PROTAC

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  1. PROTAC erf3a Degrader

    PROTAC erf3a Degrader-2 (Compound C59) is an orally active PROTAC designed to target and degrade eRF3a (GSPT1) and SRD5A3 proteins. By inducing the ubiquitination and subsequent proteasomal degradation of these proteins, it effectively inhibits cancer cell proliferation in various models, including the 22Rv1 prostate cancer cell line. PROTAC erf3a Degrader-2 is applicable for research related to multiple cancer types, including prostate, ovarian, liver, cervical, and breast cancers, as well as leukemia.
  2. SMARCA2/4 Degrader

    PROTAC SMARCA2/4-degrader-3 is a potent SMARCA2/4 degrader that utilizes the VH032-NH2 framework for targeted protein degradation. It exhibits a degradation potency (DC50) of less than 100 nM in MV4-11 cells, facilitating the selective depletion of SMARCA2 and SMARCA4 proteins. This compound is valuable for research applications involving chromatin remodeling and cancer biology, providing insights into the functional roles of these proteins in various cellular contexts.
  3. SMARCA2/4 PROTAC degrader

    PROTAC SMARCA2/4-degrader-1 is a PROTAC degrader specifically designed to target SMARCA2 and SMARCA4 proteins. It effectively degrades these proteins in A549 cells, exhibiting a DC50 of less than 100 nM and achieving over 90% degradation after 24 hours of treatment. This compound is suitable for research applications focused on understanding the role of SMARCA2 and SMARCA4 in various biological processes and disease models.
  4. SRC-1 Degrader/PROTAC

    ND1-YL2 is a PROTAC that selectively targets and degrades SRC-1 through the N-degron pathway. This compound has demonstrated significant inhibition of cancer cell invasion and migration both in vitro and in vivo. ND1-YL2 serves as a valuable tool in cancer research, providing insights into the role of SRC-1 in tumor progression and metastasis.
  5. SMARCA2/4 PROTAC degrader

    PROTAC SMARCA2/4-degrader-2 is a molecular degrader specifically designed to target SMARCA2 and SMARCA4 proteins. It effectively induces degradation of these proteins in A549 cell lines with degradation concentrations (DC50s) less than 100 nM, achieving a maximum degradation rate (Dmax%) exceeding 90% after 24 hours of exposure. This compound is valuable for investigating the roles of SMARCA2 and SMARCA4 in various biological processes and may have applications in cancer research and therapeutic development.
  6. SMARCA2 PROTAC degrader

    PROTAC SMARCA2 degrader-13 is a novel PROTAC targeted at the degradation of SMARCA2 proteins. This compound effectively induces the degradation of SMARCA2 in A549 cells with a DC50 of less than 100 nM, achieving over 90% degradation after 24 hours of treatment. It serves as a valuable tool for studying the functional role of SMARCA2 in cancer biology and other cellular processes.
  7. AR PROTAC Degrader

    PROTAC AR Degrader-5 is a potent androgen receptor (AR) PROTAC degrader, exhibiting an IC50 value of 49 nM. This compound facilitates the targeted degradation of AR, demonstrating significant potential in inhibiting sebaceous plaque formation and promoting hair regeneration. Its mechanism utilizes a bifunctional ligand to recruit an E3 ligase, making it a valuable tool for research in androgen signaling and related therapeutic applications.
  8. SMARCA2/4 PROTAC degrader

    PROTAC SMARCA2/4-degrader-33 (compound I-277) is a targeted protein degradation compound that engages and induces degradation of SMARCA2 and SMARCA4. It demonstrates effective biological activity in A549 cells, with degradation concentrations (DC50s) below 100 nM, achieving over 90% protein degradation (Dmax%) after 24 hours of treatment. This reagent is suitable for research applications involving epigenetic regulation and cancer biology.
  9. SMARCA2 PROTAC degrader

