Catalog No.
Product Name
Application
Product Information
Citations
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EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-11 is a targeted protein degrader designed to selectively degrade the EZH2 protein through a PROTAC mechanism. This compound effectively reduces tumor size and viability in three-dimensional spheroid models, demonstrating potential for cancer research applications. The technology leverages a dual-ligand system, incorporating an EZH2 ligand and a Cereblon ligand, connected by a linker to facilitate the targeted degradation process. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-45 is a specialized PROTAC protein degrader designed to target EZH2, exhibiting an IC50 of 22.97 μM in SU-DHL-6 cells. This compound is primarily utilized in research focused on diffuse large B-cell lymphoma, providing insights into epigenetic regulation through targeted protein degradation. The product includes a histone methyltransferase ligand and a VHL ligand, linked for enhanced efficacy in cellular studies. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-40 is a PROTAC protein degrader specifically designed to target the enhancer of zeste homolog 2 (EZH2), exhibiting an IC50 value of 15.35 μM in SU-DHL-6 cells. This compound is valuable for researching diffuse large B-cell lymphoma and related epigenetic mechanisms. Its structure consists of a histone methyltransferase ligand, an aminopeptidase ligand, and a linker, facilitating targeted degradation of EZH2 to explore therapeutic potential in cancer treatment. -
EZH2 PROTAC Degrader
PROTAC EZH2 Degrader-29 is a targeted protein degrader that specifically engages the EZH2 protein, exhibiting an IC50 of 24.53 μM in diffuse large B-cell lymphoma cells. This compound serves as a valuable tool for investigating the degradation of EZH2 in both basic and translational research settings related to diffuse large B-cell lymphoma and other malignancies. -
Molecule Glue
HuR degrader 2 is a molecular glue that specifically targets the RNA-binding protein Hu antigen R (HuR), leading to a significant degradation of approximately 30% of HuR at a concentration of 0.1 μM. This compound effectively inhibits the proliferation of the Colo-205 cancer cell line, demonstrating an IC50 of ≤200 nM. Additionally, HuR degrader 2 shows a high affinity for cereblon, with an HTRF ratio of less than 0.02, making it a valuable tool for studying HuR's role in cancer biology. -
Molecular Glue
MG-HuR2 is a molecular glue degrader that specifically targets the oncogenic RNA-binding protein HuR, exhibiting an IC50 of 0.5 μM. This compound is particularly relevant for research involving HuR-overexpressing malignancies, such as breast cancer, providing a valuable tool for investigating therapeutic strategies aimed at modulating HuR activity in cancerous tissues. -
METTL3-METTL14 Degrader
WD6305 is a selective PROTAC degrader targeting METTL3 and METTL14, with DC50 values of 140 nM and 194 nM, respectively. This compound effectively inhibits m6A modification and has been shown to suppress proliferation and induce apoptosis in acute myeloid leukemia (AML) cells. WD6305 demonstrates significant antitumor activity, making it a valuable tool for research on RNA modifications and cancer therapeutics. -
CRBN Degrader
WDR5 Degrader-1 is a cereblon (CRBN)-recruiting compound designed to selectively induce degradation of the WDR5 protein. This degrader effectively targets WDR5 while sparing the CRBN neo-substrate IKZF1, facilitating precise manipulation of WDR5 levels in cellular systems. It is a valuable tool for investigating the biological roles of WDR5 in transcriptional regulation and potential therapeutic strategies in diseases associated with dysregulated WDR5 expression. -
PROTAC WDR5 Degrader
