Catalog No.
Product Name
Application
Product Information
Citations
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PROTAC BRD4 Degrader
(S)-GNE-987 is a selective PROTAC BRD4 degrader that functions by abrogating binding to von Hippel-Lindau while maintaining specific interactions with BRD4 bromodomains. With IC50 values of 4 nM for BD1 and 3.9 nM for BD2, (S)-GNE-987 facilitates targeted degradation of BRD4, making it a valuable tool in research focused on epigenetic regulation and cancer therapy. Additionally, it can be instrumental in the design of PROTAC-Antibody Conjugates (PAC) for enhanced therapeutic applications. -
SMARCA2/4 PROTAC Degrader
PROTAC SMARCA2/4-degrader-4 (Compound I-434) is a targeted PROTAC degrader that specifically promotes the degradation of the catalytic subunits SMARCA2 and SMARCA4 of the SWI/SNF complex. It demonstrates robust biological activity, achieving degradation of SMARCA2 and SMARCA4 in MV411 and A549 cell lines with DC50 values below 100 nM. This compound is valuable for research applications focused on the modulation of chromatin remodeling processes and the elucidation of the roles of SMARCA proteins in cancer biology. -
BRD9 PROTAC Degrader
dBRD9 dihydrochloride is a selective degrader of BRD9, targeting the protein for degradation through the PROTAC mechanism. This compound demonstrates efficacy in inhibiting the proliferation of acute myeloid leukemia (AML) cell lines, making it a valuable tool for research in cancer biology and therapeutic development. Its utility in studying BRD9's role in oncogenic processes positions dBRD9 dihydrochloride as a significant reagent for investigators exploring targeted protein degradation strategies. -
SMARCA2/4 PROTAC Degrader
PROTAC SMARCA2/4-degrader-27 is a PROTAC-based degrader that specifically targets the SMARCA2 and SMARCA4 proteins. This compound induces targeted protein degradation, facilitating the selective modulation of these chromatin remodelers. It is essential for research applications exploring the roles of SMARCA2 and SMARCA4 in cancer and other diseases, allowing for valuable insights into epigenetic regulation and therapeutic strategies. -
PROTAC SMARCA2 Degrader
PROTAC SMARCA2 degrader-30 is an investigative PROTAC designed for targeted degradation of SMARCA2 protein. It demonstrates potent biological activity with a DC50 of less than 100 nM in H1299 cells, making it a valuable tool for research in cancer biology and therapeutic development. This compound may facilitate studies on the role of SMARCA2 in cellular processes and its potential as a therapeutic target in oncogenic pathways. -
PROTAC BRD4 Degrader
PROTAC BRD4 Degrader-3 is a targeted protein degradation compound that operates through the recruitment of von Hippel-Lindau (VHL) ligands to promote the ubiquitination and subsequent proteasomal degradation of the BRD4 protein. This compound demonstrates significant efficacy in downregulating BRD4, a key regulator in various cancers and inflammatory diseases. Research applications for PROTAC BRD4 Degrader-3 include the investigation of therapeutic strategies for cancer treatment and exploring the role of BRD4 in gene expression and signaling pathways. -
SMARCA2/4 PROTAC Degrader
PROTAC SMARCA2/4-degrader-5 is a PROTAC degrader targeting the catalytic subunits SMARCA2 and SMARCA4 of the SWI/SNF complex. It effectively degrades SMARCA2 in MV411 and A549 cell lines with a DC50 of less than 100 nM, and targets SMARCA4 in MV411 with a DC50 ranging from 100 to 500 nM. This compound is instrumental for research applications focused on epigenetic regulation and oncogenic pathways involving SWI/SNF complex alterations. -
MLLT1 PROTAC Degrader
PROTAC MLLT1 Degrader-1 is a targeted PROTAC degrader that specifically interacts with MLLT1. This compound effectively inhibits proliferation and viability of acute myeloid leukemia (AML) cells, while also suppressing tumor growth in human AML xenograft models. PROTAC MLLT1 Degrader-1 can be utilized for research focused on MLL-rearranged AML, enabling studies on its oncogene transcriptional regulation and potential therapeutic applications. -
BRD4 PROTAC Degrader
