Catalog No.
Product Name
Application
Product Information
Citations
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IKZF2 Selective and orally Inhibitor
PVTX-405 is a selective, orally bioavailable inhibitor targeting IKZF2, designed as a molecular glue degrader. With a DC50 of 0.7 nM and a Dmax of 91%, it enhances degradation efficiency while minimizing off-target effects, exhibiting an IC50 of 48 µM for hERG inhibition. PVTX-405 demonstrates significant antitumor activity by inhibiting the growth of MC38 tumors and shows improved efficacy when combined with immune checkpoint therapies, such as anti-PD1 or anti-LAG3, in mouse models. -
Molecular Glue IKZF2-Degrader
IKZF2-degrader 3 is a molecular glue that selectively targets and degrades the IKZF2 protein, exhibiting a DC50 of 2.0 nM. It enhances the understanding of IKZF2's role in various biological processes and is useful for studying its implications in hematological malignancies. This reagent is valuable for research focused on targeted protein degradation and its therapeutic potential in cancer treatment. -
IKZF1 Degrader
IKZF1-degrader-2 is a molecular glue degrader that specifically targets IKZF1, facilitating its degradation in cancer cells. This compound exhibits potent anticancer activity while demonstrating low toxicity, making it a valuable tool for oncology research. IKZF1-degrader-2 is ideal for studies focused on targeted protein degradation and its therapeutic implications in cancer treatment. -
IKZF2 Degrader
IKZF2-degrader 2 is a selective molecular glue degrader that targets IKZF2, facilitating its ubiquitination and subsequent degradation through recruitment of the CRL4-CRBN E3 ubiquitin ligase. With DC50 values of 0.5 nM and 1.8 nM in HiBit and FACS assays, respectively, this compound also induces moderate degradation of SALL4 (DC50 of 9 nM) without significantly affecting IKZF1, IKZF3, CK1α, or GSPT1. IKZF2-degrader 2 is suitable for investigating mechanisms in cancer immunology. -
IKZF2 Molecular Glue Degrader
IKZF2-degrader 1 is a selective IKZF2 molecular glue degrader that exhibits a DC50 of 0.5 nM, effectively targeting IKZF2 for degradation. With minimal activity against CK1α (DC50: 210 nM), it provides a focused approach for studying the role of IKZF2 in cellular processes. This compound is valuable for researching IKZF2-dependent cancers, enabling investigations into its therapeutic potential and biological mechanisms. -
IKZF2 Degrader
IKZF2-degrader 4 is an IKZF2-targeting compound that facilitates the degradation of the IKZF2 protein. Through its mechanism, this degrader can disrupt the function of IKZF2, which is implicated in various cancer pathways. It is a valuable tool for investigating IKZF2's role in tumor biology and for exploring therapeutic strategies in cancer research. -
IKZF1 Degrader
IKZF1-degrader-1 is a molecular glue degrader targeting IKZF1, with a DC50 value of 0.134 nM. This compound facilitates the selective degradation of IKZF1, making it a valuable tool for research into tumor biology and potential cancer therapies. Its ability to modulate IKZF1 levels may provide insights into the role of this transcription factor in oncogenesis and therapeutic resistance. -
PROTAC IRAK4 Degrader
PROTAC IRAK4 Degrader-3 is a PROTAC-based ligand designed to target and induce the degradation of interleukin-1 receptor-associated kinase 4 (IRAK4) via the von Hippel-Lindau (VHL) E3 ubiquitin ligase. This compound effectively modulates the inflammatory response by selectively degrading IRAK4, making it a valuable tool for exploring therapeutic strategies in inflammatory diseases and immune signaling pathways. Its application in research can provide insights into IRAK4's role in various pathologies, including cancer and autoimmune disorders. -
PROTAC IRAK4 Degrader
