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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.
WIZ Degrader 3 (Compound 29) is a selective degrader targeting widely interspaced zinc finger motifs (WIZ), exhibiting an AC50 of 6.4 nM. This compound effectively induces the expression of fetal hemoglobin (HbF) with an EC50 of 45 nM. WIZ Degrader 3 is valuable for research in blood disorders, including sickle cell disease and β-thalassemia, facilitating studies on therapeutic strategies for these conditions.
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WIZ Degrader 7 is a potent WIZ degrader with an IC50 value of less than 0.01 μM. It is designed for the targeted degradation of WIZ proteins, making it a valuable tool in the study of sickle cell disease (SCD) and thalassemia. This compound enables researchers to explore the mechanistic pathways involved in these hemoglobin disorders and assess potential therapeutic interventions.
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WIZ Degrader 6 is a potent WIZ degrader with an EC50 of less than 0.01 μM, effectively targeting the WIZ protein. This compound plays a critical role in cellular pathways associated with sickle cell disease, providing a valuable tool for investigating disease mechanisms and potential therapeutic approaches. Its high specificity and efficacy make it suitable for research applications focused on cellular degradation processes.
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WIZ Degrader 5 is a selective degrader targeting the WIZ protein, facilitating efficient degradation with a maximum efficacy of 88.6% observed in 293T cells. This reagent is particularly valuable for investigating the biological mechanisms underlying sickle cell disease, enabling researchers to explore novel therapeutic approaches.
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AUR1545 is a selective degrader of KAT2A and KAT2B, which plays a crucial role in the modulation of monocyte differentiation and the inhibition of acute myeloid leukemia cell proliferation. This compound has demonstrated efficacy in inducing epithelial differentiation and suppressing tumor growth in small cell lung cancer models. Additionally, AUR1545 promotes differentiation and inhibits growth in neuroendocrine prostate cancer cells, including primary patient-derived organoids. Its application extends to critical research in acute myeloid leukemia, small cell lung cancer, and neuroendocrine prostate cancer.
BT-O2C is a selective p300 PROTAC degrader that effectively reduces p300 levels in HAP1 cells. It exhibits significant cytotoxicity in CIC:DUX4 sarcoma cell lines, with IC50 values ranging from 152 to 221 nM, and notably decreases the expression of target genes associated with CDS, such as ETV1, ETV4, and ETV5. This compound serves as a valuable tool for research in cancer biology, facilitating studies on p300's role in oncogenic processes.
WIZ Degrader 4 is a WIZ degrader that exhibits an AC50 value of 160 nM. This compound plays a critical role in targeted protein degradation, facilitating the investigation of underlying mechanisms in sickle cell disease (SCD) and thalassemia. Its application in research aids in understanding disease pathology and therapeutic development.
GSK699 is a PROTAC degrader targeting PCAF/GCN5, promoting their ubiquitination and subsequent proteasomal degradation. This compound effectively inhibits the production of key cytokines and chemokines, such as interleukin-6 (IL-6) and CXCL1/GROα, thus demonstrating significant anti-inflammatory properties. GSK699 is suitable for investigations related to inflammatory diseases and other conditions modulated by these target proteins.
PROTAC CBP/p300/BRD4 Degrader-1 is a dual-target PROTAC degrader that specifically targets BRD4, CBP, and p300, achieving DC50 values of 8.8 pM, 6.55 nM, and 1.05 nM, respectively. This compound promotes CRBN- and proteasome-mediated degradation of BRD4 and CBP/p300, leading to the downregulation of c-Myc and acetyl-H3K27, and inducing apoptosis. It exhibits significant antiproliferative and antitumor effects, demonstrated by tumor growth inhibition in xenograft models. PROTAC CBP/p300/BRD4 Degrader-1 is a valuable tool for research focused on prostate and colorectal cancer.
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PROTAC CBP/P300 Degrader-2 is a PROTAC that targets the CBP and p300 proteins, promoting their degradation via the ubiquitin-proteasome system. This compound is effective in modulating gene transcription and can be utilized in research studies focused on cancer, autoimmune disorders, inflammatory conditions, and neurodegenerative diseases. Its potential to selectively degrade these co-activators makes it a valuable tool for investigating the therapeutic implications of targeting transcriptional regulation in various disease contexts.
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MRT-2359 is a selective degrader of GSPT1, exhibiting potent inhibition with an IC50 between 30 and 300 nM. This compound induces apoptosis through mechanisms that depend on protein translation, demonstrating significant anti-proliferative effects, particularly in MYC-driven cancer cell lines, including non-small cell and small cell lung cancers with elevated N-Myc or L-Myc expression. Additionally, MRT-2359 effectively targets drug-resistant NSCLC and SCLC cells, making it a valuable tool for cancer research applications.
Synonyms: KT-253
Seldegamadlin is a selective p53 stabilizer and an MDM2 PROTAC degrader with a DC50 of 0.4 nM. It effectively inhibits the proliferation of RS4;11 cancer cells, demonstrating an IC50 of 0.3 nM, and induces cell cycle arrest at the G2/M phase while promoting apoptosis. By upregulating p53 activity, Seldegamadlin overcomes the p53-MDM2 feedback loop, making it a valuable tool for research in hematologic and solid tumors, including acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL).
BWA-522 is an orally active PROTAC degrader that targets the full-length androgen receptor (AR-FL) and its splice variant AR-V7. By antagonizing the N-terminal domain of the androgen receptor, BWA-522 effectively suppresses downstream signaling pathways and induces apoptosis in cancer cells. Furthermore, this compound has demonstrated significant inhibition of tumor growth in LNCaP xenograft mouse models, making it a valuable tool for prostate cancer research.
