Catalog No.
Product Name
Application
Product Information
Citations
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PROTAC/ADC Linker
Hydroxy-PEG4-acid is a non-cleavable linker featuring a four-unit polyethylene glycol (PEG) moiety, primarily utilized in the development of antibody-drug conjugates (ADCs). This linker is also applicable in the synthesis of PROTACs (proteolysis-targeting chimeras), facilitating targeted degradation of specific proteins. Its biocompatibility and structural versatility make it valuable in various chemical biology applications, particularly in therapeutic development and research focusing on targeted protein modulation. -
PROTAC Linkers
Propargyl-PEG2-NHBoc is a cleavable linker designed for use in the synthesis of PROTACs and antibody-drug conjugates (ADCs). This PEG-based linker features an alkyne group, allowing for efficient copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. Its unique properties support robust applications in drug development and targeted protein degradation research, making it a valuable tool for chemical biology studies. -
PROTAC Linker
Bis-PEG8-acid is a polyethylene glycol-based linker designed for use in PROTAC (Proteolysis Targeting Chimeras) synthesis. This bifunctional linker facilitates the formation of PROTACs by providing a cleavable connection between the target protein and an E3 ligase. Additionally, Bis-PEG8-acid serves as a linker in the development of antibody-drug conjugates (ADCs), enhancing their stability and efficacy. Its application in chemical biology and therapeutic research supports innovative approaches in targeted protein degradation and drug delivery systems. -
ADC/PROTAC Linker
Amino-PEG9-acid is a PEG-based linker designed for use in antibody-drug conjugates (ADCs) and PROTACs. This non-cleavable linker facilitates the synthesis of PROTACs and enhances the stability and efficacy of ADC formulations. Its unique properties make it a valuable tool in the development of targeted therapies for various diseases, enabling precise delivery of therapeutic agents to specific cellular targets. -
ADC/PROTAC Linker
Propargyl-PEG8-NHS ester is a PEG-based linker specifically designed for antibody-drug conjugates (ADCs) and PROTACs. Its primary mechanism involves enabling the synthesis of these bioconjugates through a cleavable linker. This compound features an alkyne group that facilitates click chemistry, specifically the copper-catalyzed azide-alkyne cycloaddition (CuAAc), allowing for efficient conjugation with azide-containing molecules. It is a valuable tool for researchers in drug development and bioconjugation studies. -
ADC/PROTAC Linker
Propargyl-PEG6-acid is a PEG-based linker primarily utilized in the synthesis of proteolysis-targeting chimeras (PROTACs) and antibody-drug conjugates (ADCs). This cleavable linker facilitates the formation of ADCs and enables targeted protein degradation via a click chemistry reaction, leveraging its alkyne group for copper-catalyzed azide-alkyne cycloaddition (CuAAc). Its versatile applications in chemical biology make it a valuable tool for research in targeted therapeutics and bioconjugation strategies. -
PROTAC Linker
Fmoc-NH-PEG9-CH2CH2COOH is a cleavable linker designed for use in the synthesis of antibody-drug conjugates (ADCs) and PROTACs. This PEG-based compound facilitates the conjugation of therapeutic agents to targeted antibodies, enhancing efficacy and selectivity in drug delivery. Its unique structure allows for the effective modulation of protein degradation pathways, making it valuable for research applications in targeted protein degradation and drug development. -
ADC/PROTAC Linker
Propargyl-PEG8-NH2 is a PEG-based linker primarily used in antibody-drug conjugates (ADCs) and PROTAC synthesis. This non-cleavable linker enhances the stability of ADCs while facilitating the targeted delivery of therapeutic agents. Additionally, its alkyne functional group allows for copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it a valuable tool in click chemistry applications for bioconjugation and drug development. -
