Catalog No.
Product Name
Application
Product Information
Citations
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ADC/PROTAC Linker
Bis-PEG2-PFP ester is a non-cleavable linker that comprises two units of polyethylene glycol (PEG) and is essential for the synthesis of antibody-drug conjugates (ADCs). Its unique structure makes it suitable for use in peptide-based PROTACs (Proteolysis Targeting Chimeras), facilitating targeted degradation of specific proteins. This reagent supports advanced research in the fields of targeted therapy and protein regulation. -
ADC/PROTAC Linker
m-PEG9-Amine 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 attachment of biomolecules, enabling targeted protein degradation and precise delivery of therapeutic agents. m-PEG9-Amine is essential for advancing research in targeted therapy and bioconjugation applications. -
ADC/PROTAC Linker
Bis-PEG17-NHS ester is a PEG-based linker designed for efficient conjugation in both PROTAC and antibody-drug conjugate (ADC) synthesis. Its NHS ester functionality allows for selective coupling to amine-containing molecules, facilitating the development of targeted therapies. This reagent is particularly useful in the development of PROTACs for targeted protein degradation and in the construction of ADCs that deliver cytotoxic agents to specific cancer cells. -
ADC/PROTAC Linker
N-Boc-PEG9-alcohol is a polyethylene glycol (PEG)-based linker utilized in the synthesis of antibody-drug conjugates (ADCs) and PROTACs. This cleavable linker facilitates the conjugation of bioactive molecules, enhancing the pharmacokinetic properties of ADCs. Its application extends to the development of targeted degraders, making it a valuable tool in chemical biology and drug discovery research. -
PROTAC Linkers
N-Succinimidyl 3-(Bromoacetamido)propionate is a versatile PEG-based linker designed for PROTAC (proteolysis-targeting chimeras) synthesis. This compound facilitates the effective conjugation of small molecules to target proteins, enabling targeted protein degradation. Additionally, it serves as a cleavable linker for the development of antibody-drug conjugates (ADCs), enhancing therapeutic efficacy in cancer research. This reagent is essential for studies focused on protein modulation and targeted therapies. -
ADC/PROTAC Linker
DBCO-NHCO-PEG4-acid is a PEG-based linker designed for application in antibody-drug conjugates (ADCs) and PROTAC synthesis. This linker features a DBCO group that participates in strain-promoted alkyne-azide cycloaddition (SPAAC), facilitating selective conjugation with azide-containing molecules. Its chemical properties make it ideal for developing targeted therapeutics that can modulate protein levels in biological research, enhancing experimental outcomes in drug discovery and development. -
PROTAC Linker
5-Hydroxypentanoic acid serves as a versatile PROTAC linker, playing a crucial role in targeted protein degradation technology. This compound facilitates the synthesis of PROTAC AR-V7 degrader-1, contributing to innovative research in protein regulation and therapeutic development. Its structural characteristics enhance the design of bifunctional molecules for selective protein degradation, making it a valuable reagent in life sciences research. -
ADC/PROTAC Linker
Amino-PEG10-OH is a non-cleavable, 10-unit polyethylene glycol (PEG) linker primarily utilized in the development of antibody-drug conjugates (ADCs). This versatile linker also serves a critical role in the synthesis of proteolysis-targeting chimeras (PROTACs). Its hydrophilic properties enhance solubility and stability, making it suitable for diverse applications in chemical biology and therapeutic development. -
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. -
eDHFR PROTAC
PROTAC eDHFR Degrader-2 selectively targets Escherichia coli dihydrofolate reductase (eDHFR) for degradation. By utilizing a PROTAC mechanism, this compound efficiently promotes the degradation of eDHFR-tagged proteins, making it a valuable tool for studies in protein regulation and degradation pathways. Its ability to modulate protein levels can aid in the investigation of various biological processes and contribute to the development of therapeutic strategies. -
CCR2 PROTAC Degrader
LUF7996 is a potent CCR2 PROTAC degrader that selectively targets and degrades CCR2 with a DC50 value of 2.6 μM. This compound effectively engages with the E3 ligase cereblon, promoting sustained and concentration-dependent degradation of CCR2 via the lysosomal pathway. LUF7996 is particularly valuable for research applications involving the inhibition of monocyte migration in vitro, facilitating studies in inflammation and immune response modulation. -
PROTAC Degrader
FC-14367 is a PROTAC degrader that selectively targets the HIV-1 Nef protein. It facilitates the formation of a ternary complex by simultaneously binding to Nef and Cereblon E3 ubiquitin ligase, leading to the ubiquitination and subsequent proteasomal degradation of Nef. This process restores the surface expression of CD4 and MHC-I molecules while effectively inhibiting HIV-1 replication. FC-14367 is valuable for research focused on HIV infection and AIDS pathogenesis. -
Ligands for E3 Ligase
Nef ligand-2 is a specific ligand for the Nef protein, functioning primarily as a binder that targets E3 ligases. It plays a crucial role in modulating protein interactions and degradation pathways, offering valuable insights into Nef-related signaling mechanisms. This compound is particularly relevant in research applications focused on HIV pathogenesis and the exploration of therapeutic strategies targeting E3 ligase activity. -