NEP108 is a GID4 E3 ligase-based PROTAC degrader specifically targeting BRD4. With a DC50 value of approximately 3.8 μM, NEP108 demonstrates a strong affinity for GID4, exhibiting a KD value of 0.22 μM, while the KD value for its trimeric complex is 2.85 μM. This compound is suitable for research applications in cancer biology, facilitating the study of BRD4 degradation and its implications in therapeutic strategies. -
PROTAC BRD4 Degrader
PROTAC BRD4 Degrader-22 is a PROTAC-based degrader targeting the bromodomain-containing protein 4 (BRD4). This compound demonstrates significant biological activity with a pDC50 value of 9.2 in MOLT4 cells after 24 hours of treatment. It is primarily utilized in research applications focused on exploring the therapeutic potential of targeted protein degradation in various cancers and other BRD4-related disorders. -
SMARCA2/4 Degrader
PROTAC SMARCA2/4-degrader-30 is a targeted protein degradation agent specifically designed to degrade the catalytic subunits of the SWI/SNF complex, SMARCA2 and SMARCA4. This compound demonstrates effective degradation of SMARCA2 in A549 cells and SMARCA4 in MV411 cells, with a DC50 of less than 100 nM for both targets. It serves as a valuable tool for investigating the biological roles of SMARCA2 and SMARCA4 in various cancer models and for exploring potential therapeutic strategies in malignant conditions involving these proteins. -
BRD4 PROTAC Degrader
PROTAC BRD4 Degrader-35 is a PROTAC degrader specifically designed to target BRD4. This compound facilitates the ubiquitination and subsequent degradation of BRD4, making it a valuable tool in anti-cancer research. Its mechanism of action enables the modulation of BRD4-dependent pathways, providing insights into the therapeutic potential of BRD4 inhibition in various malignancies. -
SMARCA2 PROTAC Degrader
PROTAC SMARCA2/4-degrader-8 is a specialized PROTAC targeting the catalytic subunit SMARCA2 of the SWI/SNF complex. This compound effectively degrades SMARCA2 with a DC50 of less than 100 nM in A549 cells, while also targeting SMARCA4 with equivalent efficiency in MV411 cells. It serves as a valuable tool in research focused on understanding the roles of these proteins in chromatin remodeling and their implications in various cancer types. -
SMARCA2 PROTAC Degrader
PROTAC SMARCA2 degrader-5 is a potent degrader specifically designed to target the catalytic subunit SMARCA2 of the SWI/SNF chromatin remodeling complex. This compound effectively induces degradation of SMARCA2 in MV411 and A549 cell lines, demonstrating a DC50 of less than 100 nM, while also degrading SMARCA4 with a DC50 between 100-500 nM. This reagent is essential for researchers investigating the functional role of SMARCA2 and its associated pathways in cancer biology and other cellular processes. -
PROTAC BRD9 Degrader
(S,R)-CFT8634 is a selective PROTAC-class degrader targeting BRD9, designed for oral administration. This compound facilitates the ubiquitination and subsequent degradation of BRD9, which is implicated in various diseases characterized by abnormal cell proliferation. The structure comprises a BRD9 ligand, a CRBN ligase ligand, and a PROTAC linker, enabling effective recruitment of the E3 ligase for degradation. (S,R)-CFT8634 is a valuable tool for investigating BRD9-related biological processes and therapeutic strategies. -
Ligands for Target Protein for PROTAC Chemical
PROTAC BRD4 ligand-2 is a specific ligand for the BRD4 protein, designed for use in PROTAC-mediated degradation strategies. This compound facilitates the targeted degradation of BRD4, a key regulator of transcription and associated with various cancers, by recruiting the E3 ubiquitin ligase. It is instrumental in research applications aimed at understanding BRD4's role in oncogenesis and therapeutic development in cancer treatments. -
BRD4 PROTAC Degrader
PROTAC BRD4 Degrader-34 is a selective degrader that targets the bromodomain-containing protein 4 (BRD4) through a proteolysis-targeting chimera (PROTAC) mechanism. It induces the degradation of the BRD4-BD2 domain via the VHL E3 ubiquitin ligase system. This compound has significant potential for use in cancer research, enabling investigations into the therapeutic effects of targeting BRD4 in oncogenic pathways. -
