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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.
PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera (PROTAC), is a potently and selectively Mcl-1 inhibitor with an IC50 of 0.78 μM.
Synonyms: MS140
XY028-140 (MS140) is a highly potent and selective dual-function compound that acts as both a CDK4/6 kinase inhibitor and a PROTAC degrader. By combining kinase inhibition with targeted protein degradation, MS140 provides an effective approach for disrupting CDK4/6-mediated cell cycle regulation, making it a valuable tool for cancer research.
VEGFR-2-IN-39 is a potent inhibitor of the vascular endothelial growth factor receptor 2 (VEGFR-2), with an IC50 of 208.6 nM. This compound effectively inhibits the proliferation of EA.hy926 cells, a human umbilical vein endothelial cell line, in a concentration-dependent manner, exhibiting an IC50 of 38.65 µM. VEGFR-2-IN-39 has low toxicity, making it suitable for further research applications in angiogenesis and vascular biology.
HDAC6 Degrader-3 is a selective inhibitor that promotes the degradation of histone deacetylase 6 (HDAC6) through ternary complex formation and the ubiquitin-proteasome pathway, exhibiting a DC50 value of 19.4 nM. With IC50 values of 4.54 nM for HDAC6 and 0.647 μM for HDAC1, it effectively induces significant hyperacetylation of α-tubulin. This compound is valuable for research applications focused on neurodegenerative diseases and cancer, where modulation of HDAC6 activity may play a critical role.
UNC8732 (TFA) is a potent inhibitor of NSD2, functioning as a protein degrader. This compound promotes cellular degradation of NSD2, which plays a critical role in various cellular processes, including gene expression and chromatin regulation. UNC8732 (TFA) is utilized in research related to cancer biology and epigenetic regulation, providing insights into NSD2's role in disease mechanisms and potential therapeutic strategies.
SHP2 protein degrader-1 is a potent allosteric inhibitor targeting the SHP2 protein, which plays a significant role in various signaling pathways. This compound induces degradation of SHP2, leading to programmed cell death (apoptosis) in affected cells. SHP2 protein degrader-1 is valuable for research into SHP2-related diseases, including cancers and other pathologies where SHP2 dysregulation contributes to disease progression.
SMARCA2-IN-8 is a selective inhibitor of the SWI/SNF chromatin remodeling complexes SMARCA2 and SMARCA4, exhibiting potent activity with IC50 values of 5 nM and 6 nM, respectively. This compound effectively inhibits the proliferation of SMARCA2-mutated cancer cells, specifically SKMEL5, with an AAC50 of 5 nM and downregulates SMARCA2-dependent KRT80 gene expression at an AAC50 of 10 nM. SMARCA2-IN-8 demonstrates substantial antitumor efficacy and favorable pharmacokinetic properties in preclinical mouse models, making it a valuable tool for investigating chromatin remodeling in cancer research.
SMARCA2-IN-2 is a specific inhibitor of SMARCA2, demonstrating an IC50 range of 101-500 µM. This compound is relevant for investigations into cancer biology, as it provides insights into the role of SMARCA2 in tumorigenesis. Its ability to selectively modulate SMARCA2 activity makes it a valuable tool for understanding epigenetic regulation in cancer research.
XIAP degrader-1 is a small molecule designed to induce the degradation of the X-linked inhibitor of apoptosis protein (XIAP), functioning primarily as an IAP inhibitor. This compound facilitates the selective elimination of XIAP, a protein known to inhibit apoptosis, thereby promoting cell death in cancerous cells. XIAP degrader-1 is valuable for research applications aimed at understanding apoptosis regulation and evaluating potential therapeutic strategies in oncology.
SR-5037 is an orally active inhibitor of CDK12 and CDK13, with an IC50 of 31 nM, and functions as a molecular glue degrader for CycK, demonstrating a DC50 of 30 nM and Dmax exceeding 98%. By inhibiting the enzymatic activity of the CDK12/CycK and CDK13/CycK complexes, SR-5037 facilitates the recruitment of DDB1, leading to proteasome-mediated degradation of CycK. This compound has shown efficacy in degrading active CycK in mouse models of triple-negative breast cancer and is a valuable tool for investigating treatment options in such malignancies.
PIN1 Degrader-2 is a potent and selective covalent inhibitor targeting the prolyl isomerase PIN1, with an IC50 of 4.1 nM. This compound effectively induces degradation of PIN1 in cancer cell lines, demonstrating a DC50 of less than 500 nM. PIN1 Degrader-2 is valuable for research applications focused on cancer biology and the role of PIN1 in tumor progression.
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PIN1 Degrader-1 is a selective inhibitor of the proline cis-trans isomerase Pin1, exhibiting an IC50 of 21.5 nM. This compound forms a covalent bond with Cys113, inducing conformational changes that destabilize the protein and promote proteasome-dependent degradation. PIN1 Degrader-1 effectively decreases cell viability in various cancer cell lines, making it a valuable tool for cancer research applications.
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UNC8732 is a selective NSD2 inhibitor that promotes protein degradation. This compound is essential for studying the role of NSD2 in epigenetic regulation and its implications in various diseases, including cancer. UNC8732 facilitates targeted protein degradation, offering valuable insights for research in cellular signaling and therapeutic development.