PROTAC Linker
Bis-PEG9-acid is a PEG-based linker designed for use in the synthesis of PROTACs (Proteolysis Targeting Chimeras). This compound features a cleavable structure, making it suitable for the development of antibody-drug conjugates (ADCs). Its unique properties facilitate targeted degradation of proteins, enabling efficient research in drug discovery and therapeutic development. -
PROTAC Linkers
Azido-PEG4-CH2-Boc functions as a cleavable linker primarily utilized in the synthesis of antibody-drug conjugates (ADCs) and PROTACs. This versatile reagent incorporates a PEG spacer and an azide group, allowing it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) as well as strain-promoted alkyne-azide cycloaddition (SPAAC) reactions. Its effective application in the development of novel bioconjugates and protein degradation-based therapeutic strategies makes it a valuable tool in chemical biology and drug development research. -
PROTAC/ADC Linker
NH2-PEG5-OH is a PEG-based linker designed for use in the synthesis of proteolysis-targeting chimeras (PROTACs) and antibody-drug conjugates (ADCs). This non-cleavable linker, incorporating a five-unit polyethylene glycol (PEG) structure, enhances the stability and solubility of biologically active compounds. Researchers utilize NH2-PEG5-OH to facilitate targeted degradation of proteins or deliver cytotoxic agents via ADCs, improving therapeutic efficacy in various applications. -
PROTAC Linkers
N3-PEG3-CH2CH2-Boc is a cleavable linker designed for use in PROTAC synthesis, specifically serving as a 3-unit polyethylene glycol (PEG) intermediary. This compound facilitates the formation of antibody-drug conjugates (ADCs) and supports click chemistry applications through its azide group. It readily participates in copper-catalyzed azide-alkyne cycloaddition (CuAAc) with alkyne-functionalized molecules and can also engage in strain-promoted alkyne-azide cycloaddition (SPAAC) with DBCO or BCN groups, proving valuable in diverse chemical research applications. -
ADC/PROTAC Linker
Propargyl-PEG6-NHS ester is a cleavable linker designed for the synthesis of antibody-drug conjugates (ADCs) and PROTACs. This PEG-based reagent features an alkyne group that enables copper-catalyzed azide-alkyne cycloaddition (CuAAc), facilitating the conjugation of biomolecules. Its versatility as a click chemistry reagent enhances the development of targeted therapies in chemical biology and drug discovery applications. -
ADC/PROTAC Linker
Amino-PEG5-C2-acid is a PEG-based linker designed for use in the synthesis of PROTACs and non-cleavable antibody-drug conjugates (ADCs). This compound facilitates the conjugation of active pharmaceutical ingredients to antibodies, thereby enhancing target specificity and therapeutic efficacy. Its unique structure allows for optimal stability and performance in bioconjugation applications, making it a valuable tool for researchers in drug development and targeted therapy. -
PROTAC/ADC Linker
Amino-PEG4-CH2COOH is a PEG-based linker designed for use in the synthesis of proteolysis-targeting chimeras (PROTACs) and serves as a non-cleavable four-unit PEG linker for antibody-drug conjugates (ADCs). This compound facilitates the formation of stable conjugates, thereby enhancing the delivery of therapeutic agents to targeted cells. Its unique properties support research applications in targeted protein degradation and ADC development, contributing to advancements in cancer therapy and drug efficacy. -
PROTAC Linkers
NH-bis-PEG2 is a non-cleavable linker featuring a two-unit polyethylene glycol (PEG) structure, primarily utilized in the development of antibody-drug conjugates (ADCs). This PEG-based linker is also applicable in the synthesis of PROTACs, facilitating targeted protein degradation. Its chemical properties allow for improved solubility and stability, making it a valuable tool in drug development and biochemical research. -
ADC/PROTAC Linker