SMARCA2/4 PROTAC degrader
PROTAC SMARCA2/4 degrader-37 is a proteolysis-targeting chimera (PROTAC) that selectively degrades SMARCA2 and SMARCA4 proteins. It exhibits a potent inhibitory concentration (IC50) of ≤0.1 μM, highlighting its efficacy in disrupting these bromodomain-containing proteins. This reagent is suitable for applications in cancer research and therapeutic development, particularly in studies involving epigenetic modulation and chromatin remodeling. -
SMARCA2/4 Ligand
SMARCA2/4-ligand-5 is a selective ligand targeting the SMARCA2 and SMARCA4 proteins, functioning as a crucial component in the PROTAC SMARCA2/4 degrader-37. This compound demonstrates potent biological activity, achieving an IC50 of ≤0.1 μM, making it suitable for applications in targeted protein degradation studies. Research utilizing SMARCA2/4-ligand-5 contributes to understanding the roles of these chromatin remodelers in various biological processes and cancer biology. -
RAF Molecular Glue
NST-628 is a molecular glue targeting RAF within the MAPK signaling pathway. It disrupts RAF phosphorylation and MEK activation by preventing the formation of BRAF-CRAF and BRAF-ARAF heterodimers. NST-628 exhibits significant biological activity in inhibiting RAS- and RAF-driven cancers, particularly in tumors with mutant KRAS, NRAS, BRAF class II/III, and NF1 mutations. This compound is a valuable tool for research into targeted cancer therapies and understanding the RAS-MAPK pathway's role in oncogenesis. -
PROTAC BRAF-V600E Degrader
PROTAC BRAF-V600E Degrader-2 is a highly selective degrader targeting the BRAF-V600E mutant, with dissociation constants (Kd) of 14.4 nM and 9.5 nM for BRAF and BRAF-V600E, respectively. This compound effectively induces degradation of the BRAF-V600E kinase domain without impacting wild-type BRAF. Its potent biological activity makes it a valuable tool for research applications focused on melanoma cell growth inhibition and the study of BRAF-related signaling pathways. -
Ligand of BRAF
BRAF ligand-1 acts as a specific ligand for the BRAF protein, playing a crucial role in the regulation of cell signaling pathways associated with cell proliferation, survival, and differentiation. This compound is important for studying the BRAF signaling pathway and its implications in various cancers. Additionally, BRAF ligand-1 can be utilized in the synthesis of CST905, further enhancing its utility in biochemical research and drug discovery efforts targeting mutant BRAF. -
pan-KRAS PROTAC Degrader
MCB-36 is a VHL-recruiting pan-KRAS PROTAC degrader that targets various KRAS mutants, including G12D, G12C, G12V, and wild-type forms, with an exceptionally high binding affinity (Kd ≈ 1 pM). This compound effectively lowers p-ERK levels, promoting apoptosis in KRAS-driven cancer cells while showing minimal impact on HRAS and NRAS protein levels. MCB-36 is particularly useful for investigating colorectal and lung cancers, as it demonstrates efficacy against KRASG12C inhibitor-resistant tumors and aids in remodeling the tumor immune microenvironment. -
PROTAC Linker
N-(Azido-PEG3)-N-Fluorescein-PEG3-acid is a PEG-based linker utilized in PROTAC technology, featuring azide, fluorescein, and carboxylic acid functionalities. This compound serves as a versatile click chemistry reagent capable of participating in copper-catalyzed azide-alkyne cycloaddition (CuAAc) with alkyne-containing partners, as well as strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with DBCO or BCN groups. Its unique properties make it suitable for applications in tandem with targeted protein degradation and fluorescent labeling studies in chemical biology. -
PROTAC Linker
Biotin-PEG-azide (MW 1000) is a PEG-based linker designed for PROTAC synthesis, featuring an azide functional group. This versatile compound can participate in copper-catalyzed azide-alkyne cycloaddition (CuAAC) reactions with alkyne-containing molecules, as well as in strain-promoted alkyne-azide cycloaddition (SPAAC) with DBCO or BCN functionalized compounds. Its unique properties make it suitable for applications in targeted protein degradation research and other areas of chemical biology. -
