Catalog No.
Product Name
Application
Product Information
Citations
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PROTAC CDK4/6 Degrader
BSJ-03-204 is a potent and selective PROTAC degrader targeting CDK4 and CDK6, constructed by linking Palbociclib to a cereblon ligand. It exhibits IC₅₀ values of 26.9 nM for CDK4/D1 and 10.4 nM for CDK6/D1, without inducing degradation of IKZF1 or IKZF3. BSJ-03-204 demonstrates strong anti-cancer activity and is a valuable tool for cell cycle and oncology research. -
multi-kinase PROTAC degrader
TL12-186 is a cereblon-dependent PROTAC degrader with broad-spectrum activity against multiple kinases, including CDKs, BTK, FLT3, Aurora kinases, TEC, ULK, and ITK. It inhibits CDK2/cyclin A and CDK9/cyclin T1 with IC₅₀ values of 73 nM and 55 nM, respectively, making it a valuable tool for studying kinase-driven signaling pathways and cancer biology. -
PROTAC CDK4/6 degrader
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. -
estrogen receptor PROTAC protein degrader
Vepdegestrant (ARV-471) is an orally bioavailable PROTAC designed to target and degrade the estrogen receptor (ER). It is being developed for the treatment of patients with locally advanced or metastatic ER+/HER2− breast cancer, offering a novel approach to overcome endocrine resistance through targeted ER degradation. -
EZH2 PROTAC Degrader
MS177 is a fast-acting and effective PROTAC degrader targeting EZH2. It comprises a cereblon (CRBN) ligand, a linker, and the potent EZH2 enzymatic inhibitor C24 (IC₅₀: 12 nM). MS177 efficiently depletes both canonical EZH2–PRC2 and noncanonical EZH2–cMyc complexes, leading to inhibition of leukemia cell proliferation, induction of apoptosis, and cell cycle arrest. It is a valuable tool for epigenetic and cancer research. -
PROTAC-based EZH2 Degrader
MS1943 is an orally active, PROTAC-based selective degrader of EZH2 that effectively reduces cellular EZH2 levels. It exhibits strong anticancer activity, showing cytotoxic effects in various triple-negative breast cancer (TNBC) cell lines while sparing normal cells. MS1943 maintains high potency in inhibiting EZH2 methyltransferase activity (IC₅₀ = 120 nM) and demonstrates high selectivity for EZH2, making it a promising candidate for epigenetic and cancer research. -
androgen receptor (AR) PROTAC degrader
Bavdegalutamide (ARV-110) is an orally active and highly specific PROTAC degrader targeting the androgen receptor (AR). It induces ubiquitination and proteasomal degradation of AR, offering a novel therapeutic approach for AR-driven diseases such as prostate cancer. -
FKBP12F36V degrader
dTAG-13 is a PROTAC-based heterobifunctional degrader that selectively targets FKBP12^F36V fused in-frame to a protein of interest. By engaging both FKBP12^F36V and the cereblon (CRBN) E3 ligase, dTAG-13 induces efficient and selective degradation of FKBP12^F36V-tagged proteins, making it a valuable tool for conditional protein knockdown studies. -
Androgen Receptor (AR) degrader
ARCC-4 is a low-nanomolar PROTAC degrader targeting the androgen receptor (AR), with a DC₅₀ of 5 nM. Based on enzalutamide and incorporating a von Hippel-Lindau (VHL) E3 ligase ligand, ARCC-4 efficiently degrades both wild-type and clinically relevant AR mutants linked to resistance to antiandrogen therapy. It outperforms enzalutamide in potency and degradation efficacy, making it a promising candidate for advanced prostate cancer research. -
SMARCA2/SMARCA4/PBRM1 Degrader
AU-24118 is an orally bioavailable PROTAC degrader targeting the mSWI/SNF chromatin remodeling complex ATPases SMARCA2 and SMARCA4, as well as PBRM1. It offers a powerful approach for modulating epigenetic regulation and holds promise for the treatment of cancers driven by alterations in SWI/SNF complex components. -
PROTAC BRD9 Degrader
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
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. -
SMARCA2 Degrader
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. -
AR-V7 PROTAC Degrader
