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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.
TMX-4153 is a selective degrader targeting PIP4K2C through the PROTAC (Proteolysis-targeting chimera) mechanism. It effectively induces PIP4K2C degradation in MOLT4 cells with a DC50 of 24 nM and in HAP1 cells with a DC50 of 361 nM. This compound is valuable for researching the biological functions of PIP4K2C, particularly in relation to diseases associated with immune modulation.
(Rac)-P1D-34 is a PROTAC-based degrader targeting the PIN1 protein, utilizing cereblon as the E3 ligase for targeted degradation. This compound exhibits anti-cancer activity with reported IC50 values of 2248 nM in MV-4-11 cells and 3984 nM in MOLM-13 cells, demonstrating its potential in hematological malignancies. Its application as a research tool in the study of cancer biology and therapeutic development for cancers associated with PIN1 overexpression is notable.
PIN1 degrader-3 is a potent degrader of the peptidyl-prolyl isomerase protein PIN1, exhibiting an IC50 of 4.65 nM. This compound covalently binds to PIN1, leading to its degradation and a consequent reduction in cell viability, with EC50 values of 8.4 μM in MIA PaCa-2 cells and 5.3 μM in KPC cell lines after 72 hours. PIN1 degrader-3 serves as a valuable tool for investigating the role of PIN1 in pancreatic cancer research and for exploring therapeutic strategies aimed at targeting this oncogenic pathway.
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PROTAC PIN1 degrader-1 is a proteolysis-targeting chimera (PROTAC) designed to selectively degrade the prolyl isomerase PIN1, exhibiting a DC50 value of 1.8 nM. This compound demonstrates significant activity against the MDA-MB-468 cell line, with a GI50 > 30 μM. PROTAC PIN1 degrader-1 is structurally composed of the PIN1 ligand, an E3 ligase ligand derived from Thalidomide, and a PROTAC linker, enabling targeted degradation of PIN1 for potential therapeutic applications in cancer research and beyond.
Lenalidomide-CO-C7-NH2 is a CRBN-dependent intermediate designed as a BRD4-targeting PROTAC degrader. This compound facilitates the selective degradation of the oncoprotein BRD4, leading to decreased cancer cell proliferation, cell cycle arrest, and enhanced apoptosis. It demonstrates noteworthy anti-tumor efficacy in xenograft models, making Lenalidomide-CO-C7-NH2 a valuable tool for investigating mechanisms in acute myeloid leukemia research.
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SJ6986 is a potent and selective molecular glue degrader targeting GSPT1 and GSPT2, exhibiting a DC50 of 2.1 nM with a maximum degradation (Dmax) of 99% for GSPT1. This compound facilitates the targeted degradation of these proteins, making it a valuable tool for research into proteostasis and cellular stress responses. SJ6986 can be utilized in studies focusing on cancer biology and therapeutic strategies aimed at modulating protein levels within cells.
SJPYT-195 is a potent GSPT1 degrader that functions through targeted protein degradation mechanisms. This compound induces proteolysis of GSPT1, leading to cytotoxic effects in various cell types. It is a valuable tool for research applications focused on studying GSPT1-related pathways and for the synthesis of PROTACs (Proteolysis Targeting Chimeras) designed to selectively degrade proteins of interest.
Synonyms: (Rac)-CFT7455
(Rac)-Cemsidomide is a PROTAC degrader targeting IKZF1 and IKZF3, exhibiting potent antitumor activity through its molecular glue mechanism. This compound demonstrates a GI50 of 0.05 nM in NCIH929.1 cells, making it a valuable tool for research applications focused on the degradation of Ikaros and Aiolos proteins. Its unique properties facilitate investigations into mechanisms of action related to targeted protein degradation in cancer therapies.
dCeMM1 is a selective degrader of RBM39 that operates through the recruitment of the CRL4DCAF15 E3 ligase complex. This compound effectively reduces the protein levels of RBM39 in wild-type KBM7 cells, offering a potent tool for studying the role of RBM39 in cellular processes. dCeMM1's mechanism provides valuable insights for research applications in targeted protein degradation and cancer biology.
EM12-FS is a molecular glue degrader specifically targeting NTAQ1 through its interaction with the cereblon (CRBN) ligand at His353. This compound facilitates the degradation of NTAQ1, enabling researchers to investigate the role of this protein in various biological processes. With a human plasma half-life of 196 minutes, EM12-FS is suitable for in vitro studies and offers potential applications in drug discovery and therapeutic development.
GSPT1 degrader-4 is a molecular glue targeting GSPT1, exhibiting a DC50 value of 25.4 nM. This compound has demonstrated an IC50 of 39 nM in inhibiting the proliferation of CAL51 cells. GSPT1 degrader-4 is primarily utilized in research related to protein degradation mechanisms and can aid in studies of cellular processes related to GSPT1 function.
GSPT1 Degrader-16 is a potent cereblon-based molecular glue degrader that selectively targets G1 to S phase transition 1 (GSPT1). It exhibits significant inhibitory effects on various cancer cell lines, including RS4;11, Molt4, and MM.1S, with IC50 values of 0.002, 0.26, and 0.37 μM, respectively. This compound is valuable for research applications related to cancer biology, particularly in the study of acute lymphoblastic leukemia.