N-Boc-PEG7-alcohol is a PEG-based linker primarily utilized in the synthesis of PROTACs and antibody-drug conjugates (ADCs). This cleavable linker facilitates targeted drug delivery by enhancing the solubility and stability of therapeutic compounds. Its versatile applications in chemical biology make it a valuable tool for researchers aiming to develop novel targeted therapies. -
ADC/PROTAC Linker
m-PEG10-amine is a non-cleavable 10 unit polyethylene glycol (PEG) linker designed for use in the synthesis of antibody-drug conjugates (ADCs) and PROTACs (Proteolysis Targeting Chimeras). This linker enhances the solubility and stability of conjugated biomolecules, facilitating targeted delivery and improved therapeutic efficacy. It is particularly valuable in research applications focusing on ADC development and targeted protein degradation strategies. -
PROTAC Linkers
Propargyl-PEG4-Tos is a PEG-based linker specifically designed for the synthesis of PROTACs (proteolysis-targeting chimeras). It serves as a cleavable linker in antibody-drug conjugates (ADCs), facilitating targeted delivery of therapeutic agents. This compound features an alkyne group that enables copper-catalyzed azide-alkyne cycloaddition (CuAAc), allowing for efficient conjugation with azide-containing molecules. Its versatile applications make it a valuable tool in chemical biology and drug development research. -
ADC/PROTAC Linker
N-Boc-PEG6-alcohol is a PEG-based linker designed for antibody-drug conjugate (ADC) and PROTAC applications. This cleavable linker facilitates the synthesis of PROTACs, allowing for targeted degradation of specific proteins. Its unique structure provides enhanced solubility and stability, making it suitable for various biochemical studies focused on targeted therapies and protein regulation. -
PROTAC ATR Degrader
PROTAC ATR degrader-1 (compound ZS-7) is a potent degrader targeting ataxia telangiectasia and Rad3-related (ATR) proteins, demonstrated by a DC50 of 0.53 μM. This compound facilitates selective degradation of ATR, making it a valuable tool for cancer research and the study of DNA damage response pathways. Its application in cellular models aids in understanding the therapeutic potential of ATR inhibition in various malignancies. -
PROTAC ATR Degrader
Abd110 is a Lenalidomide-based PROTAC that targets and degrades ATR kinase. It selectively reduces levels of ATR and phospho-ATR while sparing related kinases such as ATM and DNA-PKcs. This compound is valuable for research applications focused on ATR-mediated pathways and innate cellular responses to DNA damage. -
Cyclin K Degrader
HQ461 is a molecular glue that facilitates the interaction between CDK12 and DDB1, leading to the targeted degradation of cyclin K. This degradation impairs CDK12 function, which in turn results in reduced phosphorylation of CDK12 substrates, downregulation of DNA damage response genes, and induces apoptosis in affected cells. HQ461 is a valuable tool for research applications focused on the modulation of cell cycle regulation and the DNA damage response pathway. -
CCND1/CDK4 PROTAC Degrader
CPD-39 is a potent heterobifunctional PROTAC degrader that targets CCND1 and CDK4. This compound effectively induces the degradation of these proteins, demonstrating significant anti-proliferative activity. CPD-39 is intended for research applications focusing on the modulation of cell cycle regulation and cancer therapeutics. -
CDK2 Molecular Glue Degrader
CDK2 degrader 6 is a potent CDK2 molecular glue degrader that functions through binding to cereblon and CDK2, leading to the ubiquitination and proteasomal degradation of CDK2. With a DC50 of 46.5 nM, it effectively modulates the cell cycle and reduces proliferation in breast cancer cells. Additionally, CDK2 degrader 6 demonstrates in vivo antitumor activity in gastric cancer mouse models, making it a valuable tool for research into breast and gastric cancers. -
Molecular Glue Degrader