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. -
EZH2 Degrader
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. -
KRAS G12D PROTAC Degrader
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. -
BLC6 PROTAC Degrader
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. -
JAK2/3 PROTAC Degrader
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. -
PROTAC BRD4 Degrader
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. -
PROTAC FKBP12 Degrader
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. -
AKT PROTAC Degrader
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. -
EGFR PROTAC Degrader
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. -
FKBP12F36V PROTAC Degrader
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. -
GPX4 PROTAC Degrader
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. -
RAF PROTAC Degrader
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. -
PROTAC Degrader
HDAC6 degrader-1 is a PROTAC degrader targeting HDAC6, exhibiting a DC50 value of 3.8 nM in MM.1S cells. This compound efficiently induces the degradation of HDAC6 through a bifunctional strategy, linking a ligand for the E3 ligase Pomalidomide with a ligand for the target protein Nexturastat A via a specialized linker. Its application is vital for investigating the role of HDAC6 in cellular processes and potential therapeutic effects in various diseases. -
EZH2 Degrader
NUCC-0226272 is a potent PROTAC that facilitates the targeted degradation of EZH2. This compound exhibits significant anti-proliferative effects, making it a valuable tool for investigating the role of EZH2 in cancer biology. Its application in cancer research provides insights into potential therapeutic strategies for malignancies associated with EZH2 dysregulation. -
SMARCA2 PROTAC Degrader
YD23 is a selective SMARCA2 PROTAC degrader with DC50 values of 64 nM and 297 nM in H1792 and H1975 cell lines, respectively. This reagent induces the degradation of SMARCA2, exhibiting synthetic lethality towards SMARCA4-deficient cells and selectively inhibiting growth in SMARCA4 mutant lung cancer cells. YD23 also reduces chromatin accessibility in SMARCA4 deficient cells, impacting genes associated with cell cycle and growth regulation. It is a valuable tool for researching non-small cell lung cancer (NSCLC) and evaluating tumor growth in SMARCA4-mutant xenograft models. -
PROTAC FKBP12 Degrader
KB02-SLF is a PROTAC-based nuclear FKBP12 degrader designed to facilitate targeted protein degradation. It achieves this by covalently modifying DCAF16, an E3 ligase, thereby enhancing the stability of FKBP12 degradation within biological systems. The compound consists of a molecular glue linking the ubiquitin E3 ligase ligand KB02 with SLF, enabling efficient degradation of FKBP12 for various research applications in protein regulation and degradation pathways. -
PROTAC BRD4 Degrader
PROTAC BRD4 Degrader-8 is a proteolysis-targeting chimera (PROTAC) that engages both von Hippel-Lindau (VHL) and BRD4, exhibiting IC50 values of 1.1 nM for BRD4 BD1 and 1.4 nM for BRD4 BD2. This compound effectively promotes the degradation of BRD4 protein in PC3 prostate cancer cells, making it a valuable tool for research into BRD4-related signaling pathways and cancer therapeutics. Its high potency highlights its potential use in studying mechanisms of protein regulation and developing novel cancer treatments. -
PROTAC BRD Degrader
β-NF-JQ1 is a PROTAC that targets bromodomain-containing (BRD) proteins by leveraging β-NF as a ligand for the Aryl Hydrocarbon Receptor (AhR) E3 ligase. This compound facilitates the degradation of BRD proteins through the recruitment of AhR, leading to effective protein knockdown. β-NF-JQ1 demonstrates significant anticancer activity, making it a valuable tool for research in cancer biology and the development of targeted therapeutic strategies. -
CBP/p300 PROTAC Degrader