    PROTAC SMARCA2 degrader-9 (compound I-285) is an innovative PROTAC agent designed to selectively degrade SMARCA2 proteins. It demonstrates potent biological activity with a DC50 value of less than 100 nM, achieving over 90% degradation of SMARCA2 in A549 cell lines after 24 hours of treatment. This compound serves as a valuable tool for research applications aimed at elucidating the role of SMARCA2 in cancer biology and exploring targeted protein degradation strategies.
  10. YN14 Mixture of Diastereomers

    YN14 is a mixture of diastereomers that functions as a proteolysis targeting chimera (PROTAC) specifically targeting KRASG12C. This compound exhibits high potency and selectivity in degrading KRASG12C by forming a stable ternary complex with VHL, characterized by low binding free energy (ΔG). YN14 demonstrates significant antiproliferative activity, effectively inhibiting the growth of KRASG12C-mutant cancer cells, making it a valuable tool for cancer research and drug development.
  11. PRT3789 Epimer

    PRT3789 epimer is an epimer of PRT3789, a selective degrader targeting SMARCA2 through the PROTAC approach. This compound facilitates the ubiquitination and subsequent proteasomal degradation of SMARCA2, thereby providing a valuable tool for studying the role of this protein in cancer and other diseases. It is essential for research applications focused on targeted protein degradation mechanisms and their therapeutic implications.
  12. PROTAC BCR-ABL Degrader

    SNIPER(ABL)-020 is a PROTAC compound designed to selectively degrade the BCR-ABL fusion protein through targeted ubiquitin-proteasome pathway engagement. By conjugating Dasatinib, an ABL inhibitor, with Bestatin, an IAP ligand, SNIPER(ABL)-020 effectively promotes the protein's ubiquitination and subsequent degradation. This reagent is valuable for research focused on chronic myeloid leukemia and BCR-ABL related signaling pathways, offering insights into targeted protein degradation mechanisms in cancer therapeutics.
  13. PROTAC ER Degrader

    SNIPER(ER)-87 is a PROTAC compound designed to efficiently degrade estrogen receptor α (ERα) through targeted ubiquitination. It consists of an IAP ligand (LCL161 derivative) linked to the ERα ligand (4-hydroxytamoxifen) via a PEG linker, resulting in an IC50 of 0.097 μM for ERα degradation. This compound preferentially recruits XIAP, the primary E3 ubiquitin ligase, to facilitate the selective degradation of ERα in cellular contexts. SNIPER(ER)-87 is valuable for research on hormone receptor regulation, breast cancer studies, and the development of targeted protein degradation strategies.
  14. SNIPERs

    BzNH-BS is a bifunctional reagent designed to target the cellular inhibitor of apoptosis protein 1 (cIAP1) through its ligand methyl-bestatin (MeBS) and a benzoyl-amide. This compound operates as a SNIPER (Specific and Non-genetic IAP-dependent protein Eraser) to promote the ubiquitination and subsequent degradation of cIAP1. BzNH-BS is useful in studying apoptosis regulation and can be applied in cancer research to explore IAP-related pathways and therapeutic interventions.
  15. PROTAC ER Degrader

    SNIPER(ER)-110 is a PROTAC compound designed for targeted degradation of the estrogen receptor (ER). Comprising an IAP ligand and an estrogen ligand linked together, SNIPER(ER)-110 effectively induces ER protein degradation, exhibiting DC50 values of less than 3 nM at 4 hours and approximately 7.7 nM at 48 hours. This reagent is valuable for studies investigating ER-related signaling pathways and therapeutic strategies in hormone-dependent cancers.
  16. Target Protein Ligand-Linker Conjugates

    K-Ras ligand-Linker Conjugate 6 is designed to selectively target K-Ras through its ligand-recruiting moiety, while featuring a PROTAC linker that facilitates the recruitment of E3 ligases such as VHL, CRBN, MDM2, and IAP. This compound is instrumental in the synthesis of PROTAC K-Ras Degrader-1, a potent degrader that demonstrates at least 70% degradation efficacy in SW1573 cells. Its unique properties make it an essential tool for researchers studying K-Ras signaling and targeted protein degradation in cancer biology.
  17. Target Protein Ligand-Linker Conjugates