PROTAC IRAK4 Degrader-8 is a targeted protein degradation compound designed to selectively degrade IRAK4, demonstrating an IC50 of 15.5 nM. This reagent effectively induces IRAK4 degradation in THP-1 cells with a DC50 of 1.8 nM. Additionally, PROTAC IRAK4 Degrader-8 inhibits L-6 production in human whole blood and LPS-induced human peripheral blood mononuclear cells, exhibiting IC50 values of 246 nM and 2.2 nM, respectively. This compound is a valuable tool for studying the role of IRAK4 in immune responses and offers potential applications in inflammatory and autoimmune research. -
PROTAC IRAK4 Degrader
PROTAC IRAK4 Degrader-5 is a Cereblon-based targeted protein degrader specifically designed to induce the degradation of IRAK4. By modulating the ubiquitin-proteasome system, it enhances protein turnover, leading to a decrease in IRAK4 levels. This compound is valuable for research applications focused on inflammation and immune response regulation, enabling the investigation of IRAK4's role in various disease models. -
PROTAC IRAK4 Degrader
PROTAC IRAK4 degrader-12 is a PROTAC compound designed to selectively target and induce the degradation of IRAK4 via the Cereblon E3 ligase pathway. It demonstrates a significant degradation efficacy, achieving a maximum degradation rate of 108.46% in K562 cells with an IC50 of 4.87 nM. This reagent is particularly useful for research applications focused on inflammatory signaling pathways and therapeutic development targeting IRAK4-related diseases. -
IRAK3 PROTAC Degrader
PROTAC IRAK3 degrader-2 is a potent IRAK3 PROTAC degrader with a DC50 of less than or equal to 50 nM. This compound promotes the ubiquitination and subsequent degradation of the IRAK3 protein, making it a valuable tool for studying immune-related diseases. Its unique design incorporates ligands for E3 ligase and a linker configuration, facilitating targeted degradation and aiding research into therapeutic strategies for modulating immune responses. -
PROTAC IRAK4 Degrader
PROTAC IRAK4 Degrader-2 is a PROTAC-based compound designed to target and degrade IRAK4, displaying potent degradation efficacy with a DC50 value of 151 nM in peripheral blood mononuclear cells (PBMCs). It effectively reduces IRAK4 protein levels, achieving a DC50 of 36 nM in these cells. Additionally, PROTAC IRAK4 Degrader-2 inhibits the production of multiple cytokines, making it a valuable tool for research in inflammation and immune response modulation. -
PROTAC IRAK4 Degrader
KTX-612 is an orally bioavailable IRAK4 PROTAC degrader with a DC50 value of 7 nM. This compound is designed to selectively target and promote the degradation of IRAK4, a key protein involved in inflammatory and oncogenic signaling pathways. KTX-612 has potential applications in oncology research, facilitating studies focused on the modulation of IRAK4 and its implications in cancer progression and treatment. -
IRAK3 Degrader PROTAC
PROTAC IRAK3 degrader-1 is a potent and selective degrader targeting IRAK3, with an IC50 of 5 nM. This compound effectively facilitates the ubiquitination and subsequent degradation of IRAK3, thereby modulating inflammatory responses. Its primary research applications include studies on innate immunity and the development of targeted therapies for inflammatory diseases. -
PROTAC IRAK4 Degrader
PROTAC IRAK4 degrader-4 is a Cereblon-based bifunctional molecule designed to degrade interleukin-1 receptor-associated kinase 4 (IRAK4). This compound facilitates targeted protein degradation, leading to effective modulation of IRAK4 levels in cells. Research applications include investigating inflammatory signaling pathways and therapeutic approaches for autoimmune diseases. -
PROTAC IRAK4 Degrader
KTX-497 is a potent IRAK4 degrader utilizing the PROTAC technology, exhibiting a DC50 value of 3 nM. This compound effectively targets and degrades IRAK4, making it a valuable tool for oncology research. Its mechanism allows for the selective modulation of signaling pathways implicated in cancer progression, facilitating the exploration of novel therapeutic strategies. -
PROTAC IRAK4 Degrader