XF067-68 is a PROTAC designed for the targeted degradation of the WD40 repeat domain protein 5 (WDR5). This compound facilitates the specific elimination of WDR5, making it a valuable tool for investigating diseases associated with WDR5 dysregulation. Researchers can employ XF067-68 to elucidate the biological roles of WDR5 and explore potential therapeutic interventions in related disorders. -
WDR5 Degrader
XF056-132 free base is a potent WDR5 (WD40 repeat domain protein 5) degrader that utilizes the proteolysis-targeting chimeric (PROTAC) mechanism. This compound effectively promotes the selective degradation of WDR5, which is implicated in various cancers and transcriptional regulation processes. XF056-132 serves as a valuable tool for research into targeted protein degradation and its therapeutic potential in oncological studies. -
WDR5 PROTAC Degrader
MS40 is a WDR5 PROTAC degrader with a Kd of 125 nM, which facilitates the ubiquitination and subsequent degradation of the WDR5 protein. The degradation of WDR5 causes the dissociation of the MLL/KMT2A complex from chromatin, leading to reduced levels of H3K4me2. This compound is instrumental in investigating the mechanistic pathways involved in primary leukemia. -
Ligands for Target Protein for PROTAC
Androgen Receptor Ligand 2 acts as a ligand for the androgen receptor, facilitating the targeted degradation of this protein through the PROTAC (proteolysis-targeting chimera) mechanism. This compound is integral for the synthesis of the PROTAC Androgen Receptor Degrader-1, enabling researchers to probe the functional role of the androgen receptor in various biological contexts. Its application extends to studies in cancer research and hormone-related disorders, where modulation of androgen receptor activity may serve as a therapeutic strategy. -
PAK4 Degrader
PAK4-IN-6 is a selective degrader of PAK4 (p21-activated kinase 4), functioning through targeted protein degradation mechanisms. This compound serves as a valuable tool in the synthesis of proteolysis-targeting chimeras (PROTACs) and has potential applications in cancer research and therapeutic development. Its ability to modulate PAK4 levels makes it instrumental in studying signaling pathways and cellular processes involving this kinase. -
PDIA1 PROTAC Degrader
PROTAC PDIA1 Degrader 1 is a PROTAC-based compound designed to selectively target and degrade PDIA1 through the recruitment of the E3 ligase CRBN. It exhibits significant anticancer activity, effectively inhibiting the proliferation of various cancer cell lines. This compound is a valuable tool for researchers investigating the role of PDIA1 in cancer biology and exploring potential therapeutic strategies for targeting this protein. -
KRAS(G12C) Degrader
YF135 is a reversible-covalent PROTAC specifically targeting KRAS(G12C). This compound facilitates the degradation of KRAS(G12C) by linking a potent KRAS G12C inhibitor with a VHL ligand scaffold, effectively promoting the proteasomal pathway via E3 ligase VHL. YF135 significantly reduces phospho-ERK levels, making it a valuable tool for research applications focused on KRAS(G12C)-associated pathways in cancer biology. -
PROTAC PLK4 Degrader
SP27 is a PROTAC that selectively degrades Polo-like kinase 4 (PLK4), exhibiting a DC50 of 19.5 nM. This compound is valuable for investigating the role of PLK4 in cellular processes and is particularly relevant in breast cancer research, enabling studies on potential therapeutic applications and mechanisms of action related to oncogenesis. -
PLK1 PROTAC Degrader
PROTAC PLK1 Degrader-3 is a PLK1-targeted PROTAC that facilitates the degradation of the Polo-like kinase 1 (PLK1) protein through the N-deglycosylation pathway, exhibiting a dissociation constant (Kd) of 2.2 μM. This compound is primarily utilized in research related to non-small cell lung cancer, enabling investigations into targeted protein degradation mechanisms. While the compound shows limited cell penetration, higher concentrations may be necessary to achieve effective degradation outcomes, making it suitable for various biological studies in oncological contexts. -