PROTAC Linkers
DBCO-NHCO-PEG12-biotin is a PEG-based PROTAC linker that facilitates the synthesis of PROTACs through its reactive DBCO moiety. This compound engages in strain-promoted alkyne-azide cycloaddition (SPAAC) with azide-bearing molecules, allowing for precise conjugation in chemical biology applications. Its utility in targeted protein degradation research makes it a valuable tool for biochemists developing innovative therapeutic strategies. -
PROTAC Linkers
Carboxyfluorescein-PEG12-NHS is a PEG-based PROTAC linker designed for the synthesis of proteolysis-targeting chimeras (PROTACs). It enables the formation of covalent bonds with target proteins, facilitating the selective degradation of unwanted intracellular proteins. This reagent is valuable for researchers exploring targeted protein degradation and developing novel therapeutics in cancer and other diseases. -
PROTAC Linker
(Rac)-Biotin-PEG3-oxyamine hydrochloride is a PEG-based linker specifically designed for the development of PROTAC (Proteolysis Targeting Chimera) molecules. This compound facilitates the conjugation of biotin to target proteins, enhancing their degradation via the ubiquitin-proteasome pathway. It is valuable in research applications focused on targeted protein degradation and the study of protein-protein interactions. -
Ligands for E3 Ligase
(Rac)-Spirotetramat-enol serves as a ligand for E3 ligases, demonstrating significant potential in targeted protein degradation research. Primarily involved in the modulation of acetyl-CoA carboxylase, this compound facilitates the synthesis of PROTAC ADC degraders. Its application in the development of innovative therapeutic strategies underscores its importance in chemical biology and drug discovery. -
DHFR-TS PROTAC Degrader
BION106 is a dihydrofolate reductase-thymidylate synthase (DHFR-TS) PROTAC degrader that effectively targets and degrades DHFR-TS. It demonstrates potent antimalarial activity against Plasmodium falciparum, with a Ki value of 2.68 nM and selective toxicity of 0.2 μM in parasite cells, while showing significantly reduced toxicity (>100 μM and 44.2 μM) in mammalian cells. BION106 is valuable for research on antimalarial therapies and the mechanisms underlying parasite survival. -
PROTAC DHFR Degrader
PROTAC DHFR Degrader-1 is a selective PROTAC degrader that targets the dihydrofolate reductase-thymidylate synthase (DHFR-TS) complex of Plasmodium falciparum, exhibiting a Ki of 2.01 nM. This compound specifically degrades the parasite's DHFR without affecting human DHFR, effectively inhibiting the growth of Plasmodium falciparum. PROTAC DHFR Degrader-1 is suitable for research focused on malaria and the molecular mechanisms related to Plasmodium falciparum. -
TEAD PROTAC Degrader
KG-FP-003 is a potent and selective TEAD PROTAC degrader, demonstrating DC50 values of 6 ± 4 nM for TEAD1, 68 ± 15 nM for TEAD2, 12 ± 5 nM for TEAD3, and 7 ± 5 nM for TEAD4. This compound effectively induces ubiquitination and degradation of TEAD proteins. KG-FP-003 has demonstrated significant anticancer activity against mesothelioma and ovarian cancer, making it a valuable tool for research in cancer biology and therapeutic development targeting TEAD pathways. -
PROTAC TEAD Degrader
PROTAC TEAD degrader-1 is a targeted molecular degrader that selectively promotes the degradation of transcriptional enhanced associate domain (TEAD) proteins via a ubiquitin-proteasome pathway. With a DC50 value of 54.1 nM in 293T cells, it effectively inhibits cell proliferation in NF2-deficient NCI-H226 cells with an IC50 of 0.21 μM. This compound also modulates the expression of yes-associated protein (YAP) target genes, making it a valuable tool for investigating TEAD-related signaling pathways and their implications in various biological processes. -
TEAD1 PROTAC Degrader