dCeMM3 is a molecular glue degrader that facilitates the ubiquitination and subsequent degradation of cyclin K. By promoting the interaction of the CDK12-cyclin K complex with the CRL4B ligase complex, dCeMM3 plays a critical role in regulating cell cycle progression. This reagent is particularly useful for research applications focused on targeted protein degradation and the elucidation of CDK12-associated pathways. -
Molecular Glue Degrader
dCeMM2 is a molecular glue degrader that specifically targets cyclin K. It induces ubiquitination and subsequent degradation of cyclin K by facilitating the interaction between CDK12-cyclin K and the CRL4B ligase complex. This compound is valuable for studying the regulation of cell cycle and transcriptional processes, and it serves as a tool in research areas focusing on cancer biology and cell signaling pathways. -
CDK7 PROTAC Degrader
JWZ-5-13 is a potent CDK7 PROTAC degrader that selectively targets cyclin-dependent kinase 7 for ubiquitin-proteasome system-mediated degradation. It exhibits significant antiproliferative effects on various cancer cell lines, making it an essential tool for studying pathways involved in malignancies such as ovarian cancer, diffuse large B-cell lymphoma, acute T-lymphoblastic leukemia, and non-small cell lung cancer. This compound facilitates the exploration of targeted protein degradation in cancer biology, offering insights into therapeutic strategies. -
CDK2/CDK5 PROTAC Degrader
TMX-2172 is a selective bivalent PROTAC that targets CDK2 and CDK5, inducing their proteasomal degradation with IC50 values of 6.5 nM and 6.8 nM, respectively. This compound demonstrates notable selectivity for CDK2 and CDK5, while sparing other cyclin-dependent kinases such as CDK1, CDK4, CDK6, CDK7, and CDK9. TMX-2172 effectively inhibits the enzymatic activity of CDK2 and CDK5, leading to a reduction in ASCL1 protein levels, induction of cancer cell death, and antiproliferative effects. This reagent is applicable in research focused on ovarian cancer and small cell lung cancer. -
CDK12/7/9 Degrader
BSJ-5-63 is a potent PROTAC degrader targeting CDK12, CDK7, and CDK9. It effectively reduces protein expression levels of these kinases as well as RNAPII and Cyclin K, resulting in decreased mRNA expression of BRCA1 and BRCA2. This compound exhibits significant anticancer activity and is particularly relevant for research focused on prostate cancer. -
CDK12/CDK13 PROTAC Degrader
ZLC491 is a PROTAC degrader that selectively targets CDK12 and CDK13, utilizing cereblon- and proteasome-dependent mechanisms for degradation. This compound effectively inhibits the transcription and expression of long genes, particularly those involved in DNA damage response pathways. ZLC491 demonstrates anti-proliferative effects in various triple-negative breast cancer cell lines, making it a valuable tool for research into targeted therapies for this aggressive cancer subtype. -
PROTAC/CDK2 Degrader
CDK2 Degrader 2 is a potent PROTAC targeting cyclin-dependent kinase 2 (CDK2), facilitating its degradation in MKN1 cells with a DC50 value of less than 100 nM. This compound employs a novel design, integrating a ligand for the target protein along with a linker and a ligand for the E3 ligase cereblon (CRBN). CDK2 Degrader 2 is valuable for research applications focused on the regulation of cell cycle progression and the exploration of targeted protein degradation mechanisms. -
Molecular Glue Degrader
dCeMM4 is a molecular glue degrader that targets cyclin K by inducing its ubiquitination and subsequent degradation. It facilitates the interaction between CDK12-cyclin K and the CRL4B ligase complex, leading to effective protein degradation. This compound is useful for research applications investigating cell cycle regulation and the ubiquitin-proteasome system. -
PROTAC CDK9 Degrader
PROTAC CDK9 degrader-9 is a selective and potent degrader designed to target cyclin-dependent kinase 9 (CDK9) via PROTAC technology. This compound facilitates the targeted degradation of CDK9, thereby modulating transcriptional regulation and influencing cell proliferation. It is particularly useful in anti-cancer research, where the inhibition of CDK9 can lead to suppression of oncogenic pathways. -
