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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.
ARD-2128 is a highly potent, orally bioavailable PROTAC degrader targeting the androgen receptor (AR). It efficiently reduces AR protein levels, downregulates AR-regulated gene expression in tumor tissues, and inhibits tumor growth without observable toxicity. ARD-2128 is a promising tool for prostate cancer research.
TL13-112 is a potent and selective PROTAC degrader targeting ALK, with an IC₅₀ of 0.14 nM for ALK inhibition. In addition to ALK, TL13-112 also induces degradation of Aurora A (IC₅₀: 8550 nM), FER (42.4 nM), PTK2 (25.4 nM), and RPS6KA1 (677 nM), supporting its utility in kinase signaling and cancer research.
XY028-133 (Example 14) is a PROTAC-based degrader targeting CDK4/6, composed of ligands for von Hippel-Lindau (VHL) and CDK. It induces selective degradation of CDK4/6 and exhibits anti-tumor activity, making it a useful tool for cell cycle and cancer research.
dTAG-47 is a heterobifunctional degrader that selectively targets FKBP12^F36V-tagged proteins for degradation. By binding FKBP12^F36V, which acts as a degradation tag (dTAG), dTAG-47 enables conditional and selective protein degradation. It is a valuable tool for studying protein function in models such as basal-like breast cancer (BBC).
QC-01-175 is a heterobifunctional PROTAC molecule designed to degrade aberrant tau protein. It effectively reduces levels of A152T and P301L mutant tau, mitigates tau-mediated neurotoxicity, and enhances neuronal survival.
PROTAC IRAK4 Degrader-1 is a cereblon-based PROTAC targeting IRAK4, derived from US patent US20190192668A1 (Compound I-210). It induces IRAK4 degradation in OCI-LY-10 cells with 20–50% at 0.1 μM, and >50% at 1 μM.
CRBN-6-5-5-VHL is a potent and selective VHL-based PROTAC degrader targeting cereblon (CRBN), with a DC₅₀ of 1.5 nM. It selectively degrades CRBN without affecting neo-substrates IKZF1 and IKZF3.
LLC0424 is a potent and selective cereblon-based PROTAC that targets NSD2 for degradation. It induces NSD2 degradation in a cereblon- and proteasome-dependent manner, with a DC₅₀ of 20 nM in RPMI-8402 cells.
CBPD-409 is an orally active PROTAC degrader targeting CBP/p300, with a DC₅₀ of 0.2–0.4 nM. It shows potent antiproliferative activity in AR⁺ prostate cancer cell lines (VCaP, LNCaP, 22Rv1) with IC₅₀ values of 1.2–2.0 nM and demonstrates significant antitumor efficacy.
xStAx-VHLL is a PROTAC degrader targeting β-catenin, promoting its ubiquitination and proteasomal degradation. It effectively inhibits the Wnt/β-catenin signaling pathway and suppresses proliferation of colon cancer cells, demonstrating anti-tumor activity.
DAS-5-oCRBN is a selective and potent PROTAC degrader of c-Src kinase, acting through CRBN-mediated ubiquitination. It effectively reduces c-Src levels and inhibits proliferation in c-Src-dependent cancer cell lines, making it a useful tool for targeted protein degradation research.
MS9427 TFA is a potent PROTAC degrader targeting EGFR, with binding affinities (K_d) of 7.1 nM for wild-type EGFR and 4.3 nM for the EGFR L858R mutant. It selectively degrades the mutant EGFR via both the ubiquitin–proteasome system (UPS) and autophagy–lysosome pathways. MS9427 TFA effectively inhibits the proliferation of non-small cell lung cancer (NSCLC) cells and is a valuable tool for anticancer research focused on EGFR-driven malignancies.
SMD-3040 formate is a potent and selective PROTAC degrader targeting SMARCA2, a core ATPase subunit of the SWI/SNF chromatin remodeling complex. It exhibits strong in vivo antitumor activity, making it a promising candidate for cancer research involving epigenetic regulation and synthetic lethality strategies.
LL-K8-22 is a potent, selective, and durable PROTAC degrader targeting the CDK8–cyclin C complex, with DC₅₀ values of 2.52 μM and 2.64 μM, respectively. It suppresses STAT1 Ser727 phosphorylation and inhibits E2F- and MYC-driven oncogenic transcriptional programs. LL-K8-22 shows potential for use in triple-negative breast cancer (TNBC) research and related therapeutic studies.