PROTAC TEAD degrader-2 is a potent degrader designed to target TEAD1 through the proteolysis-targeting chimera (PROTAC) approach. It effectively disrupts the YAP/TAZ-TEAD interaction, exhibiting a low DC50 of 0.6 nM and an IC50 of 1.8 nM. This compound demonstrates strong selective inhibitory activity against YAP-dependent cancer cell lines and significantly reduces transcriptional activity associated with YAP. PROTAC TEAD degrader-2 serves as a valuable tool for investigating the role of TEAD1 in mesothelioma and glioma research. -
PROTAC GSK-3β Degrader
PROTAC GSK-3β Degrader-1 is a targeted GSK-3β degrader that induces the proteasomal degradation of GSK-3β with an IC50 value of 833 nM. This compound integrates SB-216763, a known GSK-3β inhibitor, a PEG linker, and a CRBN ligand to facilitate E3 ligase-mediated degradation. It has demonstrated efficacy in reducing neurotoxicity induced by Aβ25-35 peptide and CuSO4, making it a valuable tool for researching Alzheimer's disease mechanisms and potential therapeutic interventions. -
GSK3α/GSK3β PROTAC Degrader
PT-65 is a PROTAC degrader targeting GSK3α and GSK3β, exhibiting DC50 values of 28.3 nM and 34.2 nM, respectively. This compound effectively inhibits excessive tau phosphorylation induced by GSK3β, amyloid-beta, and okadaic acid. PT-65 is a valuable tool for research into the pathophysiology of Alzheimer's disease, allowing for further investigation into tau-related mechanisms and potential therapeutic interventions. -
PROTAC Linkers
Fmoc-NH-PEG5-CH2COOH is a cleavable linker specifically designed for use in antibody-drug conjugates (ADCs) and as a PEG-based link in the synthesis of PROTACs. This compound facilitates the efficient conjugation of therapeutic agents to antibodies, enhancing targeted delivery. Its unique structure allows for controlled release, making it valuable in the development of innovative therapeutic strategies in drug discovery and bioconjugation research. -
ADC/PROTAC Linker
DBCO-NHCO-PEG4-NH-Boc is a versatile PROTAC linker featuring a cleavable structure designed for the synthesis of PROTACs and antibody-drug conjugates (ADCs). This compound utilizes a DBCO moiety, enabling efficient strain-promoted alkyne-azide cycloaddition (SPAAC) with azide-containing molecules. Its PEG4 spacer enhances solubility and stability, making it suitable for various biological applications in drug development and therapeutic research. -
ADC/PROTAC Linker
DBCO-NHCO-PEG4-amine is a PEG-based linker designed for use in antibody-drug conjugates (ADCs) and PROTACs. This cleavable linker facilitates the conjugation of payloads such as MMAE to antibodies, enhancing targeted delivery to cancer cells. It has demonstrated compelling biological activities, with EC50 values of 280 nM and 22 nM for DBCO-VCpAB MMAE and DBCO-TRX MMAE, respectively, in SKBR3 cells, making it a valuable tool for researchers investigating targeted therapies. -
ADC/PROTAC Linker
Tr-PEG3-OH is a non-cleavable linker comprised of a three-unit polyethylene glycol (PEG) chain, designed for use in the synthesis of antibody-drug conjugates (ADCs). This compound enhances the solubility and stability of ADCs, facilitating targeted delivery of cytotoxic agents to specific cells. Its applications extend to PROTAC (proteolysis-targeting chimera) technology, enabling the development of innovative therapies that harness targeted protein degradation. -
ADC/PROTAC Linker
Propargyl-PEG7-acid is a PEG-based linker designed for use in antibody-drug conjugates (ADCs) and proteolysis-targeting chimeras (PROTACs). It features a propargylic group that facilitates copper-catalyzed azide-alkyne cycloaddition (CuAAc), enabling effective conjugation to azide-containing molecules. This compound serves as a cleavable linker, providing versatility in drug delivery systems and targeted therapy research. Propargyl-PEG7-acid is essential for studies focusing on the development of innovative therapeutic modalities through advanced chemical synthesis techniques. -
PROTAC Linkers
DBCO-N-bis(PEG4-NHS ester) is a bifunctional polyethylene glycol (PEG) linker featuring two NHS ester groups and a dibenzocyclooctyne (DBCO) moiety. This reagent facilitates protein modification and labeling, enhancing bioconjugation applications. As a click chemistry tool, DBCO-N-bis(PEG4-NHS ester) enables efficient strain-promoted alkyne-azide cycloaddition (SPAAC) with azide-containing molecules, making it valuable for constructing PROTAC molecules and other bioorthogonal conjugates in various biochemical research settings. -