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dRRM-1 is a DCAF15-dependent molecular glue degrader targeting RBM23 and RBM39. This compound facilitates the selective degradation of these RNA-binding proteins, thereby influencing cellular RNA metabolism. dRRM-1 is designed for research applications focused on cancer biology, particularly in studies examining the regulatory roles of RNA-binding proteins in tumorigenesis.
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GSPT1 Degrader-6 is a selective degrader targeting GSPT1 through a unique mechanism that promotes the recruitment of the ubiquitin-proteasome system for degradation. With a DC50 value of 13 nM, it demonstrates potent biological activity in modulating GSPT1 levels. This compound is primarily used in research applications focusing on protein homeostasis, cellular stress responses, and the therapeutic modulation of GSPT1-related pathways.
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GSPT2 Degrader-1 is a selective molecular glue designed to target GSPT2 through a unique mechanism of action. This compound combines Thalidomide with the MDEG-541 linker, effectively inducing the degradation of GSPT2 without affecting GSPT1 or MYC. GSPT2 Degrader-1 is valuable for research applications focused on gastrointestinal cancer, offering insights into the role of GSPT2 in tumor biology and potential therapeutic interventions.
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GSPT1 Degrader-5 is a potent GSPT1-targeting molecule that functions as a proteolysis-targeting chimera (PROTAC) with a DC50 of 144 nM. This compound selectively degrades GSPT1, a crucial regulatory protein involved in translation termination and mRNA surveillance. GSPT1 Degrader-5 is valuable for research applications focused on understanding the role of GSPT1 in various cellular processes and its implications in disease models.
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GSPT1 degrader-15 is a selective degrader targeting GSPT1, with a DC50 of 154 nM. This compound demonstrates substantial anti-proliferative effects on leukemia and lymphoma cells, while exhibiting minimal impact on the expression of other proteins. GSPT1 degrader-15 is suitable for research applications focused on leukemia and lymphoma, providing a valuable tool for investigating GSPT1-related pathways in cancer biology.
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P131 is a PROTAC molecule that targets Bruton's tyrosine kinase (BTK) for degradation through the Cereblon ligase complex. This compound is effective in degrading both wild-type and C481S mutant BTK with nanomolar potencies. P131 is utilized in research applications focused on the modulation of BTK activity, providing insights into its role in various B-cell malignancies and related signaling pathways.
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NR-V04 is a selective degrader targeting NR4A1 via a PROTAC mechanism. It facilitates the formation of a ternary complex with NR4A1 and the VHL E3 ligase, promoting proteasome-dependent degradation of NR4A1. Through its action, NR-V04 has been shown to enhance the infiltration of tumor-associated B cells and effector memory CD8+ T cells while decreasing monocytic myeloid-derived suppressor cells within tumor microenvironments. This compound is valuable for research related to melanoma and colon cancer.
ZXH-4-130 TFA is a potent and selective degrader of Cereblon (CRBN), functioning as a CRBN-VHL heterobifunctional protein degrader (PROTAC). This compound exhibits significant biological activity, inducing approximately 80% CRBN degradation at a concentration of 10 nM in MM1.S cells. ZXH-4-130 TFA is a valuable tool for investigating CRBN-mediated pathways and protein degradation mechanisms in various research applications.
MS6105 is a selective LDH-targeted PROTAC that induces the degradation of LDHA and LDHB through the ubiquitin-proteasome system. This compound exhibits notable anticancer activity, making it a valuable tool for cancer research. Additionally, MS6105 features an alkyne group, facilitating copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, enabling diverse applications in chemical biology and drug discovery.
PROTAC PD-L1 degrader-1 is a CRBN-based protein degrader targeting PD-L1, facilitating the selective degradation of the PD-L1 protein. This compound demonstrates potent PD-L1 degradation in 4T1 cells, with a DC50 value of 0.609 μM. It serves as a valuable tool for investigating therapeutic approaches in breast cancer research.
ERD-3111 is an orally active PROTAC degrader targeting estrogen receptor alpha (ERα) with a reported DC50 of 0.5 nM. This compound effectively inhibits tumor growth in both wild-type MCF-7 xenograft models and in models harboring clinically relevant ESR1 mutations. ERD-3111 is a valuable tool for research focused on estrogen receptor-positive breast cancer, facilitating investigations into targeted degradation pathways and therapeutic strategies.
PROTAC ER Degrader-4 is a von Hippel-Lindau-based PROTAC that targets the estrogen receptor (ER). It demonstrates high potency, binding to ER with an IC50 of 0.8 nM, and effectively induces ER degradation in MCF-7 cells with an IC50 of 0.3 nM. This compound is valuable for research applications focused on hormone receptor signaling and targeted protein degradation.
PROTAC VHL-type degrader-1 is a VHL-type PROTAC degrader that facilitates the targeted degradation of the ATM protein. This compound enhances the efficacy of the ATR inhibitor AZD6738 through a synergistic mechanism, making it a valuable tool for investigating the interplay between ATM and ATR signaling pathways. It is applicable in research focusing on cancer therapeutics and cellular response to DNA damage.