E3 Ligase Ligand-linker Conjugate
E3 Ligase Ligand-linker Conjugate 214 is an innovative E3 ligase ligand-linker conjugate featuring a Von Hippel-Lindau (VHL) ligand. This compound effectively binds to target proteins, facilitating the formation of PROTAC (Proteolysis Targeting Chimeras) molecules, such as the PROTAC LSD1 Degrader 1. Its application in targeted protein degradation research supports the development of novel therapeutic strategies in cancer and other diseases. -
E3 Ligase Ligand and PROTAC Linker
(S)-Deoxy-thalidomide-2,7-diazaspiro[3.5]nonane-CH2-Me-PIP-Boc serves as an E3 ligase ligand and a PROTAC linker, facilitating targeted protein degradation. It is integral to the development of PROTAC K-Ras Degrader-3, demonstrating potential in cancer research. This compound is designed to help elucidate molecular mechanisms and therapeutic pathways involved in oncogenesis. -
ASK1 PROTAC Degrader
dASK1 is a selective PROTAC degrader targeting apoptosis signal-regulating kinase 1 (ASK1) through a cereblon (CRBN)-mediated pathway. This compound forms a stable ternary complex with ASK1, promoting its efficient degradation via the ubiquitin-proteasome system. dASK1 exhibits potent activity in degrading ASK1 and serves as a valuable tool in research focused on steatohepatitis and related pathologies. -
MYC Molecular Glues Degrader
MYC Degrader 1 is a potent molecular glue degrader that targets the MYC oncogene, facilitating the degradation of MYC proteins. This compound exhibits significant anti-tumor activity by restoring the functionality of the pRB1 protein, thereby reinstating the sensitivity of MYC-overexpressing cancer cells to CDK4/6 inhibitors. MYC Degrader 1 is suitable for research applications focusing on cancer therapeutics and the modulation of MYC-driven signaling pathways. -
CDK9 PROTAC Degrader
KI-CDK9d-32 is a selective and potent degrader designed to target CDK9 through a PROTAC mechanism (DC50: 0.89 nM). It facilitates the ubiquitination and subsequent degradation of CDK9, effectively inhibiting the MYC signaling pathway and disrupting nucleolar homeostasis. This compound demonstrates significant anticancer activity, particularly against acute lymphoblastic leukemia and pancreatic cancer, making it a valuable tool for research in cancer biology and therapeutic development. -
DAPK1 PROTAC Degrader
PROTAC DAPK1 Degrader-1 selectively targets DAPK1 for degradation, exhibiting a DC50 value of 119.6 nM. This compound has been shown to elevate MDM2 protein levels while concurrently decreasing cleaved caspase-3 and cleaved PARP levels in a neurotoxin-induced cell apoptosis model. Its ability to effectively inhibit neuronal apoptosis positions PROTAC DAPK1 Degrader-1 as a valuable tool for investigating neurological disorders, including cerebral ischemia and traumatic brain injury. -
PROTAC Degrader for FKBP12
22-SLF is a PROTAC degrader specifically targeting FK506-binding protein 12 (FKBP12), exhibiting a DC50 of 0.5 µM. This compound forms a ternary complex with C227 and C228 in FBXO22, facilitating FKBP12 degradation in an FBXO22-dependent manner. 22-SLF is a valuable tool for cancer research, serving as a probe to investigate the FBXO22-mediated degradation pathways. -
Ligands for Target Protein for PROTAC
POI ligand-2 is a specific ligand for the GPX4 protein, facilitating targeted protein degradation. This compound is instrumental in the synthesis of PROTACs, including PROTAC GPX4 degrader-5. Its application in protein research enables efficient modulation of GPX4 levels, aiding studies in mechanistic biology and therapeutic interventions targeting oxidative stress pathways. -
EZH2 PROTAC
PROTAC EZH2 Degrader-41 is a PROTAC designed to target EZH2 by recruiting cIAP E3 ubiquitin ligase. This compound facilitates the ubiquitination and subsequent proteasomal degradation of EZH2, thereby exerting significant antiproliferative effects in lymphoma cells. PROTAC EZH2 Degrader-41 is a valuable tool for investigating the role of EZH2 in lymphoma research and its potential as a therapeutic target. -
PROTAC MDM2 degrader
YX-02-030 is a PROTAC MDM2 degrader that effectively inhibits the MDM2-p53 interaction with an IC50 value of 63 nM, as well as the VHL-HIF1α binding, with an IC50 of 1.35 μM. By binding to MDM2, it recruits the VHL E3 ubiquitin ligase, promoting MDM2 degradation. This compound is particularly relevant in researching therapeutic strategies against p53 mutant or deleted triple-negative breast cancer (TNBC) cells. -
TAF1 PROTAC Degrader
ZS3-046 is a TAF1 PROTAC degrader that facilitates the ubiquitination and subsequent degradation of the TAF1 protein. This compound effectively activates p53, leading to apoptosis in acute myeloid leukemia (AML) cells. In vivo studies have demonstrated its antitumor efficacy in AML tumor xenograft mouse models, making ZS3-046 a valuable tool for researching targeted degradation strategies in cancer therapy. -
MDM2 Degrader
MD-265 is a potent MDM2 degrader utilizing the PROTAC (PROteolysis TArgeting Chimeras) technology. It effectively promotes the degradation of MDM2, resulting in the reactivation of the p53 tumor suppressor pathway in cancer cells with wild-type p53. Preclinical studies demonstrate that MD-265 induces complete tumor regression and enhances long-term survival in leukemia models, making it a valuable tool for cancer research and therapeutic development. -
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.
