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PROTAC degraders recruit an E3 ubiquitin ligase to a target protein so that the proteasome degrades it. Each proteolysis-targeting chimera (PROTAC) links a target-binding ligand to an E3 ligase ligand through a chemical linker. The approach was first described in 2001, and later work showed that small-molecule PROTACs can act catalytically, removing several target copies per molecule. Examples include the bromodomain and extra-terminal (BET) degraders dBET1, MZ1 and ARV-771, and the estrogen receptor degrader ERD-308. Degraders of anti-apoptotic proteins, such as PROTAC Mcl1 degrader-1, are also listed.
ZL-12A probe is a selective degrader targeting the ERCC3 helicase within the TFIIH complex. By covalently modifying cysteine residue C342, ZL-12A facilitates the targeted degradation of ERCC3. This compound is valuable for researchers studying DNA repair mechanisms and the functional role of TFIIH in nucleotide excision repair.
SH6 is a targeted degrader of the transcription factor ZBTB7A. This compound demonstrates significant potential in the study of β-hemoglobinopathies, including sickle cell disease (SCD) and β-thalassemia. By modulating ZBTB7A levels, SH6 may provide insights into the underlying mechanisms of these disorders and facilitate the development of novel therapeutic approaches.
MRC71 is a TRIMTAC degrader designed to target the Halo Tag, utilizing a PEG linker and chloroalkane moiety for enhanced specificity. This compound selectively induces the degradation of oligomeric CAV1- and Cavin1-mEGFP-Halo constructs while sparing monomeric mEGFP-Halo. MRC71 displays a characteristic hook effect, demonstrating concentration-dependent degradation profiles, making it a valuable tool for studying protein regulation and turnover in cellular models.
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FcⅢ-GN3 is a dual-functional peptide targeting IgG degradation through enhanced internalization mechanisms in HepG2 cells. Upon internalization, IgG localizes within late endosomes and lysosomes, promoting clearance via the liver's natural pathway. This agent is particularly valuable for investigating diseases associated with elevated IgG levels, facilitating the exploration of therapeutic interventions in related pathologies.
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TKP-5 is a potent PROTAC protein degrader that targets the epigenetic reader proteins BRD2, BRD3, and BRD4, exhibiting binding affinities (Ka) of 150 nM and 100 nM, respectively. This compound inhibits the production of thymic stromal lymphopoietin and downregulates IL-33 mRNA expression. Its utility extends to investigations pertaining to tape-stripping induced skin injury, making it valuable for diverse research applications in immunology and dermatology.
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MS115 TFA is a selective degrader targeting the PRMT5/MEP50 complex, demonstrating DC50 values of 17.4 nM and 11.3 nM for PRMT5 and MEP50, respectively, after 24 hours in MDA-MB-468 cells. This compound effectively inhibits the proliferation of breast cancer cells, making it a valuable tool for research into targeted protein degradation and potential therapeutic strategies in oncology.
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WCF-598 is an RXRγ-targeting PROTAC degrader with a binding affinity (Kd) of 234.2 nM. It facilitates the degradation of RXRγ through the ubiquitin-proteasome pathway, leading to the destabilization of the RXRγ-AR-V7 complex and subsequent downregulation of AR-V7 levels. This compound has been observed to induce tumor cell apoptosis, inhibit cell proliferation, activate the p53 signaling pathway, and suppress cell cycle progression, making it a valuable tool for research in prostate cancer.
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PROTAC CDK2-pRb degrader-1 is an orally active PROTAC that targets cyclin-dependent kinase 2 (CDK2) for degradation. This compound effectively inhibits the phosphorylation of retinoblastoma protein (Rb) at serine 807/811 by promoting the ubiquitination and proteasomal degradation of CDK2. Demonstrating significant biological activity with EC50 values of 12 nM and 125 nM in human cells, PROTAC CDK2-pRb degrader-1 is particularly useful in research focused on CCNE1-amplified cancers, including ovarian, gastric, and breast cancers, as it inhibits tumor growth and induces tumor stasis in xenograft models.
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PDL1 degrader-3 is a CSN5 degrader that targets human CSN5 with an affinity of 4.53 μM. This compound inhibits the enzymatic activity of CSN5, promoting PD-L1 ubiquitination and subsequent degradation through the ubiquitin-proteasome pathway, thus decreasing PD-L1 expression on tumor cell membranes. PDL1 degrader-3 effectively disrupts the PD-1/PD-L1 interaction, thereby enhancing the tumor immune microenvironment, increasing tumor-infiltrating T-cell immunity, and inhibiting the activation of immunosuppressive myeloid-derived suppressor cells (MDSCs) and regulatory T cells (Tregs). Its antitumor efficacy has been demonstrated in various mouse tumor models, making it a valuable tool for research in colorectal and lung cancer.
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PSP-0119 is a highly selective PROTAC degrader targeting IRAK4, demonstrating an IC50 of 2.83 nM. This compound effectively inhibits IRAK4 kinase activity, NF-κB signaling, and IL-1β-induced IRAK4 phosphorylation. Notably, PSP-0119 induces degradation of IRAK4 specifically in FLT3-mutant acute myeloid leukemia (AML) cell lines while sparing FLT3-wild-type AML cells and normal bone marrow. It serves as a valuable tool for research into the mechanisms underlying AML, particularly in targeting aberrant IRAK4 activity.
PROTAC SMARCA2/4 degrader-40 is a specific degrader targeting SMARCA2 and SMARCA4. It demonstrates potent degradation activity in HeLa cells, with a DC50 value of less than 0.1 nM. This compound is particularly useful for investigating cancers linked to SMARCA2/SMARCA4 abnormalities or mutations within the SWI/SNF complex, facilitating insights into their role in tumorigenesis.
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