MS15 TFA is a potent and selective PROTAC degrader targeting AKT isoforms. It inhibits the activity of AKT1, AKT2, and AKT3 with IC₅₀ values of 798 nM, 90 nM, and 544 nM, respectively. MS15 TFA serves as a valuable tool for studying AKT signaling and its role in cancer and metabolic diseases.
PROTAC NCOA4 Degrader-1 (Compound V3) is a highly potent PROTAC targeting NCOA4, with a DC₅₀ of 3 nM in HeLa cells. It functions as a ferroptosis inhibitor by reducing NCOA4 levels and lowering intracellular ferrous iron (Fe²⁺) concentrations. PROTAC NCOA4 Degrader-1 has demonstrated protective effects in a CCl₄-induced acute liver injury model, making it a valuable tool for studying ferroptosis and liver disease therapeutics.
SS47 TFA is a PROTAC-based degrader targeting hematopoietic progenitor kinase 1 (HPK1), an immunosuppressive regulatory kinase. It induces proteasome-mediated degradation of HPK1 and significantly enhances the antitumor efficacy of BCMA CAR-T cell therapy in vivo. In addition to its biological function, SS47 TFA is also a click chemistry reagent containing an alkyne group, allowing it to participate in copper-catalyzed azide–alkyne cycloaddition (CuAAC) with azide-functionalized molecules. This dual functionality makes SS47 TFA a valuable tool in both cancer immunotherapy research and chemical biology applications.
SJ1008030 (Compound 8) formic is a selective PROTAC degrader of JAK2, designed to target and eliminate JAK2 protein via the ubiquitin–proteasome pathway. It effectively inhibits the growth of MHH–CALL-4 leukemia cells with an IC₅₀ of 5.4 nM. SJ1008030 formic is a valuable tool for leukemia research and the study of JAK2-driven signaling pathways.
dAURK-4 hydrochloride is a potent and selective PROTAC degrader targeting Aurora A kinase (AURKA), derived from the AURKA inhibitor Alisertib. It effectively induces AURKA degradation and exhibits notable anticancer activity, making it a valuable agent for studying AURKA-driven oncogenic pathways and therapeutic development.
SIAIS164018 hydrochloride is a PROTAC-based dual degrader targeting ALK and EGFR, with IC₅₀ values of 2.5 nM for ALK and 6.6 nM for the ALK G1202R mutant. It effectively suppresses cancer cell migration and invasion, induces G1 phase cell cycle arrest, and promotes apoptosis, making it a promising candidate for targeted cancer therapy research.
PROTAC EZH2 Degrader-2 (Compound E-3P-MDM2) is a PROTAC molecule designed by linking the EZH2 inhibitor Tazemetostat (EPZ6438) to an E3 ligase ligand. It induces dose-dependent degradation of EZH2 in SU-DHL-6 cells, suppresses H3K27me3 expression, and concurrently degrades PRC2 components EED and SUZ12 without altering their mRNA levels. PROTAC EZH2 Degrader-2 exhibits strong anti-cancer and anti-proliferative activity, making it a valuable tool for epigenetic and oncology research.
CCT367766 formic is a third-generation, cereblon-based heterobifunctional PROTAC and pirin-targeting protein degradation probe (PDP). It effectively depletes pirin protein expression at low concentrations. CCT367766 formic demonstrates moderate affinity for the CRBN–DDB1 complex (IC₅₀ = 490 nM) and strong binding affinity for recombinant pirin and CRBN, with K_d values of 55 nM and 120 nM, respectively. This compound serves as a valuable chemical tool for exploring the biological roles of the largely understudied protein pirin.
PROTAC CDK12/13 Degrader-1 (7f) is a highly selective dual degrader targeting CDK12 and CDK13, with DC₅₀ values of 2.2 nM and 2.1 nM, respectively. It exhibits potent anti-proliferative activity and serves as a valuable tool for investigating transcriptional regulation and therapeutic strategies in breast cancer research.
MS9715 is a potent and selective PROTAC degrader targeting NSD3, designed by conjugating the NSD3 PWWP1 domain binder BI-9321 to a von Hippel-Lindau (VHL) E3 ligase ligand. It effectively induces degradation of NSD3 and holds significant potential for research in NSD3-dependent cancers, offering a novel approach to target epigenetic drivers in oncology.
MS181 (Compound 1) is a potent PROTAC degrader that targets components of the polycomb repressive complex 1 (PRC1) by recruiting cereblon (CRBN) and binding EED. It effectively reduces the expression of key PRC1 and PRC2 components, including EED, EZH2, SUZ12, BMI1, and RING1B. MS181 exhibits significant antiproliferative activity, making it a valuable tool for studying epigenetic regulation and potential cancer therapeutics.