PROTAC CDK4/6 degrader 1 is a dual-targeted degrader designed to selectively degrade cyclin-dependent kinases CDK4 and CDK6. With DC50 values of 10.5 nM and 2.5 nM, this compound effectively inhibits cell proliferation in Jurkat cells, demonstrating an IC50 of 0.18 μM. The compound promotes G1 phase cell cycle arrest and triggers apoptosis, making it a valuable tool for studying cancer biology and potential therapeutic applications in CDK-related malignancies.
CPD-10 is a targeted CCND1 and CDK4 PROTAC degrader that effectively promotes the degradation of these proteins. Exhibiting significant anti-proliferative activity, CPD-10 induces apoptosis in cancer cell lines. It decreases the expression levels of cyclin D1, cyclin D3, CDK4, and phosphorylated Rb at serines 5807 and 811 in a dose-dependent manner, making it a valuable tool for research in cancer biology and therapeutic applications targeting cell cycle regulation.
PROTAC EGFR Degrader 9 is a CRBN-based PROTAC designed to specifically target and degrade the mutant forms of the epidermal growth factor receptor (EGFR), particularly EGFRL858R/T790M/C797S. It demonstrates potent degradation activity with a DC50 of 10.2 nM and a Kd of 240.2 nM, effectively eliminating EGFR mutants while leaving wild-type EGFR unaffected. This compound serves as a valuable tool in cancer research, particularly in studies focused on targeted therapies for EGFR-driven malignancies.
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.
PROTAC AR Degrader-8 is an androgen receptor (AR) PROTAC degrader that effectively induces degradation of full-length AR (AR-FL) with DC50 values of 0.018 μM in 22Rv1 cells and 0.14 μM in LNCaP cells, as well as degrading the AR-V7 variant with a DC50 of 0.026 μM in 22Rv1 cells. This compound exhibits potent inhibition of cancer cell proliferation, with IC50 values of 0.038 μM and 1.11 μM in 22Rv1 and LNCaP cells, respectively. PROTAC AR Degrader-8 induces G2/M cell cycle arrest and promotes apoptosis in 22Rv1 cells, demonstrating significant anticancer efficacy in both murine and zebrafish models. It is a valuable tool for investigating mechanisms underlying prostate cancer and castration-resistant prostate cancer.
HEMTAC CDK4/6 degrader 1 is a PROTAC designed to target CDK4 and CDK6 through a dual-ligand approach involving HSP90. This compound effectively induces the degradation of CDK4/6 in B16F10 melanoma cells, leading to cell cycle arrest at the G0/G1 phase and subsequent apoptosis. It serves as a vital tool for cancer research, particularly in elucidating mechanisms of CDK4/6 regulation and their role in tumor progression. Additionally, HEMTAC CDK4/6 degrader 1 features an alkyne functional group, enabling copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing compounds for advanced applications in chemical biology.
PROTAC ERα Degrader-4 is a selective degrader targeting estrogen receptor alpha (ERα) through the PROTAC mechanism. It exhibits potent inhibitory activity with a Ki value of 5.08 μM, effectively leading to the degradation of ERα in both Tamoxifen-sensitive and resistant ER+ breast cancer cells, as well as in ERα-mutated breast cancer cell lines. Additionally, PROTAC ERα Degrader-4 induces apoptosis, making it a valuable tool for cancer research aimed at understanding and combating ERα-driven malignancies.
SIAIS039 is an orally active PROTAC targeting the c-ros oncogene 1 (ROS1), exhibiting DC50 values of 154.46 nM, 126.47 nM, and 143.69 nM in HCC78 cells, and Ba/F3 cells expressing the CD74-ROS1 and SDC4-ROS1 fusions, respectively. This compound effectively suppresses cell proliferation, induces cell cycle arrest and apoptosis, and inhibits clonogenicity in ROS1-positive cells. Additionally, SIAIS039 demonstrates significant anti-tumor effects in vivo against ROS1-driven tumor growth, making it a valuable tool for research in targeted cancer therapy.
SZUH280 is a selective PROTAC degrader targeting HDAC8, demonstrating a DC50 of 0.58 μM in A549 cells. It effectively induces apoptosis in cancer cells and disrupts DNA repair mechanisms, thereby enhancing cellular radiosensitivity. This compound is particularly useful for research related to cancer therapeutics and the study of epigenetic regulation.
Thalidomide-5-CH2-NH2 hydrochloride serves as an E3 ligase ligand targeting cereblon (CRBN) for the development of PROTACs (Proteolysis Targeting Chimeras). This compound facilitates the selective recruitment of CRBN to ubiquitin-proteasome pathways, promoting the degradation of specific target proteins. Its application is pivotal in targeted protein degradation studies and drug discovery processes aimed at modulating protein levels in various biological contexts.
Synonyms: YX39-105
MS105 is a selective degrader of protein tyrosine kinase 6 (PTK6), functioning through the PROTAC mechanism. By recruiting the VHL E3 ligase, MS105 facilitates the ubiquitination and subsequent proteasomal degradation of PTK6. It demonstrates notable biological activity by inhibiting the proliferation and migration of breast cancer cells while also inducing apoptosis. This compound is valuable for research applications focused on breast cancer mechanisms and therapeutic strategies.
PROTAC eEF2K degrader-1 is a small molecule designed to target and induce degradation of the elongation factor 2 kinase (eEF2K). This compound has been shown to effectively promote apoptosis in MDA-MB-231 cancer cells, demonstrating its potential in cancer research. The mechanism of action involves the targeted elimination of eEF2K, providing a valuable tool for studying the role of this kinase in cellular processes and therapeutic applications.