ADC/PROTAC Linker
Azido-PEG4-Val-Cit-PAB-OH is a cleavable polyethylene glycol (PEG) linker designed for use in antibody-drug conjugates (ADCs) and proteolysis-targeting chimeras (PROTACs). This compound features an azide group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) with alkyne-containing molecules, as well as strain-promoted alkyne-azide cycloaddition (SPAAC) with DBCO or BCN moieties. Its versatility as a click chemistry reagent supports diverse applications in chemical biology and drug development. -
PROTAC Linkers
m-PEG11-acid is a non-cleavable linker composed of 11 ethylene glycol units, functioning as a versatile agent in the synthesis of antibody-drug conjugates (ADCs) and PROTACs. This polyethylene glycol (PEG)-based linker enhances the solubility and pharmacokinetics of the conjugates while facilitating targeted degradation of proteins in research applications. m-PEG11-acid is crucial for investigating the mechanisms of protein regulation and therapeutic strategies in drug discovery. -
ADC/PROTAC Linker
m-PEG4-MS is a polyethylene glycol (PEG)-based linker designed for use in the synthesis of PROTACs and antibody-drug conjugates (ADCs). This cleavable linker facilitates the precise delivery of therapeutic agents, enhancing the stability and efficacy of the resulting compounds. Its application in PROTAC development and ADC formulation supports research into targeted protein degradation and innovative cancer therapies. -
ADC/PROTAC Linker
m-PEG7-Amine is a polyethylene glycol (PEG)-based linker designed for use in PROTAC (Proteolysis Targeting Chimeras) and antibody-drug conjugate (ADC) synthesis. This cleavable linker facilitates the targeted degradation of specific proteins, enhancing the efficacy of PROTACs. Its versatile application makes it an essential component in developing therapeutic modalities aimed at selective protein modulation and cancer treatment. -
PROTAC Linkers
m-PEG10-alcohol is a non-cleavable linker comprised of a decaethylene glycol unit, primarily used in the design of antibody-drug conjugates (ADCs). This PEG-based compound serves as a versatile PROTAC linker, facilitating the development of proteolysis-targeting chimeras. Its structure enhances solubility and stability, making it suitable for various chemical biology applications, including targeted protein degradation studies. -
PROTAC Linkers
(2R,4R)-4-Hydroxypyrrolidine-2-carboxylic acid hydrochloride functions as a non-cleavable linker in the development of antibody-drug conjugates (ADCs). Furthermore, it serves as an alkyl chain-based PROTAC linker, facilitating the synthesis of PROTACs. This compound plays a crucial role in advancing targeted protein degradation research, contributing to the exploration of innovative therapeutic strategies. -
PROTAC Linker
PC Alkyne-PEG4-NHS ester is a cleavable linker designed for use in the synthesis of antibody-drug conjugates (ADCs). Functioning as a PROTAC linker, this reagent features an alkyne group and participates in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions. Its unique structure enhances the specificity and efficiency of conjugating azide-containing molecules, making it valuable for various chemical biology applications, including targeted drug delivery and proteolysis targeting chimera (PROTAC) development. -
PROTAC Linker
TCO-PEG4-DBCO is a versatile PROTAC linker known for its ability to facilitate the synthesis of proteolysis-targeting chimeras (PROTACs). This compound features a DBCO moiety that enables strain-promoted alkyne-azide cycloaddition (SPAAC) with azide-containing compounds, while the TCO component allows for inverse electron demand Diels-Alder (iEDDA) reactions with tetrazine derivatives. TCO-PEG4-DBCO finds applications in the development of antibody-drug conjugates (ADCs), enhancing the precision and efficacy of targeted therapeutics. Its unique chemical properties make it a valuable tool for researchers in chemical biology and drug development.