    BMS-1166-N-piperidine-CO-N-piperazine dihydrochloride is a compound designed for the synthesis of Protein Targeting Chimeras (PROTACs) targeting the PD-1/PD-L1 immune checkpoint. It features a ligand that facilitates binding to PD-1/PD-L1 and includes a PROTAC linker for degradation of target proteins. This compound can be utilized in the development of PROTAC PD-1/PD-L1 degrader-1, which effectively inhibits PD-1/PD-L1 interactions with an IC50 of 39.2 nM, making it a valuable tool for cancer immunotherapy research.
  18. Target Protein Ligand-Linker Conjugates

    Desmorpholinyl Quizartinib-PEG2-COOH is a conjugate designed for targeted protein degradation, specifically targeting the FLT-3 receptor. This compound incorporates a FLT-3 ligand and a PEG-based PROTAC linker, facilitating the synthesis of PROTAC FLT-3 degrader 1, which effectively degrades FLT-3 internal tandem duplication (ITD) variants with an IC50 of 0.6 nM. This reagent is valuable for research applications focusing on targeted therapy and protein degradation mechanisms in hematological malignancies.
  19. Target Protein Ligand-Linker Conjugates

    FAK ligand-Linker Conjugate 1 is designed to target Focal Adhesion Kinase (FAK) using a PROTAC linker that recruits E3 ligases, including VHL, CRBN, MDM2, and IAP. This compound facilitates the targeted degradation of proteins through the PROTAC mechanism. Its primary applications include studies in targeted protein degradation and the modulation of FAK-related signaling pathways in various biological contexts.
  20. Target Protein Ligand-Linker Conjugates

    K-Ras ligand-Linker Conjugate 5 is designed to target the K-Ras protein through a ligand and incorporates a PROTAC linker that facilitates the recruitment of E3 ligases, including VHL, CRBN, MDM2, and IAP. This compound serves as a vital component in the synthesis of PROTAC K-Ras Degrader-1, a robust degrader that demonstrates ≥70% degradation efficacy in SW1573 cells. Its application in targeted protein degradation research makes it a valuable tool for investigating K-Ras-related pathways in oncology.
  21. Target Protein Ligand-Linker Conjugates

    K-Ras ligand-Linker Conjugate 3 is designed to selectively target K-Ras through its ligand, combined with a PROTAC linker that facilitates the recruitment of E3 ligases such as VHL, CRBN, MDM2, and IAP. This reagent is instrumental in the development of PROTAC-based degraders, particularly in the synthesis of PROTAC K-Ras Degrader-1, which demonstrates significant degradation efficacy of ≥70% in SW1573 cells. This compound is essential for research applications in targeted protein degradation and cancer therapeutics involving K-Ras.
  22. Target Protein Ligand-Linker Conjugate

    USP7 Ligand-Linker Conjugates 1 is a targeted protein ligand-linker conjugate designed to bind to the deubiquitinating enzyme USP7. This compound incorporates a specific USP7 ligand and a PROTAC linker that facilitates the recruitment of E3 ligases for targeted protein degradation. It serves as a crucial component in the synthesis of PROTAC USP7 Degrader-1, enabling researchers to investigate the functional role of USP7 in cellular processes and its potential as a therapeutic target.
  23. Target Protein Ligand-Linker Conjugate

    (Rac)-PROTAC PARP/EGFR ligand 1 is a target protein ligand-linker conjugate that features ligands for both PARP and EGFR, along with a PROTAC linker to facilitate the recruitment of E3 ligases, including VHL, CRBN, MDM2, and IAP. This reagent is instrumental in the advancement of targeted protein degradation strategies in research, enabling the synthesis of DP-C-4, a CRBN-based dual PROTAC designed for the simultaneous degradation of EGFR and PARP. Its application in drug discovery highlights its utility in elucidating the roles of these critical proteins in cancer biology.
  24. Target Protein Ligand-Linker Conjugates