CBPD-268 is a highly potent CBP/p300 PROTAC degrader, exhibiting a DC50 value of ≤ 0.03 nM. This compound effectively induces degradation of CBP/p300 and demonstrates significant inhibition of cell growth, showcasing its antitumor potential. CBPD-268 is particularly relevant for research into androgen receptor-positive prostate cancer, facilitating studies on novel therapeutic strategies. -
FKBP12(F36V) Inhibitor
dTAGV-1-NEG is a diastereomer that acts as a heterobifunctional negative control for dTAGV-1, specifically targeted at FKBP12(F36V). This compound is utilized in research to study the selectivity and efficacy of FKBP12(F36V) degraders, helping to elucidate cellular mechanisms and pathways influenced by FKBP12 modulation. Its role as a control reagent makes it essential for validating experimental results in protein degradation studies. -
Isoform of SHP2-D26
SHP2-D26 isomer-1 is an isoform of the SHP2-D26 degrader, designed specifically for targeted protein degradation applications. This compound does not induce degradation of SHP2 at concentrations ranging from 3 to 1000 nM. As a component of PROTAC technology, SHP2-D26 isomer-1 serves as a valuable tool for studying SHP2's role in signaling pathways and assessing the therapeutic potential of SHP2 modulation in various diseases. -
PROTAC Degrader
SNX7886 is a potent PROTAC degrader targeting CDK8 and CDK19. It effectively induces degradation of CDK8 and CDK19, achieving up to 90% and 80% degradation, respectively, in 293 cells. This compound is valuable for research applications in understanding the role of CDK8/19 in various biological processes and cancer pathways. -
TBK1 Degrader
PROTAC TBK1 Degrader-2 is a targeted protein degrader designed to selectively degrade the serine/threonine kinase TANK-binding kinase 1 (TBK1) with a DC50 of 15 nM and Kd of 4.6 nM, exhibiting a maximum efficiency of 96%. Additionally, this compound also influences IkB kinase IKKε, demonstrating an IC50 of 8.7 nM, and displays a low selectivity over TBK1 with an IC50 of 1.3 nM. This reagent is suitable for investigating TBK1-related signaling pathways and potential therapeutic applications in various diseases. -
EZH2 PROTAC Degrader
MS8847 is a powerful EZH2 PROTAC degrader that utilizes the E3 ligase von Hippel-Lindau (VHL) to promote the degradation of EZH2 through the ubiquitin-proteasome system. This compound demonstrates robust anti-proliferative effects in acute myeloid leukemia (AML) and triple-negative breast cancer (TNBC) cell lines. MS8847 serves as a valuable tool for investigating the role of EZH2 in oncogenic signaling pathways and developing targeted therapies for EZH2-dependent malignancies. -
PROTAC CSK Degrader
DB-3-291 is a potent and selective PROTAC degrader targeting the protein CSK, exhibiting a Kd of 1 nM. This compound facilitates the degradation of CSK through its specific interaction with the E3 ligase, enabling in-depth studies of CSK-related biological pathways and providing insights into potential therapeutic strategies. It is valuable for researchers investigating targeted protein degradation and cancer biology. -
PROTAC KRAS G12C Degrader
PROTAC KRAS G12C degrader-1 is a Cereblon-based PROTAC targeting the KRAS G12C mutant. This compound promotes the formation of a dimer between Cereblon and KRAS G12C, leading to the degradation of GFP-tagged KRAS G12C in reporter cell systems. It serves as a valuable tool for research on targeted degradation strategies in KRAS-driven cancers. -
PROTAC CRBN Degrader
TD-165 is a PROTAC (proteolysis-targeting chimera) that targets cereblon (CRBN) for selective degradation of proteins. This compound features a CRBN ligand binding group, a linker, and a von Hippel-Landau (VHL) binding group, facilitating targeted ubiquitination and proteolytic degradation of specific proteins involved in cellular processes. TD-165 is suitable for research applications focused on targeted protein degradation, therapeutic development, and elucidating protein function in various biological contexts. -
PROTAC PARP1 Degrader