PROTAC CDK9 degrader
PROTAC CDK9 degrader-2, a selective degrader of cyclin-dependent kinase 9 (CDK9), utilizes a PROTAC mechanism involving a natural product ligand, Wogonin, which targets the ubiquitin E3 ligase Cereblon (CRBN). With an IC50 of 17 μM in MCF-7 cell lines, this compound demonstrates potent activity in the degradation of CDK9, making it a valuable reagent for research applications focused on CDK9-related pathways in cancer biology and therapeutic development. -
CDK2 Degrader
(R)-CDK2 Degrader 6 is a cereblon-based molecular glue degrader specifically targeting cyclin-dependent kinase 2 (CDK2). It functions by inducing ubiquitination and subsequent proteasomal degradation of CDK2, with a DC50 value of 27 nM. This compound is suitable for cancer research applications, providing a valuable tool for studying CDK2-related pathways and therapeutic interventions. -
CDK2 Molecular Glue Degrader
(S)-CDK2 degrader 6 selectively targets cyclin-dependent kinase 2 (CDK2) as a molecular glue degrader. With a DC50 of 166.7 nM over 24 hours, this compound effectively promotes the degradation of CDK2, thereby modulating cell cycle progression. It holds significant potential for applications in breast cancer research, enabling the exploration of therapeutic strategies that involve the regulation of CDK2 activity. -
Ligands for Target Protein for PROTAC
FN-1501-propionic acid is a ligand targeting cyclin-dependent kinases 2 and 9 (CDK2/9), utilized in the development of PROTAC (proteolysis targeting chimeras) for targeted protein degradation. This compound can be combined with a CRBN ligand to facilitate the design of PROTAC-based CDK2/9 degraders, enabling selective degradation of these kinases. Its application in research enhances the study of cellular processes regulated by CDK2 and CDK9, making it a valuable tool for investigating therapeutic strategies against diseases associated with dysregulated kinase activity. -
CDK9 PROTAC Degrader
PROTAC CDK9 degrader-11 is an orally active PROTAC degrader that specifically targets CDK9, demonstrating a DC50 value of 1.09 nM. This compound shows cytotoxicity in various small cell lung cancer cell lines with an IC50 in the nanomolar range. PROTAC CDK9 degrader-11 effectively induces cell cycle arrest at the G0/G1 phase and reduces invasion in DMS114 and DMS53 cells. Additionally, it exhibits significant antitumor efficacy in NCI-H446 xenograft mouse models, making it a valuable tool for cancer research and therapeutic development. -
CDK4/6 PROTAC Degrader
CST651 is a selective proteolysis-targeting chimera (PROTAC) degrader specifically designed to target cyclin-dependent kinases CDK4 and CDK6. This compound effectively degrades CDK4 and CDK6 in MM.1S cells, exhibiting DC50 values of 20 nM and 5.1 nM, respectively. CST651 demonstrates the ability to inhibit cancer cell proliferation and migration, making it a valuable tool for research into various cancers, including acute lymphoblastic leukemia. -
PROTAC Degrader
PROTAC CDK2 Degrader-1 is a selective PROTAC degrader designed to target cyclin-dependent kinase 2 (CDK2). This compound effectively induces degradation of CDK2 and inhibits phosphorylation of the retinoblastoma (RB) protein in the CDK2-dependent OVCAR3 cell line, with an IC50 range of 100-500 nM. It serves as a valuable tool for investigating the biological functions of CDK2 in cancer research and therapeutic applications. -
Molecular Glues
CDK12 ligand-3 is a molecular glue that effectively targets and degrades the CDK12 protein, with a DC50 of 35 nM. This compound also influences the degradation of CDK13 and its regulatory partner, Cyclin K, while inhibiting serine 2 phosphorylation of the RNA polymerase II CTD. CDK12 ligand-3 demonstrates significant anti-proliferative effects on Jurkat cells and is applicable in cancer research, particularly in the study of leukemia. -
CDK9 Degrader