    K-Ras ligand-Linker Conjugate 2 is designed to specifically target K-Ras by integrating a selective ligand with a PROTAC linker that facilitates the recruitment of E3 ligases, including VHL, CRBN, MDM2, and IAP. This conjugate serves as a critical precursor for the synthesis of PROTAC K-Ras Degrader-1, demonstrating significant biological activity by achieving ≥70% degradation efficiency in SW1573 cancer cells. It is a valuable tool for research focused on protein degradation and therapeutic strategies for K-Ras-driven cancers.
  25. Target Protein Ligand-Linker Conjugates

    BMS-1166-N-piperidine-CO-N-piperazine serves as a targeted ligand-linker conjugate for the PD-1/PD-L1 immune checkpoint pathway. This compound is designed to facilitate the synthesis of a PROTAC PD-1/PD-L1 degrader, exhibiting potent inhibition of the PD-1/PD-L1 interaction with an IC50 value of 39.2 nM. Its applications are particularly relevant in cancer research, where modulating immune checkpoint pathways is critical for therapeutic intervention and study of immune evasion mechanisms.
  26. Target Protein Ligand-Linker Conjugates

    K-Ras ligand-Linker Conjugate 1 is designed to target the K-Ras protein through a specific ligand, while also incorporating a PROTAC linker that facilitates the recruitment of E3 ligases such as VHL, CRBN, MDM2, and IAP. This reagent is essential for the synthesis of PROTAC K-Ras Degrader-1, a potent degrader that demonstrates greater than 70% degradation efficacy in SW1573 cells. It serves as a valuable tool for researchers investigating K-Ras-related pathways and exploring targeted protein degradation strategies.
  27. Target Protein Ligand-Linker Conjugates

    K-Ras ligand-Linker Conjugate 4 functions as a targeted protein ligand-linker conjugate designed for K-Ras. This compound incorporates a ligand to effectively recruit K-Ras and a PROTAC linker that interacts with E3 ligases such as VHL, CRBN, MDM2, and IAP. It serves as a synthetic precursor for PROTAC K-Ras Degrader-1, demonstrating significant biological activity with at least 70% degradation efficacy in SW1573 cells. This conjugate is essential for research into targeted protein degradation and the modulation of K-Ras-related pathways.
  28. Target Protein Ligand-Linker Conjugates

    DDR1 ligand 1-piperidine is a target protein ligand and linker conjugate designed for use in the development of PROTACs targeting DDR1. This compound facilitates the synthesis of DDR1 degrader-1, enabling research into targeted protein degradation and modulation of DDR1-related signaling pathways. Its application is crucial for studies exploring the therapeutic potential of DDR1 inhibition in various disease models.
  29. Target Protein Ligand-Linker Conjugates

    FAK ligand-2-C6-amine is a target protein ligand-linker conjugate that incorporates a focal adhesion kinase (FAK) ligand with a PROTAC linker. This compound effectively recruits E3 ligases, facilitating the targeted degradation of specific proteins. FAK ligand-2-C6-amine is valuable in research applications focused on protein regulation and cellular signaling pathways, and it can be utilized in the synthesis of BSJ-04-146, a compound of interest in cancer research.
  30. Conjugate

    Ahx-DM1 is a versatile conjugate designed for the targeted delivery of therapeutic, diagnostic, or labeling agents. By facilitating effective conjugation with proteins or peptides, this compound enhances the specificity and efficacy of treatments in chemical research. Its applications extend to areas such as drug development and imaging, making it an essential tool for advancing biomedical studies and experimental therapies.
  31. Target Protein Ligand-Linker Conjugate

    Remodelin-C6-COOH is a synthesized ligand-linker conjugate designed for conjugation with target proteins. This compound facilitates the synthesis of NP1192, a potent NAT10 PROTAC degrader known for its anti-tumor activity. Remodelin-C6-COOH serves as an essential tool in the development of targeted protein degradation strategies for cancer research.
  32. Target Protein Ligand-Linker Conjugates

