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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.
GBD-9 is a dual-action degrader that targets both BTK and GSPT1 by recruiting the E3 ligase cereblon (CRBN). It acts as a PROTAC to promote BTK degradation and functions as a molecular glue to induce GSPT1 degradation. GBD-9 exhibits significant antiproliferative activity in cancer cells, making it a promising candidate for cancer research.
Synonyms: ARV-766
Luxdegalutamide (ARV-766) is an orally active proteolysis-targeting chimera (PROTAC) designed to selectively degrade the androgen receptor (AR), including clinically relevant resistance-associated mutants such as T878A, H875Y, and L702H. By inducing AR ubiquitination and proteasomal degradation, Luxdegalutamide effectively suppresses AR signaling and exhibits potent antitumor activity. It is a promising therapeutic agent and research tool for studying castration-resistant prostate cancer (CRPC) and mechanisms of AR-driven oncogenesis.
CFT8634 is an orally bioavailable PROTAC that targets the E3 ubiquitin ligase CRBN to degrade BRD9. This heterobifunctional molecule effectively inhibits the growth of tumor cells reliant on BRD9, making it a valuable tool for researching synovial sarcoma and SMARCB1-deficient solid tumors. CFT8634 facilitates targeted degradation through its unique binding properties, offering a strategic approach to investigate the role of BRD9 in SMARCB1-related cancers, including malignant rhabdoid tumors.
PROTAC B-Raf degrader 1 is a proteolysis targeting chimera (PROTAC) that facilitates the degradation of B-Raf through a Cereblon ligand. This compound demonstrates significant anti-cancer activity, making it a valuable tool for cancer research. It is particularly useful in studies investigating B-Raf-mediated signaling pathways and therapeutic strategies targeting oncogenic mutations in B-Raf.
PROTAC K-Ras Degrader-4 specifically targets and degrades mutant KRAS proteins, including KRASG12D and KRASG12V, with DC50 values of 1 nM and 13 nM, respectively. By inhibiting the MAPK signaling pathway, this compound serves as a powerful tool for studying the functional implications of KRAS mutations in cancer biology. Research applications include elucidating the role of KRAS in tumorigenesis and evaluating the therapeutic potential of targeting this oncogene in various malignancies.
PROTAC-O4I2 is a targeted protein degraders (PROTAC) that specifically degrades splicing factor 3B1 (SF3B1). It demonstrates an IC50 value of 0.244 μM for inducing FLAG-SF3B1 degradation in K562 cells. Additionally, PROTAC-O4I2 promotes cellular apoptosis in K562 wild-type cells, making it a valuable tool for studying the functional role of SF3B1 in various biological contexts. This compound is suitable for investigating the therapeutic potential of SF3B1 modulation in cancer research.
ACBI2 is a potent VHL PROTAC designed for the targeted degradation of SMARCA2. With an EC50 of 7 nM and a DC50 of 1 nM in RKO cells, ACBI2 selectively modulates SMARCA2 levels, making it a valuable tool for studying SMARCA2-related pathways. This compound is particularly relevant in lung cancer research, facilitating investigations into therapeutic strategies targeting SMARCA2 degradation.
PROTAC AR-V7 degrader-1 is a selective degrader targeting the androgen receptor variant 7 (AR-V7) through the PROTAC mechanism. With a DC50 of 0.32 μM in 22Rv1 cells, this compound demonstrates potent inhibition of tumor cell proliferation and exhibits significant anti-tumor activity. It is particularly relevant for research applications focusing on prostate cancer and can aid in the development of targeted therapeutic strategies.
MS8815 is a selective enhancer of the enhancer of zeste homolog 2 (EZH2) and functions as a PROTAC degrader. With an IC50 value of 8.6 nM, MS8815 demonstrates potent inhibitory activity against EZH2. This compound is valuable for research applications focused on triple-negative breast cancer (TNBC) and other conditions influenced by EZH2 activity.
Synonyms: ASP-3082; KRAS G12D inhibitor 17
Setidegrasib is a PROTAC degrader specifically targeting the KRAS G12D mutation with a DC50 of 37 nM. This compound effectively induces the degradation of KRAS G12D protein, leading to the suppression of key signaling molecules such as p-ERK, p-AKT, and p-S6 in AsPC-1 cells. Setidegrasib demonstrates significant anti-tumor activity across various cancer xenograft models, making it a valuable tool for studying KRAS(G12D)-mutated solid tumors.
ARV-393 is a potent BCL6 PROTAC degrader that facilitates the ubiquitination and subsequent proteasomal degradation of BCL6. This compound exhibits significant biological activity and is particularly relevant for research focused on advanced non-Hodgkin lymphoma. Its ability to modulate protein levels through targeted degradation makes it a valuable tool for elucidating BCL6-related pathways in cancer biology.
CP5V is a PROTAC that targets Cdc20 for degradation through the recruitment of the von Hippel-Lindau (VHL) complex. By facilitating the ubiquitination of Cdc20, CP5V promotes proteasomal degradation, leading to mitotic inhibition. This compound has significant applications in research focused on cancer cell proliferation and cell cycle regulation.
SJ10542 is a potent and selective PROTAC degrader targeting JAK2 and JAK3. With DC50 values of 14 nM for JAK2 and 11 nM for JAK3 in patient-derived xenograft cells (PDX), SJ10542 demonstrates significant antitumor activity. This compound is valuable for research in hematological malignancies and autoimmune diseases, facilitating the exploration of targeted degradation mechanisms in these therapeutic areas.