PROTAC PARP1 Degrader functions as a targeted protein degradation agent that specifically targets PARP1 through the MDM2 E3 ligase. This compound effectively induces PARP1 cleavage and promotes apoptosis in cancer cells, making it valuable for research in cancer therapies. The structure includes the MDM2 ligand, the PARP1 ligand, and a PEG-based linker, facilitating efficient delivery and degradation of the target protein. -
PROTACs
PROTAC BRD9 Degrader-4 is a bifunctional degrader targeting BRD9 through the proteolysis-targeting chimera (PROTAC) mechanism. It effectively induces degradation of BRD9, thereby altering oncogenic pathways associated with various cancers. This compound is utilized in cancer research to study the therapeutic potential of BRD9 modulation and the implications of targeted degradation in tumor biology. -
PROTAC IRAK Degrader
Zomiradomide is an orally bioavailable PROTAC degrader targeting IRAK4, with a DC50 of 6 nM, which effectively inhibits the NF-κB signaling pathway. In addition to its suppression of IRAK4, Zomiradomide functions as a molecular glue, facilitating the degradation of Ikaros with a DC50 of 1 nM and consequently activating the type I IFN signaling pathway. This dual action positions Zomiradomide as a valuable tool in research focused on immune modulation and inflammatory responses. -
MET Degrader
PRO-6E is a PROTAC that targets Cereblon to induce degradation of the MET protein. It achieves up to 81.9% degradation of MET at 1 μM in MKN-45 cells, effectively inhibiting tumor growth both in vitro and in vivo. Additionally, PRO-6E promotes apoptosis and cell cycle arrest, making it a valuable tool for research on MET-related oncogenic processes. -
Kinases PROTAC
DB1113 is a bifunctional compound designed for targeted protein degradation of various kinases. It effectively induces degradation of ABL1, ABL2, BLK, CDK4, CDK11B, EPHA3, MAPK7, RIPK1, and others, facilitating the investigation of kinase-related signaling pathways. DB1113 is suitable for research focusing on diseases or disorders associated with dysregulated kinase activity, providing a valuable tool for exploring therapeutic interventions in cancer and other conditions. -
dTAG-13 Negative Control
dTAG-13-NEG serves as a negative control for dTAG-13, a PROTAC-based bifunctional degrader that selectively targets FKBP12F36V in the presence of a protein of interest. While dTAG-13 promotes the degradation of FKBP12F36V, dTAG-13-NEG allows for the assessment of specificity and background in experimental setups involving this pathway. This compound is essential for validating experimental results when studying protein degradation mechanisms and their implications in cellular biology. -
SMARCA2 PROTAC degrader
SMD-3040 is a selective SMARCA2 PROTAC degrader with a DC50 of 12 nM and a maximal degradation efficiency of 91%. This compound effectively inhibits tumor cell proliferation, demonstrating significant antitumor activity. SMD-3040 is particularly useful in studies related to various tumors, including melanoma. -
PROTAC BRD4 Degrader
PROTAC BET Degrader-10 is a selective degrader targeting the BET protein BRD4 through a PROTAC mechanism, featuring a DC50 of 49 nM. This compound utilizes ligands for Cereblon and BRD4, promoting the ubiquitination and subsequent degradation of BRD4. It serves as a valuable tool for investigating the role of BRD4 in various biological processes and cancer-related research applications. -
PROTAC BTK Degrader
NRX-0492 is an orally active PROTAC BTK degrader that promotes the ubiquitination and proteasomal degradation of Bruton's tyrosine kinase (BTK) with DC50 values as low as 0.2 nM. This compound effectively inhibits B cell receptor (BCR)-mediated signaling, transcriptional programs, and chemokine secretion, demonstrating significant antitumor activity against chronic lymphocytic leukemia. NRX-0492 comprises a BTK inhibitor, an E3 ligase ligand derived from Thalidomide, and a PROTAC linker, making it a valuable tool for studying BTK-related pathways and therapies.
