ubiquitin proteasome

E3 ligase Ligand 23 is a cereblon binding agent that degrades Ikaros or Aiolos via the ubiquitin proteasome.

PROTAC BRAF-V600E degrader-1 (Compound 23) selectively induces degradation of BRAF-V600E but not wildtype BRAF.

Torbafylline, a xanthine derivative, is a phosphodiesterase (PDE) inhibitor that attenuates burn-induced protein hydrolysis in rat skeletal muscle through activation of the PDE4/cAMP/EPAC/PI3K/Akt pathway, and inhibits the enhanced ubiquitin-proteasome-dependent protein hydrolysis in skeletal muscle of cancer- and sepsis-prone rats.

USP28-IN-3 is a highly selective USP28 inhibitor with an IC50 value of 0.1 μM against USP28.USP28-IN-3 exhibits anticancer activity and inhibits USP2, USP7, USP8, USP9x, UCHL3, and UCHL5.USP28-IN-3 is cytotoxic to human colorectal and lung squamous carcinoma cells, inhibiting c-cells and c-neutralizing c-neutralizing c-neutralizing c-neutralizing c-neutralizing c-neutralizing c-neutralizing c-cells through the ubiquitin-proteasome system. -proteasome system to dose-dependently downregulate cellular levels of c-Myc.

Amino-PEG9-alcohol is a PEG-based linker for PROTACs [Proteolysis Targeting Chimeras], facilitating the conjugation of two essential ligands for PROTAC formation and enabling selective protein degradation via the ubiquitin-proteasome system within cells.

Fmoc-PEG12-NHS ester, a PEG-based linker for PROTACs, facilitates the joining of two essential ligands, crucial for the formation of PROTAC molecules, and enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.

BI-4464 is a highly selective inhibitor targeting focal adhesion kinase (FAK). BI-4464 effectively blocks the catalytic activity of FAK by competitively binding to the ATP-binding site, with an IC₅₀ of 17 nM. In addition to its role as a kinase inhibitor, BI-4464 can also serve as a FAK-targeting ligand (warhead) for PROTAC design. By conjugation with an E3 ligase ligand via an appropriate linker, the resulting PROTAC molecule can induce the selective degradation of FAK through the ubiquitin–proteasome pathway, providing a valuable tool for cancer biology and related disease research.

ARV-393 is a PROTAC degrader targeting BCL6 with the advantage of being highly potent and orally available.ARV-393 recruits BCL6 and E3 ligase cerebellum to rapidly degrade BCL6 through the cell's natural ubiquitin proteasome system for the treatment of diffuse large b-cell lymphoma (DLBCL) and non-Hodgkin's lymphoma (NHL).

RAMB4 (PTP1B-IN-9) is a ubiquitin-proteasome system (UPS)-stressor,with anticancer activity.

UT-34 is a selective and orally active antagonist of second-generation pan-androgen receptor (AR) and degrader(IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively), and has anti-prostate cancer efficacy.

Arimoclomol (BRX-220 free base), a co-inducer of heat shock proteins (HSP), is utilized in studies on the treatment of amyotrophic lateral sclerosis (ALS).

Arimoclomol maleate (BRX-220) (BRX-220) is a heat shock protein (HSP) co-inducer.

RA190 inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.

SNIPER(TACC3)-1 targets TACC3 protein degradation via the ubiquitin-proteasome pathway.It induces cancer cell death.

SNIPER(TACC3)-2 targets TACC3 protein degradation via the ubiquitin-proteasome pathway. It induces cancer cell death.

2-(Benzyloxy)ethanol is a PEG-based linker for PROTACs, facilitating the connection of two essential ligands necessary for forming PROTAC molecules, thereby enabling selective protein degradation via the ubiquitin-proteasome system within cells.

3,4-Dibromo-Mal-PEG2-N-Boc is a PEGylated PROTAC linker that enables conjugation between target-binding ligands and E3 ligase ligands during PROTAC assembly. 3,4-Dibromo-Mal-PEG2-N-Boc supports the design of heterobifunctional degraders that exploit the ubiquitin–proteasome system for selective protein degradation。

Acid-C2-PEG3-NHS ester is a PEG-based linker for PROTACs, joining two essential ligands crucial for PROTAC formation, enabling selective protein degradation via the ubiquitin-proteasome system within cells.

Acid-PEG1-C2-Boc is a PEG-based linker for PROTACs that joins two essential ligands, facilitating the formation of PROTAC molecules and enabling selective protein degradation through the ubiquitin-proteasome system within cells.

Acid-PEG2-C2-Boc is a PEG-based linker for PROTACs, joining two essential ligands crucial for forming PROTAC molecules, enabling selective protein degradation through the ubiquitin-proteasome system within cells.

Acid-PEG3-PFP ester is a PEG-based linker for PROTACs that joins two essential ligands, facilitating the formation of PROTAC molecules and enabling selective protein degradation by leveraging the ubiquitin-proteasome system within cells.

Acid-PEG5-C2-Boc, a PEG-based linker for PROTACs, facilitates the connection of two essential ligands necessary for PROTAC molecule formation, enabling selective protein degradation via the ubiquitin-proteasome system within cells.

Acid-PEG5-TEMPO is a PEG-based linker for PROTACs, joining two essential ligands crucial for PROTAC molecule formation, and facilitates selective protein degradation using the ubiquitin-proteasome system within cells.

Acid-PEG6-C2-Boc is a PEG-based linker for PROTACs that joins two essential ligands, facilitating the formation of PROTAC molecules and enabling selective protein degradation via the ubiquitin-proteasome system within cells.