Synonyms: PROTAC BRD4 Degrader-5
GAL-02-221 is a PROTAC designed to target and degrade BRD4 through ligands that recruit von Hippel-Lindau (VHL) E3 ligase. This compound effectively promotes the degradation of BRD4 in both HER2-positive and negative breast cancer cell lines, demonstrating potential utility in the study of tumor biology and therapeutic approaches. Its ability to selectively eliminate BRD4 highlights its relevance in cancer research and provides a valuable tool for investigating mechanisms of oncogenesis and treatment resistance.
MS159 is a potent PROTAC degrader targeting nuclear receptor binding SET domain protein 2 (NSD2). It effectively inhibits tumor cell growth, making it a valuable tool for investigating the biological functions of NSD2 in various health and disease contexts. This compound serves as an important resource for researchers studying the therapeutic potential of NSD2 modulation.
SIM1 is a highly potent von Hippel-Lindau (VHL)-based trivalent PROTAC that specifically targets the degradation of BET family proteins, with a notable preference for BRD2 (IC50=1.1 nM; Kd=186 nM). This compound has demonstrated sustained anti-cancer activity, making it a valuable tool for researchers investigating the roles of BET proteins in oncogenesis and other related biological pathways. Its application in PROTAC-mediated protein degradation provides unique avenues for therapeutic intervention in cancers driven by BET overexpression.
Synonyms: RC32
FKBP12 PROTAC RC32 is a targeted protein degrader utilizing PROTAC technology to selectively degrade FKBP12. This compound combines Rapamycin, a well-characterized immunosuppressant, with a Cereblon E3 ubiquitin ligase ligand derived from Pomalidomide, facilitating the ubiquitination and subsequent proteasomal degradation of FKBP12. It serves as an important tool in research applications aimed at investigating the modulation of protein levels and the functional consequences of targeted degradation in various biological contexts.
SHP2-D26 is a potent SHP2 degrader that functions as a PROTAC by facilitating the recruitment of the VHL-1 E3 ligase to the SHP2 protein. This dual-target mechanism efficiently induces the degradation of SHP2 in a neddylation- and proteasome-dependent manner. SHP2-D26 is valuable for research applications in understanding esophageal cancer and acute myeloid leukemia, providing insights into SHP2's role in these malignancies.
SK-3-91 is a multi-kinase degrader functioning through the ubiquitin biotinylation (E-STUB) pathway to induce the degradation of over 125 unique kinases. This PROTAC effectively reduces the levels of YTHDF2, contributing to the inhibition of cell proliferation and morphological alterations in treated cells. Its design facilitates the selective targeting and degradation of diverse kinases, making it a valuable tool for studying kinase function and exploring therapeutic applications in cancer research.
MS21 is a potent AKT PROTAC degrader designed to selectively target and degrade AKT proteins. This compound effectively inhibits mutations within the PI3K/PTEN pathway, leading to suppressed tumor cell proliferation and induction of cell cycle arrest. MS21 demonstrates significant anti-tumor activity, making it a valuable tool for cancer research and therapeutic development.
HJM-561 is a selective EGFR PROTAC degrader that effectively targets and degrades EGFR mutations resistant to conventional therapies, such as Osimertinib. It demonstrates potent degradation activity against key triple mutations including Del19/T790M/C797S (DC50: 9.2 nM) and L858R/T790M/C797S (DC50: 5.8 nM). HJM-561's mechanism provides promising potential for anti-tumor applications in the treatment of EGFR-driven malignancies.
PROTAC Bcl-xL Degrader-2 is a highly effective protein degrader targeting Bcl-xL, a member of the Bcl-2 family. Utilizing a von Hippel-Lindau ligand, this compound demonstrates a potent inhibition with an IC50 of 0.6 nM. It facilitates the selective degradation of Bcl-xL, making it a valuable tool for research in apoptotic processes and cancer therapy. Laboratory applications include studying the role of Bcl-xL in cell survival and investigating therapeutic strategies in Bcl-2-associated malignancies.
dTAGV-1 hydrochloride is a highly selective degrader targeting FKBP12F36V-tagged proteins through the PROTAC mechanism. This compound effectively induces the degradation of FKBP12F36V-Nluc in vivo, making it a valuable tool for studies involving targeted protein degradation. Its application in research facilitates the investigation of protein function, dynamics, and the development of therapies that exploit the proteolysis pathway.
PROTAC GPX4 degrader-1 functions as a targeted protein degradation agent specifically for GPX4. It exhibits a DC50 of 0.03 μM in HT1080 cells, demonstrating potent activity in promoting the degradation of GPX4. This compound is applicable in research exploring the role of GPX4 in various cellular processes and the therapeutic potentials of targeting antioxidant defenses in disease models.
SJF-0628 is a RAF PROTAC degrader that facilitates the targeted degradation of BRAF protein in cancer cell lines, specifically in colorectal cancer models (Colo-205, LS-411N, HT-29, RKO) and the triple-negative breast cancer line DU-4475. This compound significantly reduces levels of phosphorylated MEK and ERK in DU-4475 cells, demonstrating notable anti-tumor activity. SJF-0628 is valuable for research studies focused on the mechanisms of colorectal cancer and triple-negative breast cancer.