PROTAC CDK9 degrader-8 is a potent degrader targeting CDK9, exhibiting an IC50 value of 0.01 μM. This compound effectively induces the degradation of CDK9, making it a valuable tool for investigating the role of CDK9 in cancer biology and therapeutic resistance. It is suitable for use in studies aimed at understanding the mechanisms of tumor progression and exploring potential treatment strategies. -
CDK12/CDK13 Inhibitor/CycK Molecular Glue Degrader
SR-5037 is an orally active inhibitor of CDK12 and CDK13, with an IC50 of 31 nM, and functions as a molecular glue degrader for CycK, demonstrating a DC50 of 30 nM and Dmax exceeding 98%. By inhibiting the enzymatic activity of the CDK12/CycK and CDK13/CycK complexes, SR-5037 facilitates the recruitment of DDB1, leading to proteasome-mediated degradation of CycK. This compound has shown efficacy in degrading active CycK in mouse models of triple-negative breast cancer and is a valuable tool for investigating treatment options in such malignancies. -
CDK2/4/6 PROTAC Degrader
PROTAC CDK2/4/6 Degrader-1 is a potent orally bioavailable degrader targeting CDK2, CDK4, and CDK6 through the proteolysis-targeting chimera (PROTAC) mechanism. This compound functions by facilitating the ubiquitination and degradation of these cyclin-dependent kinases, thereby inhibiting their activity. Its applications extend to the study of malignant melanoma, providing valuable insights into tumor biology and potential therapeutic interventions. This degrader is synthesized as a prodrug from PROTAC CDK2/4/6 Degrader-2, enabling enhanced functionality in biological systems. -
CDKs PROTAC Degrader
TMX-2138 is a potent CDKs PROTAC degrader that achieves IC50 values of 8.7 nM for CDK1/cyclinB, 10.9 nM for CDK2/cyclinA, 7.0 nM for CDK5/p25, and 25.7 nM for CDK9/cyclinT1. This compound facilitates the ubiquitination and subsequent degradation of cyclin-dependent kinases (CDKs), making it a valuable tool for investigating their roles in cellular processes. TMX-2138 is particularly relevant for research focused on ovarian cancer, enabling the study of CDK-targeted therapies and their potential therapeutic implications. -
CDK9 Degrader/Ligands for Target Protein for PROTAC
(R)-PROTAC CDK9 ligand-1 is a potent degrader targeting cyclin-dependent kinase 9 (CDK9), a key regulator of transcription and cell cycle progression. This compound facilitates the synthesis of PROTACs (proteolysis-targeting chimeras), which exhibit antitumor activity by promoting the degradation of CDK9. Research applications include investigations into cancer biology and therapeutic strategies aimed at modulating CDK9 levels for improved treatment outcomes. -
PROTAC USP7 Degrader
PROTAC USP7 Degrader-2 targets the ubiquitin-specific protease 7 (USP7) and functions as a selective degrader. Demonstrating a DC50 of 1.91 μM in TE-12 cells, this compound effectively inhibits the migration of upper gastrointestinal tract cancer cells, although its anti-proliferative activity is relatively modest. PROTAC USP7 Degrader-2 is valuable for research focused on metastatic upper gastrointestinal cancer, aiding in the exploration of therapeutic strategies targeting USP7. -
MNK1 PROTAC Degrader
PROTAC MNK1 degrader-1 is a selective degrader that targets MNK1, exhibiting a DC50 of 11.92 nM and a Dmax exceeding 96% in MV4-11 cells. This compound effectively reduces phosphorylated eIF4E levels (IC50: 22.07 nM), triggers apoptosis, and causes G1 phase cell cycle arrest. With demonstrated potent antitumor activity, PROTAC MNK1 degrader-1 also shows robust antileukemic efficacy in MV4-11 xenograft mouse models while maintaining acceptable drug safety profiles. -
SARS-CoV-2 Mpro PROTAC degrader
HP211206 is a PROTAC degrader targeting the main protease (Mpro) of SARS-CoV-2, designed to selectively degrade both the protease and its drug-resistant variants. This compound demonstrates an IC50 of 181.9 nM and a DC50 of 621 nM, reflecting its potency in disrupting viral replication. HP211206 also exhibits antiviral activity, making it a valuable tool for research aimed at understanding and combating SARS-CoV-2 infections.