Ligands for Target Protein for PROTAC
SMARCA-BD ligand 1 for PROTAC hydrochloride is a selective ligand that specifically targets the BAF ATPase subunit SMARCA2. This compound facilitates the degradation of SMARCA2 through the PROTAC mechanism, making it a valuable tool for research into protein degradation pathways and epigenetic regulation. Its applications extend to studies on cancer biology and the development of targeted therapeutic strategies. -
SMARCA2 PROTAC Degrader
PRT3789 is a selective PROTAC degrader targeting SMARCA2, exhibiting a DC50 of 0.72 nM in HeLa cells for SMARCA2 and 14 nM for SMARCA4. By forming a stable ternary complex with Von Hippel-Lindau (VHL) E3 ligase, PRT3789 facilitates polyubiquitination and subsequent proteasomal degradation of SMARCA2. This compound effectively disrupts the integrity of the SWI/SNF chromatin remodeling complex, leading to the downregulation of oncogenic gene expression, decreased chromatin accessibility, and enhanced expression of genes related to antigen processing and presentation. PRT3789 is applicable in research on SMARCA4-mutated solid tumors, including non-small cell lung cancer, endometrial cancer, and several other malignancies. -
SMARCA2 PROTAC Degrader
NEP202 is a potent SMARCA2 PROTAC degrader that engages the GID4 E3 ligase to facilitate targeted protein degradation. This reagent is valuable for cancer research, enabling the selective degradation of SMARCA2, a key protein implicated in various oncogenic processes. NEP202 offers researchers a powerful tool for studying the role of SMARCA2 in tumor biology and therapeutic responses. -
Ligands for Target Protein for PROTAC
SMARCA-BD ligand 1 for PROTAC dihydrochloride is a selective ligand targeting the BAF ATPase subunit SMARCA2. This compound facilitates the proteolytic degradation of SMARCA2 through the PROTAC mechanism, thereby modulating its biological activity. It is utilized in research applications focused on the regulation of chromatin remodeling and exploring therapeutic avenues for diseases associated with altered SMARCA2 function. -
SMARCA2 Ligand
SMARCA2 ligand-11 is a specific ligand for the chromatin remodeling factor SMARCA2, facilitating the development of PROTACs such as SMARCA2 degrader-32. This compound is instrumental in research applications focused on targeted protein degradation, particularly in studies aimed at elucidating the role of SMARCA2 in various biological processes and diseases. Its ability to selectively engage with SMARCA2 allows for investigations into novel therapeutic strategies in cancer and other conditions where SMARCA2 activity is implicated. -
SMARCA2 Degrader
PROTAC SMARCA2 degrader-32 is a targeted protein degradation agent that selectively degrades SMARCA2 with a DC50 of 1.3 nM. This compound demonstrates significant inhibitory activity against lung cancer cell line NCI-H838, with a GI50 of 34 nM. Its application in research includes studies on the role of SMARCA2 in cancer biology and therapeutic strategies leveraging PROTAC technology for targeted degradation. -
SMARCA2 PROTAC Degrader
PROTAC SMARCA2 degrader-24 is a selective degrader targeting the SMARCA2 protein through a PROTAC mechanism. It exhibits potent biological activity with a DC50 value of less than 0.1 µM in HeLa cells, facilitating effective degradation of SMARCA2. Additionally, it demonstrates lower activity against SMARCA4, with a DC50 greater than 10 μM in the same cellular context. This compound serves as a valuable tool for studying the functional roles of SMARCA2 in various biological processes and disease models. -
SMARCA2 PROTAC Degrader
PROTAC SMARCA2 degrader-22 is a potent proteolysis-targeting chimera (PROTAC) specifically designed to degrade the SMARCA2 protein. It exhibits a degradation efficacy of 94% at a concentration of 100 nM. Additionally, PROTAC SMARCA2 degrader-22 demonstrates effective inhibition of A549 cell proliferation with an EC50 of less than 250 nM, making it a valuable tool for research into cancer biology and therapeutic applications targeting the chromatin remodeling complex. -
