2. Signaling Pathways
  3. PROTAC
  4. DUBTACs

DUBTACs

Deubiquitinase-targeting chimeras

Deubiquitinase-targeting chimeras (DUBTACs), a class of heterobifunctional protein stabilizers consisting of deubiquitinase (DUB) and protein-of-interest (POI) targeting ligands conjugated with a linker, can rescue such proteins from aberrant elimination. DUBTACs stabilize the levels of POIs in a DUB-dependent manner, removing ubiquitin from polyubiquitylated and degraded proteins. DUBTACs can induce a new interaction between POI and DUB by forming a POI-DUBTAC-DUB ternary complex. The chemically induced proximity of a DUB with a POI by the DUBTAC promotes the removal of polyubiquitin chains attached to the POI to block proteasome-mediated degradation, thereby stabilizing and elevating the level of the POI with protective functions. Rescuing the POIs by DUBTACs from aberrant degradation provides therapeutic potential for the treatment of various diseases.

DUBTACs Related Products (2):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-182350
    FXR DUBTAC modulator-1 3081876-96-9
    FXR DUBTAC modulator-1 is a deubiquitinase-targeting chimeric molecule (DUBTAC) that targets FXR, with a Ka value of 2.12e-5 M for FXR. FXR DUBTAC modulator-1 recruits the deubiquitinase OTUB1, binds to OTUB1 and forms a ternary complex with FXR, reduces the polyubiquitination level of FXR, prevents FXR degradation via the ubiquitin-proteasome pathway, and elevates the protein level of FXR. FXR DUBTAC modulator-1 can be used in the research of cholestatic liver injury.
    FXR DUBTAC modulator-1
  • HY-183725
    MS5128 3060520-82-0
    MS5128 is an OTUB1-based deubiquitinase-targeting chimera (DUBTAC) targeting CFTR. MS5128 recruits OTUB1 to CFTR to induce deubiquitination and stabilization of CFTR. MS5128 can be used for the research of cystic fibrosis. (Blue: CFTR Ligand (HY-183724); Pink: OTUB1 Ligand (HY-13262); Black: Linker)
    MS5128