KTX-955 is a potent IRAK4 degrader that facilitates the targeted degradation of IRAK4 protein. With DC50 values of 5 nM for IRAK4 and 130 nM for Ikaros, this compound demonstrates significant efficacy in modulating signaling pathways involved in tumorigenesis. KTX-955 comprises a CRBN ligand derived from Pomalidomide and a specific ligand targeting IRAK4, making it a valuable tool for research into cancer biology and therapeutic interventions. -
PROTAC IRAK4 Degrader
PROTAC IRAK4 Degrader-10 is a potent IRAK4 degrader that utilizes a Cereblon ligand to initiate targeted protein degradation. It demonstrates remarkable biological activity, achieving a maximum degradation of 95.94% with a DC50 value of 7.68 nM in HEK293 cells. This compound is essential for research applications focused on inflammatory signaling pathways and therapeutic strategies targeting IRAK4. -
PROTAC IRAK4 Degrader
PROTAC IRAK4 Degrader-6 is a Cereblon-based PROTAC designed to selectively degrade interleukin-1 receptor-associated kinase 4 (IRAK4). This compound targets IRAK4 for ubiquitination and subsequent proteasomal degradation, effectively modulating inflammatory signaling pathways. It is utilized in research applications focused on understanding the role of IRAK4 in immune responses and developing novel therapeutic strategies for inflammatory diseases. -
PROTAC K-Ras Degrader
PROTAC K-Ras Degrader-2 is a selective PROTAC degrader designed to target pan-KRAS mutants, exhibiting an IC50 of ≤200 nM against KRAS G12V and RAF1. This compound effectively degrades KRAS G12D in SW620 cells with a DC50 of ≤200 nM and inhibits cell growth in 3D cultures at an IC50 of ≤20 nM. PROTAC K-Ras Degrader-2 is a valuable tool for investigating therapeutic strategies in colorectal cancer research. -
KRAS G12C Degrader
KRAS G12C degrader-1 is a potent degrader targeting the KRAS G12C mutation, exhibiting a DC50 of less than 100 nM. This compound functions as a chaperone-mediated protein degrader (CHAMP), leveraging HSP90 to promote the degradation of KRAS G12C. It is invaluable for cancer research, particularly in studies aimed at delineating the impact of KRAS mutations on tumorigenesis and therapeutic resistance. -
PROTAC SOS1 Degrader
PROTAC SOS1 degrader-5 is a potent PROTAC compound that targets SOS1 for ubiquitin-proteasome mediated degradation. It exhibits strong biological activity, demonstrated by a DC50 value of 13 nM and an IC50 of 5 nM in inhibiting the proliferation of NCI-H358 cells. This reagent is valuable for research applications investigating the role of SOS1 in cancer biology and provides insights into targeted protein degradation strategies. -
KRAS Degrader
KRAS degrader-1 is a selective KRAS degrader that induces targeted proteolysis of KRAS proteins via the autophagy-lysosomal degradation pathway. This compound demonstrates robust biological activity in modulating KRAS signaling, making it a valuable tool for research into KRAS-driven cancers. Its application in understanding the dynamics of protein degradation could provide insights into therapeutic strategies for targeting KRAS-dependent malignancies. -
SOS1 PROTAC Degrader
PROTAC SOS1 degrader-7 is a targeted degradation compound designed to selectively degrade SOS1, a critical regulator in tumorigenesis. This PROTAC exhibits anti-tumor activity by promoting the ubiquitination and subsequent proteasomal degradation of SOS1. It is useful for researchers investigating the effects of SOS1 inhibition in cancer models and exploring potential therapeutic strategies for malignancies involving aberrant SOS1 signaling pathways. -
Target Protein Ligand for PROTAC K-Ras Degrader-3
KRAS ligand 5 is a target protein ligand utilized in the development of PROTAC K-Ras Degrader-3. This compound specifically facilitates the degradation of KRAS mutated proteins, making it a vital tool for research focused on targeted protein degradation. It is particularly relevant in studies addressing KRAS-related oncogenesis and potential therapeutic applications in cancer treatment. -
PROTAC SOS1 Degrader