PROTAC SMARCA2 Degrader
PROTAC SMARCA2 Degrader-27 is a proteolysis-targeting chimera (PROTAC) that selectively degrades the SMARCA2 protein. By utilizing a VHL ligand, it engages the ubiquitin-proteasome system to induce targeted degradation of SMARCA2, demonstrating significant potential for research in cancer biology. This compound allows for the investigation of SMARCA2's role in oncogenesis and therapeutic resistance, contributing to the development of novel cancer treatments. -
SMARCA2 PROTAC Degrader
PROTAC A515 is a targeted protein degradation agent that selectively degradas the SMARCA2 protein. By promoting the ubiquitination of SMARCA2, it facilitates its subsequent degradation via the proteasome pathway. This compound is valuable for cancer research, allowing for the investigation of SMARCA2's role in tumorigenesis and potential therapeutic applications. -
WEE1 Kinase Molecular Glue Degrader
BMS-986463 is a WEE1 kinase molecular glue degrader that functions as a CRBN E3 ligase modulator (CELMoD). It significantly inhibits tumor growth while reducing phospho-CDK2 levels, making it a valuable tool in cancer research. This compound is particularly relevant for studies focusing on advanced malignant solid tumors, including non-small cell lung cancer (NSCLC). -
Molecular Glue Degrader
WEE1 Degrader 1 is a CRBN-dependent molecular glue degrader that targets WEE1 and casein kinase 1α (CK1α) with sub-2 nM DC50 values for both proteins. This compound effectively induces the proteasomal degradation of its targets, providing a valuable tool for studying cell cycle regulation. WEE1 Degrader 1 is particularly relevant in the research of acute lymphoblastic leukemia, acute monocytic leukemia, acute promyelocytic leukemia, colorectal adenocarcinoma, and diffuse large B-cell lymphoma. -
SALL4/OSR1 Dual Molecular Glue Degrader
HRZ-01-082-5 is a dual-functional molecular glue degrader targeting SALL4 and OSR1, exhibiting a DC50 of 4.8 nM for OSR1. This compound effectively induces the degradation of both SALL4 and OSR1 via the CRBN mechanism. HRZ-01-082-5 is applicable in the study of heart and urogenital development as well as in cancer research, providing valuable insights into these critical biological processes. -
NEK7 Molecular Glue Degrader
NEK7 degrader-3 is an orally active NEK7 molecular glue degrader with a DC50 of 33.1 nM, which effectively mediates the interaction between NEK7 and the E3 ligase cereblon, leading to the proteasomal degradation of NEK7. This degradation process attenuates NLRP3 inflammasome-mediated inflammatory responses, resulting in the inhibition of caspase-1 activity and the release of pro-inflammatory cytokines IL-1β, IL-1α, and IL-18. NEK7 degrader-3 demonstrates significant anti-inflammatory effects in LPS-induced neuroinflammation mouse models, serving as a valuable tool for research focused on neuroinflammation. -
Molecular Glue
ABT-002 is a molecular glue degrader that targets GSPT1 and NEK7, enhancing the ubiquitin-proteasome system's ability to degrade these proteins. This compound is the active metabolite of ABS-752 and demonstrates potential in the research of hepatocellular carcinoma (HCC). Its unique mechanism of action makes it a valuable tool for elucidating cellular pathways and therapeutic strategies in cancer biology. -
GSPT1/NEK7 Degrader
ABS-752 is a potent molecular glue degrader targeting GSPT1 and NEK7. It demonstrates significant cytotoxicity by reducing the protein levels of both GSPT1 and SALL4, along with NEK7. As a prodrug, ABS-752 is activated by monoamine oxidase, VAP-1, into an aldehyde intermediate and further converted to its active form, ABT-002. This compound has promising applications for research into hepatocellular carcinoma. -
GSPT1 Molecular Glue
