TD-802  TD-802 is an androgen receptor (AR) PROTAC degrader with good microsomal stability.
M57178 ARD-266  ARD-266 is a highly potent and von Hippel-Lindau E3 ligase-based Androgen Receptor (AR) PROTAC degrader.
M57177 GNE-987  GNE-987 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4.
M57175 PhosTAC7  PhosTAC7 is a heterobifunctional molecule named as a Phosphorylation Targeting Chimera (PhosTAC). PhosTAC7 can dephosphorylate the PDCD4 protein, FOXO3a protein, and Tau protein by recruiting serine/threonine protein phosphatase 2A (PP2A). Similar to PROTACs in their ability to induce ternary complexes, PhosTAC7 focuses on recruiting a Ser/Thr phosphatase to a phosphosubstrate to mediate its dephosphorylation.
M57174 SJ995973  SJ995973 (PROTAC) is a uniquely potent degrader of bromodomain and extra-terminal (BET) proteins.
M57173 ARD-2585  ARD-2585 is an exceptionally potent and orally active PROTAC degrader of androgen receptor.
M57172 XF067-68  XF067-68 is a PROTAC for targeted degradation of WD40 repeat domain protein 5 (WDR5).
M57171 SJF-8240  SJF-8240 (PROTAC 7) is a proteolysis targeting chimera (PROTAC) degrader.
M57170 dBRD4-BD1  dBRD4-BD1 is a selective and durable BRD4 degrader with an DC50 value of 280 nM (Dmax=77%).
M57169 SB1-G-187  SB1-G-187, a PROTAC, is a multi-kinase degrader.
M57168 QC-01–175  QC-01-175 is a heterobifunctional molecule, which degrades aberrant tau.
M57167 XY028-133  XY028-133 is a PROTAC-based CDK4/6 degrader with anti-tumor activity, which consists of ligands for von Hippel-Lindau and CDK.
M57166 PROTAC-O4I2  PROTAC-O4I2 is a PROTAC targets splicing factor 3B1 (SF3B1).
M57165 FKBP12 PROTAC RC32 FKBP12 PROTAC RC32 (RC32) is a potent FKBP12 degrader based on PROTAC technology.
M57164 PROTAC ERRα Degrader-3  PROTAC ERRα Degrader-3 is a potent and selective ERRα degrader based on von Hippel-Lindau ligand.
M57163 PROTAC FKBP Degrader-3  PROTAC FKBP Degrader-3 is a PROTAC that comprises a FKBP ligand binding group, a linker and an von Hippel-Lindau binding group.
M54696 DGY-09-192 DGY-09-192 is a bivalent degrader that couples the pan-FGFR inhibitor BGJ398 to the CRL2VHL E3 ligase-recruiting ligand, which induces degradation of FGFR1/2 and largely avoids degradation of FGFR3/4.DGY-09-192 exhibits a nanomolar DC50 against both wild-type FGFR2 and several FGFR2 fusions. In addition, DGY-09-192 has antiproliferative activity in gastric and cholangiocarcinoma cells.
M54671 BTX-6654 BTX-6654 is a targeted and specific cerebellar-based bifunctional SOS1 PROTAC degrader.BTX-6654 reduces the downstream signaling markers pERK and pS6 and displays antiproliferative activity in a wide range of KRAS-mutant cells. In two KRAS G12C xenograft models, BTX-6654 degraded SOS1 in a dose-dependent manner correlating with tumor growth inhibition, additionally exhibiting synergy with KRAS and MEK inhibitors.




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