PROTAC SOS1 degrader-6 is a targeted degradative compound designed to selectively degrade the SOS1 protein through a PROTAC mechanism. By utilizing a ligand for SOS1, an E3 ubiquitin ligase ligand, and an effective linker, this reagent enhances the efficacy of KRASG12C inhibitors. Its application is primarily in the study of KRAS-driven cancers and the exploration of protein homeostasis through targeted protein degradation pathways. -
SOS1 PROTAC Degrader
PROTAC SOS1 degrader-9 is a PROTAC (Proteolysis Targeting Chimeras) compound designed for targeted degradation of the SOS1 protein. It employs a specific ligand to bind SOS1, linking it to an E3 ligase for ubiquitination and subsequent proteasomal degradation. This compound is useful in research applications focused on elucidating SOS1's role in cellular signaling pathways and its implications in disease contexts such as cancer. -
PROTAC SOS1 Degrader
(4S)-PROTAC SOS1 degrader-1 is a selective degrader targeting SOS1 through the PROTAC mechanism. This compound effectively reduces the expression of phosphorylated ERK (pERK) and levels of RAS-GTP in a dose-dependent manner, making it a valuable tool for studying RAS signaling. Its ability to significantly inhibit tumor growth in vivo underscores its potential applications in cancer research and therapy. -
KRAS PROTAC Degrader
PROTAC K-Ras Degrader-6 is a cereblon-based KRAS PROTAC degrader that effectively targets and promotes the degradation of KRAS proteins. With a DC50 of ≤100 nM, it exhibits significant anticancer activity, making it a valuable tool for research in cancer biology. This compound is particularly relevant for studies focusing on KRAS-driven malignancies and the development of targeted therapies that leverage the ubiquitin-proteasome system. -
PROTAC Degrader
LC-2 epimer is a differential isomer of LC-2, functioning as a PROTAC degrader. This compound selectively targets mutant KRAS through its unique linkage of a von Hippel-Lindau (VHL) E3 ligase ligand and the KRAS inhibitor MRTX849. LC-2 epimer is intended for research applications focused on targeted protein degradation and the study of KRAS-related pathways in cancer. -
PROTAC SOS1 Degrader
PROTAC SOS1 Degrader-10 is a novel PROTAC compound designed to target and degrade the son of sevenless 1 (SOS1) protein via a cereblon (CRBN) and proteasome-dependent pathway. It effectively reduces SOS1 levels in KRAS mutant cancer cell lines, including SW620, A549, and DLD-1, with DC50 values of 2.23, 1.85, and 7.53 nM, respectively. In addition to inducing degradation, PROTAC SOS1 Degrader-10 also inhibits cell proliferation in these models, displaying IC50 values of 36.7, 52.2, and 107 nM. Furthermore, it inhibits ERK phosphorylation, highlighting its potential role in cancer research and therapeutic applications targeting the RAS signaling pathway. -
PROTAC SOS1 Degrader
PROTAC SOS1 degrader-3 is a targeted protein degradation compound that selectively promotes the degradation of SOS1 via the ubiquitin-proteasome pathway. This degrader exhibits potent activity in downregulating SOS1, a key player in RAS signaling pathways. It is useful for researchers studying the roles of SOS1 in cancer biology and therapeutic interventions that disrupt aberrant signaling associated with this target. -
SOS1 PROTAC Degrader
PROTAC SOS1 degrader-8 is a PROTAC-based molecule designed to target and degrade the SOS1 protein. By utilizing a specific SOS1 ligand, a linker, and an E3 ligase ligand, this compound promotes the ubiquitination and subsequent proteasomal degradation of SOS1. Its primary biological activity involves the modulation of downstream signaling pathways associated with oncogenic processes. This reagent is suitable for research applications focused on elucidating the role of SOS1 in cancer biology and exploring novel therapeutic strategies. -
PROTAC SOS1 degrader