    SMARCA2/4 Ligand-Linker Conjugate 2 is a specialized ligand-linker conjugate designed for targeting SMARCA2 and SMARCA4 proteins. This compound facilitates the synthesis of Proteolysis Targeting Chimeras (PROTACs), specifically enabling the development of AU-15330. It is a valuable tool in chemical biology for studying protein degradation pathways and investigating the functional roles of SMARCA family proteins in various cellular processes.
  33. Target Protein Ligand-Linker Conjugate

    JQ-1 (carboxylic acid)-NH-C8-COOH is a synthetic linker designed for conjugation with target proteins. This compound facilitates the synthesis of JQ1-S(GlcNAc)Cq, a bifunctional degrader that exhibits significant anti-tumor activity through its Sugar-Coated PROTAC mechanism. It serves as a valuable tool in chemical research focused on targeted protein degradation and cancer biology applications.
  34. Target Protein Ligand-Linker Conjugate

    AZD9496-O-C3-O-C3-O-C-acid is a targeted protein ligand-linker conjugate that includes a ligand specific for estrogen receptor alpha (ERα) and a PROTAC linker designed to recruit E3 ligases. This compound facilitates the development of PROTAC AZ'6421, enabling researchers to investigate targeted protein degradation pathways. It is applicable in studies focusing on hormone receptor modulation and protein regulation in cellular contexts.
  35. PROTAC E3 Ligases and Linkers

    Adamantane-Butyl alcohol serves as a crucial linker for PROTACs targeting E3 ligases, specifically in the degradation of the CDK8-cyclin C complex. This compound facilitates targeted protein degradation, thereby enhancing the modulation of cellular processes and offering a strategic approach in research applications such as cancer biology and therapeutic development. Its selective and persistent nature makes it an integral component in the design of novel protein degraders.
  36. Target Protein Ligand-Linker Conjugates

    BRAF ligand-Linker Conjugate 1 is a compound designed to target the BRAF protein through a ligand-linker approach. It serves as a crucial precursor for the synthesis of PROTAC CST905, facilitating targeted protein degradation. This reagent is applicable in studies focused on BRAF-related signaling pathways and therapeutic interventions for diseases associated with BRAF mutations.
  37. Target Protein Ligand-Linker Conjugate

    TEAD ligand-Linker Conjugate 1 is a synthetic ligand-linker conjugate designed for the development of PROTACs, specifically for creating PROTAC TEAD degrader-2, which demonstrates potent degradation of the TEAD1 protein. This compound is pivotal for anti-cancer research, facilitating targeted protein degradation to study TEAD1’s role in cancer progression and therapeutic responses. Its application in PROTAC technology presents opportunities for innovative approaches in cancer treatment and molecular biology research.
  38. Conjugate

    Ahx-DM1 TFA is a conjugate designed for the covalent attachment of proteins or peptides to therapeutic, diagnostic, or labeling agents. This compound facilitates the targeted delivery of payloads in biological applications, enhancing the efficacy of treatments. Its structural properties enable effective conjugation, making it suitable for research in drug development and protein engineering.
  39. Target Protein Ligand-Linker Conjugates Chemical

    BRD4 ligand-Linker Conjugate 1 is a ligand-linker conjugate specifically designed for targeting the BRD4 protein. This compound plays a crucial role in the synthesis of Proteolysis Targeting Chimeras (PROTACs), facilitating targeted protein degradation. Its application is instrumental in studying BRD4-related signaling pathways and advancing drug discovery efforts in cancer and other diseases associated with epigenetic dysregulation.
  40. E3 Ligase Ligand-Linker Conjugates

    DCAF11 ligand-Linker Conjugate 1 is a conjugate designed to facilitate targeted protein degradation through the DCAF11 E3 ubiquitin ligase. This compound serves as a key component for synthesizing PROTAC LGF308, enabling the selective degradation of specific proteins within cellular systems. Its utility in research applications includes the exploration of protein degradation pathways and investigating therapeutic targets in cancer and other diseases.
  41. Ligand-Linker Conjugate