ABS-752 hydrochloride is a prodrug that targets GSPT1 through CRBN modulation, functioning as a molecular glue. It effectively degrades GSPT1 and NEK7, without forming ternary complexes with CRBN and neosubstrates. The compound is activated by the enzyme VAP-1, converting it into an aldehyde intermediate and subsequently yielding the active molecule, ABT-002. ABS-752 is utilized in research focused on hepatocellular carcinoma (HCC) and related therapeutic pathways. -
STING Molecular Glue
NVS-STG2 is a molecular glue that targets the STING receptor by binding to the interstitial regions of adjacent STING dimers, thereby enhancing STING signaling. This compound promotes the activity of cGAMP, leading to the formation of larger and more stable oligomers, which amplifies the immune response. NVS-STG2 has demonstrated significant antitumor effects in preclinical animal models, making it a valuable tool for cancer immunotherapy research. -
STING PROTAC Degrader
PROTAC STING degrader-3 is a potent STING PROTAC degrader that operates through the ubiquitin-proteasome pathway, exhibiting a DC50 of 0.62 μM. This compound facilitates STING degradation, resulting in the inhibition of STING/TBK1/NF-κB signaling, thereby exerting notable anti-inflammatory effects. Additionally, PROTAC STING degrader-3 demonstrates renal protective properties and serves as a valuable tool for investigating acute kidney injury (AKI). -
PROTAC STING Degrader
PROTAC STING Degrader-2 is a targeted protein degrader that specifically induces the degradation of the Stimulator of Interferon Genes (STING) through a covalent interaction with STING and an E3 ubiquitin ligase. With a DC50 value of 0.53 μM, this compound facilitates the study of STING's biological functions, particularly in the context of autoinflammatory and autoimmune diseases. This reagent is instrumental for researchers exploring the therapeutic potential and role of STING in immune regulation. -
cGAS PROTAC Degrader
PROTAC cGAS degrader-1 is a selective degrader targeting cGAS through a proteolysis-targeting chimera (PROTAC) mechanism. It effectively induces proteasome-mediated degradation of cGAS, leading to the inhibition of the cGAS signaling pathway and a reduction in double-stranded DNA-induced cGAS activation in both human and mouse cell models. This compound is particularly relevant for research applications in inflammatory diseases such as ulcerative colitis. -
IRF5/8 Molecular Glue Degrader
EN1033 is a covalent molecular glue degrader targeting immune regulatory transcription factors IRF5 and IRF8. It induces proteasome-dependent degradation of IRF5 and demonstrates a more rapid and robust degradation of IRF8. By covalently modifying specific residues, EN1033 destabilizes these factors, leading to a reduction in their pro-inflammatory transcriptional activity. This reagent is valuable for exploring mechanisms in autoimmune and inflammatory disorders. -
IKZF2 degrader
NVP-DKY709 is an orally active molecular glue degrader targeting IKZF2. This compound demonstrates a Dmax of 53% and a DC50 of 4 nM, indicating potent degradation efficacy. Additionally, NVP-DKY709 can also degrade IKZF4 and SALL4 with DC50 values of 13 nM and 2 nM, respectively. Its mechanism involves binding to CRBN, altering its conformation to facilitate the recruitment and degradation of IKZF2, thereby exerting significant anti-tumor activity. This functionality positions NVP-DKY709 as a valuable tool in cancer research and therapeutic development targeting IKZF protein family members. -
PROTAC IKZF1/3 Degrader
Cemsidomide is a PROTAC degrader targeting IKZF1 and IKZF3, utilizing the ubiquitin ligase pathway. It exhibits potent biological activity with a GI50 of 0.05 nM against NCIH929.1 cells. This compound is primarily employed in the exploration of multiple myeloma (MM) research, facilitating the study of targeted protein degradation in cancer therapeutics. -
IKZF2 Molecular Glue Degrader