PROTAC SOS1 degrader-1 is a targeted degrader that effectively induces the degradation of SOS1, with an observed DC50 value of 98.4 nM. This compound exhibits significant antiproliferative activity against cancer cells harboring various KRAS mutations. Additionally, PROTAC SOS1 degrader-1 demonstrates notable antitumor effects while maintaining low toxicity, making it a valuable tool for research in cancer therapeutics. -
PROTAC SOS1 Degrader
SIAIS562055 is a cereblon-based PROTAC targeting the SOS1 protein, exhibiting a dissociation constant (Kd) of 95.9 nM. This compound effectively induces degradation of SOS1, leading to downstream inhibition of ERK signaling pathways. Notably, SIAIS562055 blocks the interaction of KRASG12C and KRASG12D with SOS1, with IC50 values of 95.7 nM and 134.5 nM, respectively. Its potent anticancer activity makes it a valuable tool for research in cancer biology and therapeutic development. -
BCL6 Degrader
BMS-986458 is a selective cereblon-based BCL6 degrader that exerts antitumor effects through the targeted degradation of the BCL6 protein. By binding to cereblon and interacting with the BTB domain of BCL6, it modulates key pathways such as cell cycle regulation, antiproliferative signals, and interferon responses, while also enhancing CD20 expression and distribution. BMS-986458 influences follicular helper T cell physiology and reduces circulating tumor DNA levels. Its combination with CD20xCD3 bispecific antibodies has been shown to improve T cell infiltration and expansion in tumors. This compound is applicable in research related to B-cell non-Hodgkin lymphoma, diffuse large B-cell lymphoma, follicular lymphoma, and relapsed/refractory lymphoma. -
PROTAC BCL6 Degrader
PROTAC BCL6 Degrader-3 is a selective degrader targeting the BCL6 protein through the proteolysis-targeting chimera (PROTAC) approach. This compound mediates the ubiquitination and subsequent degradation of BCL6, facilitating the modulation of pathways associated with cancer and autoimmune diseases. It serves as a valuable tool for researchers exploring therapeutic strategies aimed at BCL6 inhibition and the underlying mechanisms of related diseases. -
BCL-6 PROTAC Degrader
BCL6-760 is an orally active BCL-6 PROTAC degrader that selectively targets and degrades BCL-6 with an EC50 of 0.8 nM, without affecting other CRBN substrates. This compound exhibits notable efficacy in orthotopic xenograft mouse models of OCI-LY-1 tumors. BCL6-760 serves as a valuable tool for investigating diffuse large B-cell lymphoma (DLBCL) and for exploring mechanisms related to BCL-6 signaling pathways in cancer research. -
BCL6 PROTAC
BCL6 PROTAC 1 is a selective proteolysis targeting chimera (PROTAC) that targets B-cell lymphoma 6 (BCL6) for degradation. It exhibits potent inhibitory activity on BCL6 cell reporter assays, with an IC50 value of 8.8 µM. This reagent effectively induces degradation of BCL6 in diffuse large B-cell lymphoma (DLBCL) cell lines, making it a valuable tool for tumor-related research applications. -
α1A-AR Degrader
α1A-AR Degrader 9c is a selective, reversible degrader specifically targeting the α1A-adrenergic receptor (α1A-AR) through the proteasomal degradation pathway. It demonstrates significant biological activity, inhibiting the proliferation of PC-3 cells with an IC50 value of 6.12 μM. This compound is valuable for research applications in prostate cancer, providing insights into the therapeutic potential of α1A-AR degradation in oncology studies. -
PROTAC BRD4 Degrader
L134 is a potent PROTAC BRD4 degrader that targets BRD4 for ubiquitination and subsequent degradation via the ubiquitin-proteasome pathway, demonstrating a DC50 value of 7.36 nM. This compound operates in a DCAF11-dependent manner, making it a valuable tool for studying BRD4-related signaling and therapeutic applications in cancer and other diseases. As a versatile reagent, L134 supports research in targeted protein degradation and the modulation of gene expression pathways. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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.