    N-Descyclopropanecarbaldehyde Olaparib suberic acid is a ligand-linker conjugate designed for the synthesis of DDO3602. This compound functions as a crucial intermediate, facilitating the development of targeted therapeutics that leverage olaparib’s mechanism of action. Its versatility makes it relevant for applications in drug discovery and conjugation chemistry in the context of cancer research.
  42. BRM2 Degrader

    PROTAC SMARCA2 degrader-1 is a targeted degrader designed to selectively degrade BRM2 (SMARCA2) with a DC50 value of less than 0.1 μM. This compound functions as an E3 ubiquitin ligase binding linker, facilitating the targeted degradation of specific proteins. Its application in cancer research makes it a valuable tool for elucidating the role of BRM2 in tumor biology and developing potential therapeutic strategies.
  43. PROTAC Linkers

    3-Maleimidopropionic acid is a versatile linker designed for use in the synthesis of PROTACs (Proteolysis Targeting Chimeras). Its maleimide functional group allows for the selective formation of thioether bonds with cysteine residues, facilitating targeted protein degradation. This compound is instrumental in advancing research in cellular signaling pathways and drug discovery by enabling the development of innovative therapeutics.
  44. PROTAC Linker

    Biotin-EDA is an alkyl chain-based linker specifically designed for use in the synthesis of PROTACs (proteolysis-targeting chimeras). This compound facilitates targeted protein degradation by connecting E3 ligases to the protein of interest. Its unique structure enhances the efficiency of PROTAC development, making it a valuable tool in drug discovery and development for therapeutic interventions. Biotin-EDA is particularly useful in studies involving targeted therapeutics and protein regulation mechanisms.
  45. PROTAC linker

    Mal-NH2 TFA is an alkyl chain-based PROTAC linker designed for the synthesis of PROTACs (proteolysis-targeting chimeras). This compound facilitates the development of bifunctional molecules that can selectively target and degrade specific proteins within the cell. Its application is crucial in various research areas, including drug discovery and the investigation of protein function and degradation pathways.
  46. PROTAC Linker

    Biotin-bis-amido-SS-NHS is a versatile PROTAC linker designed for targeted protein degradation applications. This compound facilitates the synthesis of PROTACs by enabling efficient conjugation to target proteins, leveraging the biotin-streptavidin interaction for cellular applications. Its unique structure enhances stability and biocompatibility, making it suitable for diverse research purposes in drug discovery and cellular biology.
  47. PROTAC Linker

    CH2COOH-PEG6-CH2COOH is a polyethylene glycol (PEG)-based linker designed for use in the synthesis of PROTACs (proteolysis targeting chimeras). This compound facilitates the conjugation of target proteins and E3 ligase, enhancing the degradation of specific proteins through the ubiquitin-proteasome pathway. Its application is significant in drug discovery research, particularly in the development of targeted protein degradation therapies.
  48. PROTAC Linker

    Icosane-1,20-diol serves as a versatile PROTAC linker, facilitating the development of proteolysis-targeting chimeras (PROTACs) for targeted protein degradation. Its unique structure enhances the molecular design of PROTACs, optimizing their biological activity and efficacy. This reagent is essential for researchers aiming to explore targeted therapies and investigate protein regulation mechanisms in various biological contexts.
  49. PROTAC Linker

    2-(Benzyloxy)ethanol is a PEG-based PROTAC linker utilized in the synthesis of proteolysis-targeting chimeras (PROTACs). This compound provides a flexible and functional scaffold, facilitating the efficient degradation of target proteins through the ubiquitin-proteasome system. Its application in chemical biology enables researchers to explore targeted protein degradation mechanisms and therapeutic strategies.
  50. PROTAC Linker

    Diethyl nonanedioate, also known as diethyl azelate, serves as a versatile PROTAC linker essential for the synthesis of Proteolysis Targeting Chimeras (PROTACs). This compound facilitates the selective degradation of target proteins via the ubiquitin-proteasome system, enabling researchers to investigate protein function and modulation. Its application in PROTAC development aids in the advancement of targeted therapy strategies in various diseases, including cancer and neurodegenerative disorders.

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