PLX-4545 is an orally active and selective molecular glue degrader that targets IKZF2 (zinc finger transcription factor Helios) via cereblon. This compound reprograms immunosuppressive regulatory T cells into pro-inflammatory effector T cells, thereby enhancing anti-tumor immune responses. PLX-4545 is intended for research applications related to solid tumors and the modulation of T cell functionality. -
IKZF2 Molecular Glue Degrader
(S,S)-PLX-4545 is a cereblon-based molecular glue degrader targeting IKZF2, a zinc finger transcription factor involved in immune regulation. This compound effectively promotes the degradation of IKZF2, making it a valuable tool for investigating IKZF2-related diseases, including various proliferative disorders and cancers. Researchers can leverage (S,S)-PLX-4545 to explore therapeutic strategies targeting IKZF2 functionality in different biological contexts. -
Enantiomer Of PLX-4545
(1S,2S,3R)-PLX-4545 is the (1S,2S,3R) enantiomer of PLX-4545, functioning as a selective cereblon-based molecular glue degrader that targets IKZF2 (zinc finger transcription factor Helios). This compound effectively reprograms immunosuppressive regulatory T cells into pro-inflammatory effector T cells, enhancing anti-tumor immune responses. Its applications extend to immunology and cancer research, providing insights into T cell modulation and potential therapeutic strategies for cancer immunotherapy. -
IKZF2 Selective and orally Inhibitor
PVTX-405 is a selective, orally bioavailable inhibitor targeting IKZF2, designed as a molecular glue degrader. With a DC50 of 0.7 nM and a Dmax of 91%, it enhances degradation efficiency while minimizing off-target effects, exhibiting an IC50 of 48 µM for hERG inhibition. PVTX-405 demonstrates significant antitumor activity by inhibiting the growth of MC38 tumors and shows improved efficacy when combined with immune checkpoint therapies, such as anti-PD1 or anti-LAG3, in mouse models. -
Molecular Glue IKZF2-Degrader
IKZF2-degrader 3 is a molecular glue that selectively targets and degrades the IKZF2 protein, exhibiting a DC50 of 2.0 nM. It enhances the understanding of IKZF2's role in various biological processes and is useful for studying its implications in hematological malignancies. This reagent is valuable for research focused on targeted protein degradation and its therapeutic potential in cancer treatment. -
IKZF1 Degrader
IKZF1-degrader-2 is a molecular glue degrader that specifically targets IKZF1, facilitating its degradation in cancer cells. This compound exhibits potent anticancer activity while demonstrating low toxicity, making it a valuable tool for oncology research. IKZF1-degrader-2 is ideal for studies focused on targeted protein degradation and its therapeutic implications in cancer treatment. -
IKZF2 Degrader
IKZF2-degrader 2 is a selective molecular glue degrader that targets IKZF2, facilitating its ubiquitination and subsequent degradation through recruitment of the CRL4-CRBN E3 ubiquitin ligase. With DC50 values of 0.5 nM and 1.8 nM in HiBit and FACS assays, respectively, this compound also induces moderate degradation of SALL4 (DC50 of 9 nM) without significantly affecting IKZF1, IKZF3, CK1α, or GSPT1. IKZF2-degrader 2 is suitable for investigating mechanisms in cancer immunology. -
IKZF2 Molecular Glue Degrader
IKZF2-degrader 1 is a selective IKZF2 molecular glue degrader that exhibits a DC50 of 0.5 nM, effectively targeting IKZF2 for degradation. With minimal activity against CK1α (DC50: 210 nM), it provides a focused approach for studying the role of IKZF2 in cellular processes. This compound is valuable for researching IKZF2-dependent cancers, enabling investigations into its therapeutic potential and biological mechanisms. -
IKZF2 Degrader
IKZF2-degrader 4 is an IKZF2-targeting compound that facilitates the degradation of the IKZF2 protein. Through its mechanism, this degrader can disrupt the function of IKZF2, which is implicated in various cancer pathways. It is a valuable tool for investigating IKZF2's role in tumor biology and for exploring therapeutic strategies in cancer research.
